Search Result
Results for "
first-in-class
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-18233
-
|
E1210; APX001A
|
Fungal
|
Infection
|
|
Manogepix (E1210) is a first-in-class, broad-spectrum and orally active antifungal. Manogepix has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis .
|
-
-
- HY-139399
-
|
JNJ-67856633
|
MALT1
|
Cancer
|
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Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis .
|
-
-
- HY-141680
-
CPS2
1 Publications Verification
|
PROTACs
CDK
|
Cancer
|
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CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia .
|
-
-
- HY-109123
-
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TAK-935; OV935
|
Cytochrome P450
|
Neurological Disease
|
|
Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, and orally active cholesterol 24-hydroxylase (CH24H) inhibitor. Soticlestat has the potential for epilepsy syndromes research .
|
-
-
- HY-149831
-
|
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FXR
|
Metabolic Disease
|
ZLY28 is the first-in-class intestinal restricted and orally active FXR and FABP1 dual modulator. ZLY28 also is a novel anti-NASH agent. ZLY28 can be used for the research of nonalcoholic steatohepatitis (NASH) .
|
-
-
- HY-139535
-
|
CG-806
|
FLT3
Btk
Apoptosis
|
Cancer
|
|
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .
|
-
-
- HY-132283
-
PF-9363
1 Publications Verification
CTx-648
|
Histone Acetyltransferase
|
Cancer
|
|
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer .
|
-
-
- HY-132309
-
BRD0639
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
|
-
-
- HY-P9927
-
|
Ain457
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis .
|
-
-
- HY-108024A
-
|
KAF156 hydrochloride; GNF156 hydrochloride
|
Parasite
|
Infection
|
|
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite .
|
-
-
- HY-109058
-
|
QGC001; RB150
|
Aminopeptidase
|
Cardiovascular Disease
|
|
Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .
|
-
-
- HY-109017
-
-
-
- HY-109025A
-
|
Baloxavir acid; S-033447
|
Influenza Virus
|
Infection
Cancer
|
|
Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity .
|
-
-
- HY-115881
-
|
|
PROTACs
|
Cancer
|
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SR-1114 is a first-in-class PROTAC ENL degrader. SR-1114 elicits rapid, CRBN-dependent degradation of ENL with DC50s of 150 nM, 311 nM, and 1.65 μM in MV4;11 , MOLM-13, and OCI/AML-2 cells, respectively .
|
-
-
- HY-100025A
-
-
-
- HY-101772
-
-
-
- HY-18690A
-
-
-
- HY-109160
-
|
CAD-1883
|
Potassium Channel
|
Neurological Disease
|
|
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA) .
|
-
-
- HY-100025
-
-
-
- HY-138684
-
-
-
- HY-138684A
-
-
-
- HY-12814A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
-
- HY-12814
-
TH588
2 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
-
- HY-138630
-
-
-
- HY-114419
-
|
KZR-616
|
Proteasome
|
Inflammation/Immunology
|
|
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases .
|
-
-
- HY-114419A
-
|
KZR-616 maleate
|
Proteasome
|
Inflammation/Immunology
|
|
Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate has the potential for the research of multiple autoimmune diseases .
|
-
-
- HY-109025AR
-
|
|
Influenza Virus
|
Infection
|
|
Baloxavir (Standard) is the analytical standard of Baloxavir. This product is intended for research and analytical applications. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity .
|
-
-
- HY-122913
-
|
|
Akt
|
Cancer
|
|
Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt .
|
-
-
- HY-16518
-
|
SNS-595 Hydrochloride; Vosaroxin Hydrochloride; AG 7352 Hydrochloride
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
|
-
-
- HY-161017
-
|
|
Others
|
Others
|
|
WDR91-IN-1 (Compd 1) is a first-in-class small-molecule ligand for WDR91, with a KD of 6 μM .
|
-
-
- HY-139742
-
|
|
Sirtuin
|
Cancer
|
|
ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
|
-
-
- HY-133740
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM .
|
-
-
- HY-139396
-
-
-
- HY-121467S
-
-
-
- HY-133735
-
|
|
RABV
|
Infection
|
|
GRP-60367 is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains .
|
-
-
- HY-123981
-
|
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
|
-
-
- HY-124600
-
|
|
HBV
|
Infection
|
|
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity .
|
-
-
- HY-101772R
-
|
GLPG1690 (Standard)
|
Reference Standards
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Ziritaxestat (Standard) is the analytical standard of Ziritaxestat. This product is intended for research and analytical applications. Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM .
|
-
-
- HY-B0790
-
|
|
NEKs
Apoptosis
|
Cancer
|
|
TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells .
|
-
-
- HY-137459
-
|
CA-008
|
TRP Channel
|
Neurological Disease
|
|
Vocacapsaicin (CA-008), a proagent of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief .
|
-
-
- HY-157728
-
|
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research .
|
-
-
- HY-137459A
-
|
CA-008 hydrochloride
|
TRP Channel
|
Neurological Disease
|
|
Vocacapsaicin (CA-008) hydrochloride, a proagent of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride can provide meaningful and long-lasting pain relief .
|
-
-
- HY-12484
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity .
|
-
-
- HY-P99631
-
|
CSL312
|
Factor Xa
|
Cardiovascular Disease
|
|
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research .
|
-
-
- HY-150203
-
-
-
- HY-10534
-
|
SNS-595; Vosaroxin; AG 7352
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
|
-
-
- HY-135653
-
EC5026
1 Publications Verification
BPN-19186
|
Epoxide Hydrolase
|
Neurological Disease
|
|
EC5026 (BPN-19186) is a first-in-class, non-opioid and orally active soluble Epoxide Hydrolase (sEH) inhibitor. EC5026 shows efficacy for inflammatory and neuropathic pain .
|
-
-
- HY-U00141
-
|
α-Hydroxylinoleic acid
|
Autophagy
|
Metabolic Disease
Cancer
|
|
ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity .
|
-
-
- HY-131181
-
LEI-401
2 Publications Verification
|
Phospholipase
|
Neurological Disease
|
|
LEI-401 is a first-in-class, selective, and CNS-active NAPE-PLD (N-acylphosphatidylethanolamine phospholipase D) inhibitor, with an IC50 of 27 nM. LEI-401 modulates emotional behavior in mice .
|
-
-
- HY-18652
-
|
Ro 5126766; CH5126766
|
MEK
Raf
|
Cancer
|
|
Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
|
-
- HY-135145
-
|
CB-103
|
Notch
|
Cancer
|
|
Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity .
|
-
- HY-139611C
-
|
MRTX-1719 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
Navlimetostat hydrochloride is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAP DEL SDMA cells .
|
-
- HY-134836
-
|
|
Apoptosis
METTL3
|
Cancer
|
|
STM2457 is a first-in-class, highly potent, selective and orally active METTL3 inhibitor with an IC50 of 16.9 nM. STM2457 can be used for the research of acute myeloid leukaemia (AML) .
|
-
- HY-132885
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
|
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- HY-107093
-
|
|
Apoptosis
|
Cancer
|
|
MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 has the potential for tumor-induced bone disease (TIBD) research .
|
-
- HY-133735A
-
|
|
RABV
|
Infection
|
|
GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein .
|
-
- HY-109108
-
|
DS-3201
|
Histone Methyltransferase
|
Cancer
|
|
Valemetostat (DS-3201), a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
|
-
- HY-109108A
-
|
DS-3201 tosylate
|
Histone Methyltransferase
|
Cancer
|
|
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma .
|
-
- HY-W751835
-
|
Baloxavir acid-d4; S-033447-d4
|
Isotope-Labeled Compounds
|
Others
Cancer
|
|
Baloxavir-d4 (Baloxavir acid-d4; S-033447-d4) is the deuterium-labeled Baloxavir (HY-109025A). Baloxavir-d4 (Baloxavir-d4 acid), derived from the proagent Baloxavir-d4 marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir-d4 inhibits viral RNA transcription and replication and has potently antiviral activity .
|
-
- HY-117421A
-
|
|
Histone Methyltransferase
DNA Methyltransferase
|
Cancer
|
|
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
|
-
- HY-P99330
-
|
Anti-Human VEGFA Recombinant Antibody; RO5520985
|
VEGFR
Tie
|
Cancer
|
|
Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects .
|
-
- HY-128357A
-
|
ACX-362E hydrochloride; GLS-362E hydrochloride
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Ibezapolstat hydrochloride is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat hydrochloride is developed for the research of C. difficile infection(CDI) .
|
-
- HY-117421
-
|
|
Histone Methyltransferase
DNA Methyltransferase
|
Cancer
|
|
CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
|
-
- HY-107093B
-
|
|
Apoptosis
|
Cancer
|
|
MBC-11 triethylamine is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 triethylamine has the potential for tumor-induced bone disease (TIBD) research .
|
-
- HY-107093A
-
|
|
Apoptosis
|
Cancer
|
|
MBC-11 trisodium is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C. MBC-11 trisodium has the potential for tumor-induced bone disease (TIBD) research .
|
-
- HY-153306A
-
|
|
PI3K
Drug Isomer
|
Cancer
|
|
(S)-RLY-2608 is an S-enantiomer of of RLY-2608 (HY-153306). RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity .
|
-
- HY-12861
-
|
|
p97
|
Cancer
|
|
CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM .
|
-
- HY-110273
-
-
- HY-159989
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
UNC10142 (Compound 44) is a first-in-class small molecule antagonist of CHD1 that binds with an IC50 value of 1.7 μM. UNC10142 leads to a dose-dependent reduction in viability in PTEN-deficient prostate cancer cells .
|
-
- HY-101124
-
|
KAR5585
|
Tryptophan Hydroxylase
5-HT Receptor
|
Cardiovascular Disease
|
|
Rodatristat ethyl (KAR5585) is a first-in-class oral tryptophan hydroxylase 1 (TPH1) Inhibitor with nanomolar in vitro potency. Rodatristat ethyl reduces the level of 5-HT and significantly reduces pulmonary arterial hypertension (PAH) .
|
-
- HY-P99480
-
|
M7824; MSB0011359C
|
TGF-β Receptor
|
Cancer
|
|
Bintrafusp alfa (M 7824) is a first-in-class bifunctional fusion protein composed of the extracellular domain of TGF-βRII fused to a human IgG1 mAb blocking programmed cell death ligand. Bintrafusp alfa can be used for the research of cancer .
|
-
- HY-109064
-
|
Oxycodegol; NKTR-181
|
Opioid Receptor
|
Neurological Disease
|
|
Loxicodegol (Oxycodegol) is a first-in-class, long-acting, orally active, and selective mu-opioid agonist with structural properties that reduce its rate of entry across the blood-brain barrier compared with traditional mu-opioid agonists .
|
-
- HY-112606
-
|
|
RXFP Receptor
|
Others
|
|
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM . ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.
|
-
- HY-12057
-
Vemurafenib
Maximum Cited Publications
83 Publications Verification
PLX4032; RG7204; RO5185426
|
Raf
Autophagy
|
Cancer
|
|
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-15262
-
|
|
Sirtuin
|
Neurological Disease
Metabolic Disease
Cancer
|
|
SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD + dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease .
|
-
- HY-130800
-
-
- HY-136198
-
|
|
Syk
PI3K
|
Cancer
|
|
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression .
|
-
- HY-128357
-
|
ACX-362E; GLS-362E
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI) .
|
-
- HY-108024
-
|
KAF156; GNF156
|
Parasite
|
Infection
|
|
Ganaplacide (KAF156) is a first-in-class,
orally active imidazolopiperazine antimalarial agent.
Ganaplacide is active against a broad range of Plasmodium
species, including drug-resistant parasites. Ganaplacide is parasiticidal
against both asexual and sexual blood stages as well as the liver stages of the
parasite .
|
-
- HY-19837
-
|
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
|
-
- HY-148683
-
|
|
Arp2/3 Complex
|
Cancer
|
|
EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas .
|
-
- HY-16726
-
|
CG100649
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-P9915
-
|
Anti-Human CD38, Human Antibody
|
CD38
ADC Antibody
|
Inflammation/Immunology
Cancer
|
|
Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
|
-
- HY-128587
-
|
SY-1365
|
CDK
|
Cancer
|
|
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
|
-
- HY-139664
-
|
|
DNA Methyltransferase
|
Cancer
|
|
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-12820
-
|
Antibiotic-202
|
Bacterial
Antibiotic
|
Infection
|
|
Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD) .
|
-
- HY-112233
-
O-304
4 Publications Verification
|
AMPK
|
Cardiovascular Disease
Metabolic Disease
|
|
O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a agent to treat type 2 diabetes (T2D) and associated cardiovascular complications .
|
-
- HY-143899
-
|
|
Fungal
|
Infection
|
|
FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC80 of 1 μg/mL .
|
-
- HY-130000
-
|
STP0404
|
HIV Integrase
HIV
|
Infection
|
|
Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase (ALLINI) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties .
|
-
- HY-139290A
-
|
RG4326 sodium
|
MicroRNA
|
Cancer
|
|
RGLS4326 sodium is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 sodium can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 sodium inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM .
|
-
- HY-123134
-
|
|
FGFR
|
Cancer
|
|
FIIN-4 is a first-in-class, orally active and covalent FGFR inhibitor with IC50s of 2.6 nM, 2.6 nM, 5.6 nM, 9.2 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. FIIN-4 can inhibit metastatic tumor growth.
|
-
- HY-P9915A
-
|
Anti-Human CD38, Human Antibody (PBS)
|
ADC Antibody
CD38
|
Cancer
|
|
Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
|
-
- HY-12057S1
-
|
PLX4032-d7; RG7204-d7; RO5185426-d7
|
Isotope-Labeled Compounds
Raf
Autophagy
|
Cancer
|
|
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-12057S
-
|
|
Isotope-Labeled Compounds
Raf
Autophagy
|
Cancer
|
|
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-161847
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor .
|
-
- HY-100037
-
NT157
1 Publications Verification
Tyrphostin NT157
|
Insulin Receptor
STAT
|
Endocrinology
Cancer
|
|
NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway .
|
-
- HY-104037A
-
|
LYC-55716 sodium
|
ROR
|
Cancer
|
|
Cintirorgon sodium is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon sodium (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
|
-
- HY-126810
-
|
|
Fungal
|
Infection
|
|
NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections .
|
-
- HY-119708
-
|
RPL-554
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-153306
-
|
|
PI3K
|
Cancer
|
|
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
|
-
- HY-123875A
-
|
EPI-506
|
Androgen Receptor
|
Cancer
|
|
Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .
|
-
- HY-127105
-
|
LNP023
|
Complement System
|
Metabolic Disease
Inflammation/Immunology
|
|
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
|
-
- HY-18204A
-
|
LCZ696
|
Angiotensin Receptor
Neprilysin
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Sacubitril/Valsartan (LCZ696), comprised Valsartan and Sacubitril (AHU377) in 1:1 molar ratio, is a first-in-class, orally bioavailable, and dual-acting angiotensin receptor-neprilysin (ARN) inhibitor for hypertension and heart failure . Sacubitril/Valsartan ameliorates diabetic cardiomyopathy by inhibiting inflammation, oxidative stress and apoptosis .
|
-
- HY-128777
-
|
|
VDAC
Apoptosis
|
Cancer
|
|
WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX .
|
-
- HY-17614
-
|
SMT C1100; BMN 195; VOX-C1100
|
Cytochrome P450
|
Others
|
|
Ezutromid (SMT C1100) is a first-in-class, orally active benzoxazole utrophin modulator with an EC50 of 0.91 μM. Ezutromid can be used for the research Duchenne muscular dystrophy (DMD). Ezutromid inhibits CYP1A2 enzymic activity in human liver microsomes (HLM) with an IC50 of 5.4 μM .
|
-
- HY-141429C
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-141521
-
|
NX-13
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NX-13 is a first-in-class, orally active and gut-restricted agent that selectively targets and activates the NLRX1 pathway to induce immunometabolic changes. NX-13 results in lower inflammation and responses in inflammatory bowel disease. NX-13 can be used for the research of crohn's disease and ulcerative colitis .
|
-
- HY-126810A
-
|
|
Fungal
|
Infection
|
|
NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections .
|
-
- HY-P2076
-
|
SGX942
|
p62
Bacterial
|
Infection
Cancer
|
|
Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection . DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
|
-
- HY-139402
-
|
|
Ras
|
Cancer
|
|
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM) .
|
-
- HY-124069
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .
|
-
- HY-139290
-
|
RG4326
|
MicroRNA
|
Metabolic Disease
Cancer
|
|
RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM .
|
-
- HY-19980
-
|
APR-246; PRIMA-1Met
|
MDM-2/p53
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
|
-
- HY-120118
-
|
ML246
|
DNA/RNA Synthesis
|
Cancer
|
|
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models .
|
-
- HY-104037
-
|
LYC-55716
|
ROR
|
Cancer
|
|
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival .
|
-
- HY-141429
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-124071
-
|
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
ACT-389949 is a first-in-class, potent and selective and agonist of formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX), with an EC50 of 3 nM for FPR2/ALX internalization into monocytes. ACT-389949 has potential for the treatment of inflammatory disorders .
|
-
- HY-12057R
-
|
|
Raf
Autophagy
|
Cancer
|
|
Vemurafenib (Standard) is the analytical standard of Vemurafenib. This product is intended for research and analytical applications. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-120934
-
|
|
TNF Receptor
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity .
|
-
- HY-109567
-
|
PD-72953
|
LDLR
|
Metabolic Disease
Inflammation/Immunology
|
|
Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity .
|
-
- HY-12481
-
|
|
PI3K
Autophagy
|
Cancer
|
|
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
|
-
- HY-141429A
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
|
-
- HY-18614
-
|
|
Notch
γ-secretase
|
Cancer
|
|
LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibits Notch signalling in tumor cell lines and endothelial cells (IC50=0.005-20 nM). LY900009 can be used for advanced cancer research .
|
-
- HY-13591
-
|
IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
|
-
- HY-134823
-
|
|
MDM-2/p53
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects .
|
-
- HY-P991066
-
|
|
nAChR
|
Neurological Disease
|
|
ARGX-119 is a first-in-class humanized agonist monoclonal antibody specific for muscle-specific kinase (MuSK). ARGX-119 can be used for the study of neuromuscular diseases. The isotype control for ARGX-119 can refer to Human IgG1 lambda1, Isotype Control (HY-P99992) .
|
-
- HY-164202
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
ORM-5029 is a first-in-class human epidermal growth factor receptor 2 (HER2)-targeted antibody-drug conjugate (ADC) comprised of SMol006, a highly potent GSPT1 degrader, conjugated to Pertuzumab (HY-P9912). ORM-5029 can be used for study of cancer .
|
-
- HY-130602
-
|
|
PROTACs
MEK
|
Cancer
|
|
MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively .
|
-
- HY-109025AS
-
|
Baloxavir acid-d5; S-033447-d5
|
Isotope-Labeled Compounds
Influenza Virus
|
Infection
|
|
Baloxavir-d5 is deuterium labeled Baloxavir. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity .
|
-
- HY-145169
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects .
|
-
- HY-120051
-
|
S44819; Egis-13529
|
GABA Receptor
|
Neurological Disease
|
|
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
|
-
- HY-108706
-
|
|
Histone Demethylase
|
Cancer
|
|
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases .
|
-
- HY-16726R
-
|
|
COX
Carbonic Anhydrase
|
Cancer
|
|
Polmacoxib (Standard) is the analytical standard of Polmacoxib. This product is intended for research and analytical applications. Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase . Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models .
|
-
- HY-139664A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-109567A
-
|
PD-72953 calcium
|
LDLR
|
Metabolic Disease
Inflammation/Immunology
|
|
Gemcabene calcium (PD-72953 calcium), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity .
|
-
- HY-112090
-
|
|
Epigenetic Reader Domain
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability .
|
-
- HY-P2076A
-
|
SGX942 TFA
|
p62
Bacterial
|
Infection
Cancer
|
|
Dusquetide (SGX942) TFA is a first-in-class innate defense regulator (IDR). Dusquetide TFA modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide TFA shows activity in both reducing inflammation and increasing clearance of bacterial infection . DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
|
-
- HY-168448
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBAZ2 is a first-in-class BAZ2A and BAZ2B PROTAC degrader with DC50 values of 180 nM and 250 nM for BAZ2A and BAZ2B, respectively. (Blue: E3 ligase ligand (VH 101, thiol (HY-47851); Black: linker (HY-168450); pink: target protein ligand (HY-168449)) .
|
-
- HY-12820R
-
|
Antibiotic-202 (Standard)
|
Bacterial
Antibiotic
|
Infection
|
|
Sibofimloc (Standard) is the analytical standard of Sibofimloc. This product is intended for research and analytical applications. Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD)[1][2].
|
-
- HY-10220
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor, has antitumor and anti-angiogenic activity. SF1126 is an RGDS-conjugated LY294002 proagent, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment. SF1126 induces cell apoptosis .
|
-
- HY-108468
-
|
|
Cryptochrome
|
Metabolic Disease
|
|
KL001 is a first-in-class cryptochrome (CRY, a flavoproteins that are sensitive to blue light, and is involved in the circadian rhythms of plants and animals) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis .
|
-
- HY-129241
-
|
|
DNA/RNA Synthesis
DNA Alkylator/Crosslinker
|
Cancer
|
|
AGX51 is the first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and viability reduction. AGX51 can inhibit TNBC and has an IC50 of about 25 nM. AGX51 can be used in cancer research.
|
-
- HY-139403
-
|
|
Target Protein Ligand-Linker Conjugates
Ras
|
Cancer
|
|
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (IC50s between 0.25 and 0.76 μM) .
|
-
- HY-100487
-
|
MLN7243
|
E1/E2/E3 Enzyme
NF-κB
Apoptosis
|
Cancer
|
|
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .
|
-
- HY-12248
-
|
CB-839
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
|
-
- HY-148369
-
|
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
|
Cancer
|
|
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
|
-
- HY-162362
-
|
|
PROTACs
GLP Receptor
|
Cancer
|
|
MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .
|
-
- HY-100201
-
|
|
Histone Methyltransferase
|
Cancer
|
|
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
|
-
- HY-112804
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
SGC-iMLLT is a first-in-class chemical probe and a potent, selective inhibitor of MLLT1/3-histone interactions with an IC50 of 0.26 μM. SGC-iMLLT shows high binding activity towards MLLT1 YEATS domain (YD) and MLLT3 YD (AF9/YEATS3) with Kds of 0.129 and 0.077 μM, respectively .
|
-
- HY-139664B
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-12248A
-
|
CB-839 hydrochloride
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
|
-
- HY-114277
-
|
AMG-510
|
Ras
|
Cancer
|
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-134539
-
IMT1
4 Publications Verification
|
Oxidative Phosphorylation
Mitochondrial Metabolism
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
|
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
|
-
- HY-119708S
-
|
RPL-554-d6
|
Isotope-Labeled Compounds
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Ensifentrine-d6 (RPL-554-d6) is deuterium labeled Ensifentrine. Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-173639
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
AZD0516 is a first-in-class antibody-drug conjugate (ADC) targeting six-transmembrane epithelial antigen of the prostate-2 (STEAP2). The anti-STEAP2 monoclonal antibody (mAb) is conjugated via interchain cysteines to a maleimide-reactive, β-glucuronidase-cleavable linker (HY-173635) bearing the topoisomerase 1 inhibitor, Exatecan (HY-13631). AZD0516 can be used for the study of prostate cancer .
|
-
- HY-137464A
-
OATD-01
1 Publications Verification
|
Others
|
Inflammation/Immunology
|
|
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
|
-
- HY-19980G
-
|
APR-246; PRIMA-1Met
|
MDM-2/p53
Apoptosis
Ferroptosis
|
Cancer
|
|
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
|
-
- HY-107390A
-
|
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-123611
-
|
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
|
-
- HY-15614A
-
|
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells .
|
-
- HY-15614
-
|
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells .
|
-
- HY-107390
-
AX-024
1 Publications Verification
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
Cancer
|
|
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-14865
-
|
PTK 0796; Amadacycline
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (PTK 0796), a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections .
|
-
- HY-101925
-
CM-272
3 Publications Verification
|
Histone Methyltransferase
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .
|
-
- HY-107146
-
|
P1pal-7
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Cancer
|
|
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
|
-
- HY-14865B
-
|
PTK 0796 tosylate; Amadacycline tosylate
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (PTK 0796) tosylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline tosylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline tosylate possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline tosylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections .
|
-
- HY-131177
-
|
|
GSK-3
|
Metabolic Disease
|
|
yGsy2p-IN-H23 is a potent and first-in-class inhibitor for yeast glycogen synthase 2 (yGsy2p) with an IC50 of 875 μM for human glycogen synthase 1 (hGYS1). yGsy2p-IN-H23 bounds within the uridine diphosphate glucose binding pocket of yGsy2p. yGsy2p-IN-H23 is used for the research of glycogen storage diseases (GSDs) .
|
-
- HY-14865C
-
|
PTK0796 hydrochloride; Amadacycline hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (PTK 0796) hydrochloride, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline hydrochloride acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline hydrochloride possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline hydrochloride can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections .
|
-
- HY-14865A
-
|
PTK 0796 mesylate; Amadacycline mesylate
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (PTK 0796) mesylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline mesylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline mesylate possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline mesylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections .
|
-
- HY-16350
-
|
NKP-1339; IT-139; KP-1339
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu .
|
-
- HY-114277S
-
|
AMG-510-d7
|
Isotope-Labeled Compounds
Ras
|
Cancer
|
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
- HY-137516
-
LC-2
1 Publications Verification
|
PROTACs
Ras
|
Cancer
|
|
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .
|
-
- HY-114277S2
-
|
AMG-510-d3
|
Isotope-Labeled Compounds
Ras
|
Cancer
|
|
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
|
-
- HY-136351
-
|
|
Autophagy
|
Cancer
|
|
THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines .
|
-
- HY-141640
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently induces the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines. MS154 potently inhibits cell proliferation in lung cancer cells (Blue: E3 Ligase ligand (HY-103596); Black: linker (HY-W096167); Pink: EGFR ligand (HY-168305)) .
|
-
- HY-160481
-
|
|
Tau Protein
MicroRNA
|
Neurological Disease
|
|
MG-1102 is first-in-class dual binder of monomeric tau and pre-miRNA-146a. MG-1102 shows specific inhibition of miRNA146a with IC50s of 0.21 mM and 0.36 mM specific inhibition of doublelabeled pre-miRNA146a and mono-labeled pre-miRNA146a, respectively. MG-1102 interacts with tau monomers with a Kd of 3.21 mM by surface plasmon resonance (SPR). MG-1102 is a potential multi-target-directed ligands (MTDLs) for Alzheimer’s disease (AD) .
|
-
- HY-111789
-
|
TAK-981
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
Cancer
|
|
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .
|
-
- HY-136259
-
ML188
5 Publications Verification
|
SARS-CoV
Virus Protease
|
Infection
|
|
ML188, a first in class probe, is a selective non-covalent SARS-CoV 3CLpro inhibitor with an IC50 of 1.5 μM. Antiviral activity .
|
-
- HY-14865R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (Standard) is the analytical standard of Omadacycline. This product is intended for research and analytical applications. Omadacycline (PTK 0796), a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections .
|
-
- HY-P99575
-
|
AMG-757
|
Notch
|
Inflammation/Immunology
Cancer
|
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
|
-
- HY-14865CR
-
|
PTK0796 hydrochloride (Standard); Amadacycline hydrochloride (Standard)
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (hydrochloride) (Standard) is the analytical standard of Omadacycline (hydrochloride). This product is intended for research and analytical applications. Omadacycline (PTK 0796) hydrochloride, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline hydrochloride acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline hydrochloride possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline hydrochloride can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections[1][2][3][4].
|
-
- HY-14865BR
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Omadacycline (tosylate) (Standard) is the analytical standard of Omadacycline (tosylate). This product is intended for research and analytical applications. Omadacycline (PTK 0796) tosylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline tosylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline tosylate possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline tosylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections .
|
-
- HY-131708A
-
|
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
|
-
- HY-129738
-
|
|
Ras
|
Cardiovascular Disease
|
|
I942 is a first in class, selective non-cyclic nucleotide (NCN) EPAC1 agonist. I942 can attenuate proinflammatory cytokine signalling normally associated with cardiovascular diseases .
|
-
- HY-14931
-
|
AZD 3582; HCT 3012; Nitronaproxen
|
COX
|
Inflammation/Immunology
|
|
Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation .
|
-
- HY-111789A
-
|
(S)-TAK-981
|
Drug Isomer
|
Inflammation/Immunology
Cancer
|
|
(S)-Subasumstat is the isomer of Subasumstat (HY-111789). Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .
|
-
- HY-131708
-
|
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
|
-
- HY-114312
-
MD-224
5 Publications Verification
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-170944
-
|
|
HSP
Apoptosis
Caspase
|
Cancer
|
|
BAG3/HSP70-IN-1 (compound 16) is the first-in-class BAG3/HSP70 dual modulator. BAG3/HSP70-IN-1 inhibits HeLa cells with an IC50 of 49.46 μM. BAG3/HSP70-IN-1 induces Apoptosis by activating caspase 3 and caspase 9 levels in HeLa cells. BAG3/HSP70-IN-1 elevates p21 levels while reduces FOXM1 expression in HeLa cells. BAG3/HSP70-IN-1 decreases ATPase activity .
|
-
- HY-123693
-
|
|
Insecticide
|
Inflammation/Immunology
|
|
ML358 is a first in class, potent, and selective inhibitor of the SKN-1 pathway (IC50=0.24 μM). ML358 sensitizes the model nematode C. elegans to oxidants and anthelmintic. ML358 potentially used as adjuvants to increase the efficacy and useful life of current anthelmintics .
|
-
- HY-161667
-
|
|
GSK-3
HDAC
|
Neurological Disease
|
|
GSK-3β/HDAC-IN-1 (Compd 4) is a brain-penetrant and first in class dual non-ATP-competitive Glycogen Synthase Kinase 3β/Histone Deacetylases (GSK-3β/HDACs) Inhibitor with IC50s of 0.142, 0.03 and 0.045 μM against GSK-3β, HDAC2 and HDAC6, respectively. GSK-3β/HDAC-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-134813A
-
|
|
Ras
|
Cancer
|
|
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-P99010
-
|
|
FGFR
|
Cancer
|
|
Bemarituzumab is a humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has antitumor activity against gastric and breast cancer .
|
-
- HY-145310
-
-
- HY-133129
-
MS1943
1 Publications Verification
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MS1943 is an orally active, PROTAC-based, selective degrader of EZH2 that effectively reduces EZH2 levels in cells. MS1943 has anticancer activity and exhibits cytotoxic effects in a variety of TNBC cells while sparing normal cells. In addition, MS1943 maintains high potency (IC50=120 nM) in inhibiting EZH2 methyltransferase activity and is highly selective for EZH2. (Structure Note: RED, EZH2 ligand (HY-148458); Blue, Hyt (HY-W001578)) .
|
-
- HY-134813
-
|
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-19980G
-
|
APR-246 (GMP); PRIMA-1Met (GMP)
|
Fluorescent Dye
|
|
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
|
| Cat. No. |
Product Name |
Type |
-
- HY-19980G
-
|
APR-246 (GMP); PRIMA-1Met (GMP)
|
Biochemical Assay Reagents
|
|
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-126810A
-
|
|
Fungal
|
Infection
|
|
NP213 TFA is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 TFA targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 TFA is effective and well-tolerated in resolving nail fungal infections .
|
-
- HY-P2076
-
|
SGX942
|
p62
Bacterial
|
Infection
Cancer
|
|
Dusquetide (SGX942) is a first-in-class innate defense regulator (IDR). Dusquetide modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide shows activity in both reducing inflammation and increasing clearance of bacterial infection . DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
|
-
- HY-107146
-
|
P1pal-7
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Cancer
|
|
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
|
-
- HY-126810
-
|
|
Fungal
|
Infection
|
|
NP213 is a rapidly acting, novel, first-in-class synthetic antimicrobial peptide (AMP), has anti-fungal activities. NP213 targets the fungal cytoplasmic membrane and plays it role via membrane perturbation and disruption. NP213 is effective and well-tolerated in resolving nail fungal infections .
|
-
- HY-P2076A
-
|
SGX942 TFA
|
p62
Bacterial
|
Infection
Cancer
|
|
Dusquetide (SGX942) TFA is a first-in-class innate defense regulator (IDR). Dusquetide TFA modulates the innate immune response to both PAMPs and DAMPs by binding to p62. Dusquetide TFA shows activity in both reducing inflammation and increasing clearance of bacterial infection . DAMPs: damage-associated molecular patterns; PAMPs: pathogen-associated molecular patterns
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P9927
-
|
Ain457
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis .
|
-
- HY-P99631
-
|
CSL312
|
Factor Xa
|
Cardiovascular Disease
|
|
Garadacimab (CSL312) is a first-in-class, fully human IgG4 monoclonal antibody targeting activated factor XII (FXIIa). Garadacimab has the potential for hereditary angioedema research .
|
-
- HY-P99537
-
|
PBP1510
|
Inhibitory Antibodies
|
Cancer
|
|
Ulenistamab (PBP1510) is a first-in-class hunamised IgG1 monoclonal antibody targeting pancreatic adenocarcinoma upregulated factor (PAUF). Ulenistamab can be used for pancreatic cancer (PC) research .
|
-
- HY-P99330
-
|
Anti-Human VEGFA Recombinant Antibody; RO5520985
|
VEGFR
Tie
|
Cancer
|
|
Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects .
|
-
- HY-P99480
-
|
M7824; MSB0011359C
|
TGF-β Receptor
|
Cancer
|
|
Bintrafusp alfa (M 7824) is a first-in-class bifunctional fusion protein composed of the extracellular domain of TGF-βRII fused to a human IgG1 mAb blocking programmed cell death ligand. Bintrafusp alfa can be used for the research of cancer .
|
-
- HY-P9915
-
|
Anti-Human CD38, Human Antibody
|
CD38
ADC Antibody
|
Inflammation/Immunology
Cancer
|
|
Daratumumab (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab has anti-multiple myeloma (MM) effect. Daratumumab impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
|
-
- HY-P9915A
-
|
Anti-Human CD38, Human Antibody (PBS)
|
ADC Antibody
CD38
|
Cancer
|
|
Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition .
|
-
- HY-P99575
-
|
AMG-757
|
Notch
|
Inflammation/Immunology
Cancer
|
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research .
|
-
- HY-P99010
-
|
|
FGFR
|
Cancer
|
|
Bemarituzumab is a humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has antitumor activity against gastric and breast cancer .
|
-
- HY-P991066
-
|
|
nAChR
|
Neurological Disease
|
|
ARGX-119 is a first-in-class humanized agonist monoclonal antibody specific for muscle-specific kinase (MuSK). ARGX-119 can be used for the study of neuromuscular diseases. The isotype control for ARGX-119 can refer to Human IgG1 lambda1, Isotype Control (HY-P99992) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W751835
-
|
|
|
Baloxavir-d4 (Baloxavir acid-d4; S-033447-d4) is the deuterium-labeled Baloxavir (HY-109025A). Baloxavir-d4 (Baloxavir-d4 acid), derived from the proagent Baloxavir-d4 marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir-d4 inhibits viral RNA transcription and replication and has potently antiviral activity .
|
-
-
- HY-114277S
-
|
|
|
Sotorasib-d7 (AMG-510-d7) is a deuterium-labeled Sotorasib (HY-114277). Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C‑mutated locally advanced or metastatic non‑small cell lung cancer (NSCLC) .
|
-
-
- HY-121467S
-
|
|
|
Acotiamide-d6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia .
|
-
-
- HY-12057S1
-
|
|
|
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
-
- HY-12057S
-
|
|
|
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
-
- HY-109025AS
-
|
|
|
Baloxavir-d5 is deuterium labeled Baloxavir. Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity .
|
-
-
- HY-119708S
-
|
|
|
Ensifentrine-d6 (RPL-554-d6) is deuterium labeled Ensifentrine. Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research .
|
-
-
- HY-114277S2
-
|
|
|
Sotorasib-d3 (AMG-510-d3) is deuterium labeled Sotorasib. Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib leads to the regression of KRAS G12C?mutated locally advanced or metastatic non?small cell lung cancer (NSCLC) .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-134813
-
|
|
|
Alkynes
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-139290A
-
|
RG4326 sodium
|
|
Antisense Oligonucleotides
|
|
RGLS4326 sodium is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 sodium can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 sodium inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM .
|
-
- HY-139290
-
|
RG4326
|
|
Antisense Oligonucleotides
|
|
RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM .
|
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