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Results for "

isoform selectivity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (2) 5-HT Receptor (1) AAK1 (1) Adenylate Cyclase (1) Adrenergic Receptor (1) Akt (1) Aldehyde Dehydrogenase (ALDH) (1) AMPK (3) Apoptosis (12) Aquaporin (1) Autophagy (22) Bcl-2 Family (1) Carbonic Anhydrase (8) Casein Kinase (6) CCR (1) CDK (2) COMT (1) Cryptochrome (1) Cytochrome P450 (12) DAGL (1) DNA-PK (1) DNA/RNA Synthesis (1) Dopamine Transporter (1) Drug Metabolite (1) DYRK (1) Endogenous Metabolite (4) Epigenetic Reader Domain (2) ERK (1) Estrogen Receptor/ERR (1) FLT3 (3) Fluorescent Dye (1) Free Fatty Acid Receptor (1) GABA Receptor (1) Glucocorticoid Receptor (2) Glycosidase (2) GPR119 (2) GSK-3 (1) HCV (1) HCV Protease (2) HDAC (11) HSP (3) IFNAR (1) iGluR (1) IKK (2) Interleukin Related (1) IRE1 (1) Isocitrate Dehydrogenase (IDH) (1) Isotope-Labeled Compounds (7) JAK (2) JNK (4) LPL Receptor (1) MAGL (1) Microtubule/Tubulin (2) Mitochondrial Metabolism (1) MNK (2) mTOR (1) Na+/H+ Exchanger (NHE) (5) NO Synthase (2) p38 MAPK (6) PD-1/PD-L1 (2) PDGFR (3) Phosphatase (2) Phosphodiesterase (PDE) (6) PI3K (15) PKA (1) PKC (2) PKD (1) Potassium Channel (3) PPAR (8) Progesterone Receptor (1) PROTACs (1) Protein Arginine Deiminase (2) RAR/RXR (2) Ras (1) Reference Standards (8) RET (1) ROR (1) Sirtuin (1) Sodium Channel (5) Src (1) SRPK (1) STAT (1) Trk Receptor (4) Urea Transporter (1) VEGFR (1) α-synuclein (1)
By Research Areas:	Cancer (73) Cardiovascular Disease (23) Endocrinology (1) Infection (6) Inflammation/Immunology (25) Metabolic Disease (21) Neurological Disease (27)
Click Chemistry:	Azide (1)

151

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-113957

MPI_5a	HDAC	Cancer
MPI_5a is a potent and selective HDAC6 inhibitor (IC₅₀=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC₅₀ value of 210 nM .

HY-131305

HBDDE	PKC Apoptosis	Neurological Disease
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC₅₀s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .

HY-126073

DFP00173 4 Publications Verification	Aquaporin	Inflammation/Immunology Cancer
DFP00173 is a potent and selective aquaporin-3 (AQP3) inhibitor. DFP00173 inhibits mouse and human AQP3 with an IC₅₀ of ～0.1-0.4 μM. DFP00173 is selective for AQP3 over the homologous AQP isoforms AQP7 and AQP9 .

HY-105064D

Zoniporide hydrochloride hydrate 1 Publications Verification CP-597396 hydrochloride hydrate	Na+/H+ Exchanger (NHE)	Cardiovascular Disease
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC₅₀=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC₅₀=59 nM) .

HY-101972

AZ-PFKFB3-67 1 Publications Verification	Phosphatase Bcl-2 Family	Neurological Disease Metabolic Disease
AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with IC₅₀s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1, respectively. AZ-PFKFB3-67 reduces MCL-1. AZ-PFKFB3-67 has neuroprotective activity .

HY-105064B

Zoniporide hydrochloride CP-597396 hydrochloride	Na+/H+ Exchanger (NHE)	Cardiovascular Disease
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC₅₀=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC₅₀=59 nM) .

HY-105064DR

Zoniporide hydrochloride hydrate (Standard) CP-597396 hydrochloride hydrate (Standard)	Reference Standards Na+/H+ Exchanger (NHE)	Cardiovascular Disease
Zoniporide (hydrochloride hydrate) (Standard) is the analytical standard of Zoniporide (hydrochloride hydrate). This product is intended for research and analytical applications. Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .

HY-103384

TMCB	Casein Kinase	Cancer
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct K_i values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .

HY-101972A

AZ-PFKFB3-67 quarterhydrate	Phosphatase	Metabolic Disease
AZ-PFKFB3-67 quarterhydrate is potent and selective metabolic kinase PFKFB3 inhibitor, with IC₅₀s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively .

HY-150692

Estrogen receptor α antagonist 1	Estrogen Receptor/ERR	Cancer
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC₅₀s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .

HY-15224

PCI-34051 Maximum Cited Publications 24 Publications Verification	HDAC Apoptosis	Cancer
PCI-34051 is a potent and selective HDAC8 inhibitor with IC₅₀ of 10 nM, with >200-fold selectivity over the other HDAC isoforms.

HY-162767

KUNG65	HSP	Neurological Disease
KUNG65 is a selective inhibitor of Grp94, with a target K_d of 540 nM and at least 73 fold selectivity vs. the other Hsp90 isoforms .

HY-125838

J30-8	JNK	Neurological Disease
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC₅₀ of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases .

HY-D1341

Coumberone 1 Publications Verification	Fluorescent Dye	Cancer
Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C .

HY-16596

CNX-1351	PI3K	Cancer
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC₅₀ of 6.8 nM.

HY-103683

PF-06409577 1 Publications Verification	AMPK	Metabolic Disease
PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM.

HY-108526

AC-55649	RAR/RXR Autophagy	Others
AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC₅₀ of 6.9.

HY-119254

BAY-850 4 Publications Verification	Epigenetic Reader Domain	Metabolic Disease
BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC₅₀ of 166 nM.

HY-159568

hCAIX-IN-22	Carbonic Anhydrase	Cancer
hCAIX-IN-22 is a highly selective inhibitor of human carbonic anhydrase (hCA) isoform XII (K_i=9.7 nM) with anticancer activity .

HY-17464

Cilostazol 4 Publications Verification OPC 13013	Phosphodiesterase (PDE) Autophagy	Cardiovascular Disease Cancer
Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-108532

AC-261066	RAR/RXR	Cancer
AC-261066 is a potent, orally available and isoform-selective retinoic acid beta2 (RARbeta2) receptor agonist, with a pEC₅₀ of 8.0 .

HY-P5174

MitTx	Sodium Channel	Neurological Disease
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC₅₀ values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .

HY-P2261

STAD 2	PKA	Infection
STAD 2 is a potent and selective disruptor of PKA-RII, with a K_d of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .

HY-112286

PI3Kγ inhibitor 2	PI3K	Inflammation/Immunology
PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a K_i of 4 nM .

HY-158078

Carbonic anhydrase inhibitor 21	Carbonic Anhydrase	Cancer
Carbonic anhydrase inhibitor 21 (Compound 5h) is a selective carbonic anhydrase (hCA IX) inhibitor, with a K_i of 15.1?nM, and is highly selective against other investigated isoform. Carbonic anhydrase inhibitor 21 can be used for anticancer research .

HY-108318

RK-24466 KIN 001-51	Src	Cardiovascular Disease Inflammation/Immunology
RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC₅₀s of less than 1 and 2 nM, respectively.

HY-147220

Dexamethasone oxetanone Dex-Ox	Progesterone Receptor	Endocrinology
Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms .

HY-123825

GX-674	Sodium Channel	Cardiovascular Disease Neurological Disease
GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC₅₀ of 0.1 nM at -40 mV .

HY-15245

GSK2636771 5+ Cited Publications	PI3K	Cancer
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a K_i of 0.89 nM and an IC₅₀ of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

HY-13802

SC-514 5 Publications Verification GK 01140	IKK	Cancer
SC-514 is a selective IKK-2 inhibitor (IC₅₀=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

HY-111791

ACY-1083 1 Publications Verification	HDAC	Cancer
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC₅₀ of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .

HY-156181

hCAIX/XII-IN-8	Carbonic Anhydrase	Cancer
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with K_i values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .

HY-17464S

Cilostazol-d11	Isotope-Labeled Compounds Phosphodiesterase (PDE) Autophagy	Cardiovascular Disease Cancer
Cilostazol-d₁₁ is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-17464S1

Cilostazol-d4 OPC-13013-d₄	Isotope-Labeled Compounds Phosphodiesterase (PDE) Autophagy	Cardiovascular Disease Cancer
Cilostazol-d₄ is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-12866

Larotrectinib 10+ Cited Publications LOXO-101; ARRY-470	Trk Receptor Apoptosis	Cancer
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).

HY-163145

α-Synuclein inhibitor 11	α-synuclein	Neurological Disease
α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .

HY-134194

KL201 1 Publications Verification	Cryptochrome	Metabolic Disease
KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues .

HY-163316

SIRT4-IN-1	Sirtuin	Metabolic Disease Cancer
SIRT4-IN-1 (compound 69) is selective sirtuin 4 (Sirt4) inhibitor with an IC₅₀ of 16 μM.SIRT4-IN-1 shows no relevant effects on other sirtuin isoforms .

HY-126145

S1PR1 modulator 1	LPL Receptor	Inflammation/Immunology
S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC₅₀ of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4 .

HY-P1219

Jingzhaotoxin-III β-TRTX-Cj1α	Sodium Channel	Neurological Disease
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC₅₀ of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .

HY-15280

GSK2292767	PI3K	Inflammation/Immunology
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC₅₀ of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease .

HY-13223A

Crenolanib benzenesulfonate CP 868596-26	Autophagy PDGFR FLT3	Cancer
Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

HY-13223

Crenolanib 10+ Cited Publications CP-868596	FLT3 PDGFR Autophagy	Cancer
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

HY-144639

Carbonic anhydrase inhibitor 5	Carbonic Anhydrase	Infection Inflammation/Immunology Cancer
Carbonic anhydrase inhibitor 5 is a potent and selective human carbonic anhydrase (hCA) inhibitor with IC₅₀s of 42.9, 47,6 and 6.7 nM for hCA II, hCA IX and hCA XII, respectively .

HY-119254A

trans-BAY-850	Epigenetic Reader Domain	Metabolic Disease
trans-BAY-850 is the trans isomer of BAY-850 (HY-119254). BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC₅₀ of 166 nM.

HY-17464R

Cilostazol (Standard) OPC 13013 (Standard)	Reference Standards Phosphodiesterase (PDE) Autophagy	Cardiovascular Disease Cancer
Cilostazol (Standard) is the analytical standard of Cilostazol. This product is intended for research and analytical applications. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-139177

PPARα agonist 2	PPAR	Cardiovascular Disease
PPARα agonist 2 (compound 4u) is a potent and selective PPARα agonist with an EC₅₀ of 37 nM. PPARα agonist 2 exhibits >2,700-fold selectivity for PPARα over other PPAR isoforms. PPARα agonist 2 has the potential for retinal disorders research .

HY-13245B

(Rac)-PF-4136309 (Rac)-INCB8761	CCR	Inflammation/Immunology
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which is a potent, selective, and orally bioavailable CCR2 antagonist, with IC₅₀s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

HY-148742

RET-IN-21	RET	Cancer
RET-IN-21 (compound 5) is a selective RET ^V804M inhibitor with the IC₅₀ of 0.02 μM. RET-IN-21 does not inhibit the wild type isoforms of RET or KDR. RET-IN-21 has antitumor activity .

HY-160469

INY-05-040	Akt PROTACs	Cancer
INY-05-040 is a AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines, with anti-cancer activity .

Cat. No.	Product Name

HY-L099

Targeted Diversity Library

2,293 compounds

MCE Targeted Diversity Library contains 2,293 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.

HY-L158

Highly Selective Inhibitors Library

5,438 compounds

According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 5,438 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes

HY-L159

Highly Selective Activators Library

1,793 compounds

Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 1,793 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.

HY-L083

Anti-Cancer Metabolism Compound Library

2,825 compounds

Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.

MCE provides a unique collection of 2,825 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.

Cat. No.	Product Name	Type

HY-17356G

Fenofibrate (GMP)

Fluorescent Dye

Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

Cat. No.	Product Name	Type

HY-17356G

Fenofibrate (GMP)

Biochemical Assay Reagents

Cat. No.	Product Name	Target	Research Area

HY-P5174

MitTx	Sodium Channel	Neurological Disease
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC₅₀ values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .

HY-P2261

STAD 2	PKA	Infection
STAD 2 is a potent and selective disruptor of PKA-RII, with a K_d of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .

HY-P1219

Jingzhaotoxin-III β-TRTX-Cj1α	Sodium Channel	Neurological Disease
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC₅₀ of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-126585

SAICAR 1 Publications Verification	Structural Classification Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Disease Research Fields Cancer	Endogenous Metabolite
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates *pyruvate kinase isoform* M2 (PKM2)** in an isozyme-selective manner, with an EC₅₀ of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .

HY-16482

Teglicar 1 Publications Verification	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC₅₀ value of 0.68 μM and a K_i value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD) .

HY-N2574

Gitogenin 2 Publications Verification	Tribulus terrester Linn. Structural Classification Classification of Application Fields Zygophyllaceae Source classification Metabolic Disease Plants Disease Research Fields Steroids	Glycosidase
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC₅₀ values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .

HY-137295

Ingenol 3,20-dibenzoate	Classification of Application Fields Terpenoids Source classification Diterpenoids Euphorbia esula L. Euphorbiaceae Plants Inflammation/Immunology Disease Research Fields	PKC Apoptosis
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .

HY-111355B

Cholesteryl sulfate sodium	Structural Classification Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields Steroids	Endogenous Metabolite
Cholesteryl sulfate sodium is an orally available, NPC2-targeted cholesterol biosynthesis agonist. Cholesteryl sulfate sodium activates SREBP2 by competitively binding to NPC2, promoting cholesterol synthesis (EC₅₀=50 μM). Cholesteryl sulfate sodium enhances the self-assembly ability of Mitoxantrone hydrochloride (HY-13502A), while repairing the intestinal mucosal barrier and inhibiting inflammation by regulating serine protease activity and PKCη signaling pathway. Cholesteryl sulfate sodium is a component of the platelet cell membrane and supports platelet adhesion. Cholesteryl sulfate sodium also regulates the activity of selective protein kinase C isoforms and modulates the specificity of PI3K, playing a role in keratinocyte differentiation .

HY-N1373A

d-Sophoridine (+)-Sophoridine	Structural Classification Alkaloids Leguminosae Other Alkaloids Source classification Plants Sophora flavescens Aiton	Apoptosis
d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .

HY-N2574R

Gitogenin (Standard)	Tribulus terrester Linn. Structural Classification Zygophyllaceae Source classification Plants Steroids	Reference Standards Glycosidase
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC₅₀ values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .

Cat. No.	Product Name	Chemical Structure

HY-17356S

Fenofibrate-d6
Fenofibrate-d₆ is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

HY-17464S

Cilostazol-d11
Cilostazol-d₁₁ is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-17464S1

Cilostazol-d4
Cilostazol-d₄ is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-17464S2

Cilostazol-d2
Cilostazol-d₂ (OPC 13013-d₂) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-17464S3

Cilostazol-d6
Cilostazol-d₆ (OPC 13013-d₆) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM .

HY-126585S

SAICAR-d3
SAICAR-d₃ is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC₅₀ of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .

HY-17356S2

Fenofibrate-13C6
Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.

HY-17356S1

Fenofibrate-d4
Fenofibrate-d₄ is the deuterium labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC₅₀ of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC₅₀s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively .

HY-10405S

Pamapimod-d4

Pamapimod-d₄ (Ro4402257-d₄) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC₅₀s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .

HY-B0822S1

Fipronil-13C6

Fipronil- ¹³C₆ is the ¹³C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.

Cat. No.	Product Name		Classification

HY-159584

LBG20304		Azide
LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC₅₀: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .

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