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PK7088 is a pyrazole and a specific peptide. PK7088 supports the reactivation of mutant p53 by converting it to a form exhibiting wild-type properties. PK7088 exhibit anticancer activity in cancer research .
PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels .
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
PK-THPP is a potent and brain-penetrant TWIK-related acid-sensitive K + ion channel (K2P9.1 or TASK-3) blocker with IC50s of 35 nM and 300 nM for TASK-3 and TASK-1, respectively. PK-THPP shows no or less activity against other K + channels. PK-THPP is an effective breathing stimulant and can be used for the study of breathing disorders .
PK 130 is a 2-nitroimidazole derivative that has radiosensitizing effects on hypoxic cells. PK 130 increases the radiosensitivity of Chinese hamster V79 cells under hypoxic conditions .
PK-10 is a synergistic antibacterial agent of Fluconazole (HY-B0101) and has strong antifungal activity against a variety of Fluconazole-resistant Candida albicans strains. PK-10 combined with Fluconazole can inhibit hyphae formation and induce the accumulation of reactive oxygen species. It further causes damage to mitochondrial membrane potential, reduces intracellular ATP content, and leads to mitochondrial dysfunction .
Quinacainol (PK 10139) is an inhibitor for sodium current with an EC50 of 95 µM. Quinacainol exhibits antiarrhythmic activity by affecting the electrophysiological properties of the heart .
PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis .
Quinacainol dihydrochloride (PK 10139 dihydrochloride) is the dihydrochloride salt form of Quinacainol (HY-19679). Quinacainol dihydrochloride is an inhibitor for sodium current with an EC50 of 95 µM. Quinacainol dihydrochloride exhibits antiarrhythmic activity by affecting the electrophysiological properties of the heart .
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 μM, respectively .
PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
Pipequaline (Standard) is the analytical standard of Pipequaline. This product is intended for research and analytical applications. Pipequaline (PK 8165) is a partial benzodiazepine receptor agonist with anxiolytic activity .
Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19 .
Homocarbonyltopsentin (PK4C9) is a small-molecule TSL2-binding compound, binds to pentaloop conformations of TSL2 and promotes a shift to triloop conformations that display enhanced SMN2 exon 7 (E7) splicing with EC50 value of 16 μM .
Riluzole- 13C6 (PK 26124- 13C6) is 13C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Riluzole hydrochloride is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Riluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension .
PKRA83 (PKRA7) is a potent prokineticin (PK2) antagonist, which can compete for the binding of PK2 to its receptors PKR1 and PKR2. PKRA83 potently inhibits PK2 receptors, with IC50 values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 has anticancer, anti-arthritis and anti-angiogenic activities. PKRA83 can penetrate the blood-brain barrier .
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole . Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM .
DNA-PK-IN-2 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-2 has the potential for the research of cancer diseases (extracted from patent WO2021136462A1, compound 1) .
DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4) .
DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1) .
DNA-PK-IN-4 is a potent inhibitor of DNA-PK. DNA-PK-IN-4 is a imidazolinone derivative compound. DNA-PK-IN-4 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021209055A1, compound 27) .
DNA-PK-IN-9 (compound YK6) is a potent DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 10.47 nM. DNA-PK-IN-9 can be used for researching anticancer .
DNA-PK-IN-14 (compound 78) is a potent, selective DNA-PK inhibitor with an IC50 value of 7.95 nM. DNA-PK-IN-14 has oral activity and has the potential to be a radiosensitizer for cancer treatment .
DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .
DNA-PK-IN-12 (compound 31t) is an oral active DNA-PK inhibitor with the IC50 of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC50 of 33.28 μM, and shows antitumor activity in vivo .
Pyruvate Kinase (PK),Rabbit Muscle (ATP:Pyruvate 2-0-phosphotransferase,PK) is a biological material or organic compound that can be used in life science research .
DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2) .
DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6) .
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
EGFR-PK/JNK-2-IN-1 (Compound 6c) is a dual inhibitor of EGFR-PK and JNK-2 with IC50s of 2.7 and 3.0 μM, respectively. EGFR-PK/JNK-2-IN-1 can induce apoptosis and induce cell cycle arrest at different cell phases. EGFR-PK/JNK-2-IN-1 can be used for the research of cancer .
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
HBV-IN-25 is a good potency, orally active novel HBV cccDNA reducer. HBV-IN-25 has anti-HBeAg potency and anti-HBV activity with IC50 values of 0.58 μM and 1.15 μM, respectively. HBV-IN-25 has good aqueous solubility (LYSA＞452 μg/mL) and good PK property with no cellular toxicity .
Hexadecenyl-2-hydroxy-sn-glycero-3-PC (C16(Plasm) LPC) is a phosphatidylcholine. Hexadecenyl-2-hydroxy-sn-glycero-3-PC prolongs the lag-phase of α-syn aggregation, and can be used in Parkinson’s disease research .
ZPD-2 inhibits the aggregation of C-terminally truncated and full-length α-synuclein. ZPD-2 inhibits the formation and fibrillation of α-Syn, thereby preventing its propagation. ZPD-2 can be used in research of Parkinson's disease .
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain .
LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines .
Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency .
Mitapivat hemisulfate is an orally active pyruvate kinase allosteric activator. Mitapivat hemisulfate increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat hemisulfate can be used in study of PK deficiency .
Mitapivat hemisulfate sesquihydrate (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency .
PfGSK3/PfPK6-IN-2 is a potent dual PfGSK3/PfPK6 (Plasmodium falciparumGSK3/PK6) inhibitor (IC50: 172 nM and 11 nM respectively). PfGSK3/PfPK6-IN-2 can be used in the research of Malaria .
KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively .
Protein kinase affinity probe 1 is a novel protein kinase affinity probe for the functional identification of protein kinases (PKs). Protein kinase affinity probe 1 is a modified Purvalanol B (HY-18299) probe with 50% beads loading (Compound S3) .
Andrimid is a lipoacyl peptide with polyketide-nonribosomal peptide hybrid products (PK-NRPs). Andrimid can be widely applied in biomedical and biological agriculture .
SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
Mitapivat (AG-348) hydrochloride is an orally active and selective allosteric pyruvate kinase R (PK-R) activator. Mitapivat hydrochloride accelerates the reaction of PK-R catalyzing the conversion of phosphoenolpyruvate to pyruvate, thereby promoting the glycolytic pathway, increasing the production of adenosine triphosphate (ATP) in red blood cells, and reducing the level of 2,3-diphosphoglycerate (2,3-DPG). Mitapivat hydrochloride is promising for research of pyruvate kinase deficiency and other anemia-related diseases .
2-AHA-cAMP is an analogue of natural signal molecule cAMP and an activator of cAMP-dependent protein kinase. 2-AHA-cAMP has a free terminal primary amino group, which can be used for coupling to gels or fluorescent dyes .
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 hydrochloride induces apoptosis .
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 induces apoptosis .
XEN445 is an endothelial lipase (EL) inhibitor with an IC50 of 0.237 uM. It has excellent ADME and PK activity and can increase the concentration of high-density lipoprotein cholesterol in mouse plasma.
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator .
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC50=81 nM). BAY-8400 can be used for the research of cancer .
Deoxytopsentin is a compound that can be found in marine sponges. It is an inhibitor of pyruvate kinase (PK) in methicillin-resistant Staphylococcus aureus (MRSA), with an IC50 value of 240 nM. Deoxytopsentin can be used in research in the field of anti-infection .
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research .
AN7973 is the 6-carboxamide benzoxaborole, blocks intracellular parasite development and inhibits Cryptosporidium growth. AN7973 is orally active, possesses favorable safety, stability, and PK parameters, and is an exciting agent candidate for treating cryptosporidiosis.
LY294002 (Standard) is the analytical standard of LY294002. This product is intended for research and analytical applications. LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC50 of 98 nM . LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4?μM. LY294002 is an apoptosis activator .
BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity .
KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
PF-06455943 is a leucine rich repeat kinase 2 (LRRK2) inhibitor with IC50 value of 3 nM. PF-06455943 also is a PET radioligand. PF-06455943 can be used for the research of ADME/neuro PK characterization and Parkinson disease (PD) .
ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively .
7-Ketositosterol is a phytosterol isolated from the fruits of the mulberry tree (Morus alba L.). 7-Ketositosterol can significantly inhibit Cisplatin (HY-17394)-induced apoptosis in LLC-PK1 cells and has the potential to improve Cisplatin-induced nephrotoxicity .
NU-7163 is an ATP-competitive DNA-PK inhibitor (IC50=0.19 μM; Ki=24 nM). NU-7163 enhances the cytotoxicity of ionizing radiation against the HeLa human tumor cell line in vitro .
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
Yhhu6669 is an anti-HBV agent. Yhhu6669 inhibits HBV DNA. Yhhu6669 inhibits HBV replication by inducing the formation of DNA-free capsids. Yhhu6669 decreases HBV DNA and HBcAg in AAV/HBV-infected mice. Yhhu6669 has favorable PK properties .
Glucosylceramide synthase-IN-4 (compound 12) is a potent glucosylceramide synthase (GCS) inhibitor, with an IC50 of 6.8 nM. Glucosylceramide synthase-IN-4 shows excellent PK properties and stability in human hepatocytes. Glucosylceramide synthase-IN-4 has good CNS penetration and acceptable PXR selectivity .
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
Axl-IN-19 (Compound 68) is a selective AXL (a membrane-bound receptor tyrosine kinase) inhibitor (IC50: 5.3 nM; Cellular KD = 6.8 nM). Axl-IN-19 has favorable rat PK with low clearance and moderate bioavailability. Axl-IN-19 can be used for cancer research .
Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar .
URAT1&XO inhibitor 3 (compound 27) is an orally active anti-gout agent targeting XO (IC50: 35 nM) and URAT1 (IC50: 31 nM). URAT1&XO inhibitor 3 has good pharmacological and pharmacokinetic (PK) characteristics and in vivo safety .
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research .
EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes .
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC50 of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC50s of 5.0 and 1.7 μM, respectively .
IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile .
SC-75416 is a selective cyclooxygenase-2 inhibitor. Its pharmacokinetic/pharmacodynamic (PK/PD) model was used for development and clinical trial simulation to design a study protocol to verify its analgesic effect in a post-oral surgery pain model. The simulation results showed that 360 mg of SC-75416 may provide better pain relief than 400 mg of ibuprofen. The actual clinical trial results confirmed this hypothesis, and 360 mg of SC-75416 was indeed superior to 400 mg of ibuprofen in pain relief. The PK/PD model of SC-75416 showed good predictive performance and successfully predicted its clinical effect. These research results show that SC-75416, as a new selective COX-2 inhibitor, has potential clinical application value in the management of post-oral surgery pain.
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment .
Irpagratinib (ABSK011) is an orally active FGFR4 inhibitor (IC50<10 nM). Irpagratinib inhibits FGFR4 autophosphorylation and blocks signaling from FGFR4 to downstream pathway activation. Irpagratinib has shown high exposure in PK studies in mice, rats, and dogs, and also demonstrated antitumor activity in a subcutaneous xenograft tumor model .
UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
Pheromonotropin (Pseudaletia separata) (Pss-PT) is an armyworm (Pseudaletia separata) pheromone with the C-terminal pentapeptide FXPRL-amide. Pheromonotropin (Pseudaletia separata) belongs to the PK/PBAN family and stimulates sex pheromone biosynthesis in moths, mediating feeding (intestinal muscle contraction), development (embryonic diapause, pupal diapause, and pupation), and defense against natural enemy insects wait .
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .
Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity .
ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals .
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
D-Xylulose 5-phosphate (sodium) is a pentose phosphate ester and an essential intermediate metabolite in the pentose phosphate pathway (PPP) and the non-oxidative phase of the pentose phosphate pathway. D-xylulose-5-phosphate can be efficiently synthesized through the phosphorylation of D-xylulose catalyzed by D-xylulokinase (XKS1 from Saccharomyces cerevisiae), with ATP regeneration facilitated by the phosphoenolpyruvate (PEP)/pyruvate kinase (PK) system .
Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies .
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects .
Flubi-2 is a fluorescein-biotin based pH-ratio dye (Ex=480 nm, Em= 520-560 nm) with a pK value of 6.7. Flubi-2 is a hydrolysis product of Flubida-2 (non-fluorescent, membrane permeable). Flubi-2 can be used for pH determination of organelles of the secretory pathway (such as golgi apparatus and endoplasmic reticulum) in living cells .
Cimicoxib (Standard) is the analytical standard of Cimicoxib. This product is intended for research and analytical applications. Cimicoxib (CX) is an orally active potent and selective COX-2 (cyclo-oxygenase-2) inhibitor. Cimicoxib exhibits promising anti-inflammatory and analgesic activity. The PK parameters of Cimicoxib in dogs given precise (2 mg/kg) and approximate doses (1.95-2.5 mg/kg) are similar .
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis . GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC50 of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC50=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets .
PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used for cancer research .
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .
PolQi2 is a PolΘ inhibitor that targets and inhibits alt-EJ (alternative end-joining) repair by inhibiting the helicase domain at the N-terminus of PolΘ. PolQi2 enhances the precision and integration efficiency of gene editing at different loci and in various cell lines. Furthermore, the combined use of PolQi2 with DNA-PK inhibitors reduces the off-target effects of Cas9. PolQi2 can be used in gene editing research .
IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .
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 .
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy .
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity .
Sp-5,6-DCl-cBIMPS sodium is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS sodium stimulates insulin release. Sp-5,6-DCl-cBIMPS sodium inhibits U-46619 (HY-108566)-induced activation of Rho, Gq and G12/G13 in platelets .
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy .
Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
A 62176 hydrochloride is a compound that targets DNA topoisomerase II and has the activity of inhibiting purine synthesis in cancer cells. A 62176 hydrochloride interferes with c-MYC mRNA expression by interacting with G-quadruplex. The main mechanism of action of A 62176 hydrochloride is by displacing nucleosomes from the quadruplex of non-template strand rDNA, resulting in rapid redistribution of nucleosomes. The application potential of A 62176 hydrochloride is that it causes DNA damage and relies on BRCA1/2-mediated homologous recombination and DNA-PK-mediated non-homologous end-joining pathways to repair the damage .
hURAT1 inhibitor 1 (compound 27b) is an isomarine-based, orally active dual hURAT1/GLUT9 inhibitor with IC50s of 0.16 μM and 4.47 μM, respectively, and has anti-hyperuricemia effects. hURAT1 inhibitor 1 showed significant uric acid-lowering activity in a hyperuricemia mouse model (10 mg/kg dose). hURAT1 inhibitor 1 had no significant in vitro cytotoxicity or in vivo hepatotoxicity and showed good PK characteristics .
PSMA-trillium is a PSMA targeting compound, consisting of a PSMA targeting molecule (PSMA binder), a Macropa chelating molecule, and a group that regulates pharmacokinetics (PK modifier). PSMA-trillium is a non-radioactive form of Actinium-225-PSMA-Trillium (BAY 3563254) with improved PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind Ac through the Macropa chelating molecule, or the radioactive isotope 225Actinium. Actinium-225-PSMA-Trillium is a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC) .
ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer .
PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals. PLX5622 is predominantly administered via ad libitum diets. Custom diet of PLX5622 (1200 ppm in AIN-76A) (HY-114153C) is available from MedChemExpress (MCE) .
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43?nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150?nM) and mTOR (IC50=157?nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the pharmacokinetic properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound .
(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research .
EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .
PI-103 (Standard) is the analytical standard of PI-103. This product is intended for research and analytical applications. PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy .
PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM) .
PI-103 (Hydrochloride) (Standard) is the analytical standard of PI-103 (Hydrochloride). This product is intended for research and analytical applications. PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy .
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
R1-ICR-5 is a selective PROTAC degrader that targets serine/threonine-protein kinase 1 (RIPK1). R1-ICR-5 mediates the degradation of RIPK1 through VHL, thereby deregulating the TNFR1 and TLR3/4 signaling hubs, enhancing the output of NF-κB, MAPK, and IFN signaling, and simultaneously promoting the activation of RIPK3 and the induction of necroptosis. R1-ICR-5 is promising for research of cancers and inflammatory diseases. (Pink: PK68 (HY-128348); Black: linker (HY-W012241); Blue: (S,R,S)-AHPC (HY-125845) .
PolQi1 is a selective inhibitor targeting the Polθ domain of DNA polymerase. PolQi1 inhibits the Polθ-mediated microhomology end joining (TMEJ/alt-EJ) pathway, reducing insertion/deletion (Indels) and imprecise editing events during DNA repair. PolQi1 can enhance the efficiency and accuracy of homology-directed repair (HDR) or Prime editing, and reduce off-target effects; and in combination with DNA-PK inhibitor AZD-7648 (HY-111783), exert efficient genome editing capabilities with dual pathway regulation. PolQi1 can be mainly used in gene editing research (such as CRISPR-Cas9 or Prime editing system optimization) to improve the precision editing efficiency of difficult-to-edit cells (such as primary hepatocytes and mouse embryos) .
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B(pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B(pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
Frovatriptan (succinate hydrate) (Standard) is the analytical standard of Frovatriptan (succinate hydrate). This product is intended for research and analytical applications. Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
The MCE 1K Drug Fragment Library consists of 1,168 drug fragments. These drug fragments are derived from 2,946 FDA-approved drug molecules, and fragments from one drug can appear in other drugs, so these fragments are somewhat correlated with good PK/PD properties. Fragment-based screening can reserve enough chemical space for subsequent structural optimization. This compound library is an essential tool for drug screening based on FBDD (Fragment-Based Drug Discovery).
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.
MCE owns a unique collection of 793 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.
DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 2,624 cell cycle/DNA damage-related compounds which can be used in the research of the same.
Macrocycles, molecules containing 12-membered or larger rings, are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, showing favorable ADME- and PK-properties. Macrocycles have demonstrated repeated success when addressing targets that have proved to be highly challenging for standard small-molecule drug discovery, especially in modulating macromolecular processes such as protein–protein interactions (PPI). Otherwise, the size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity.
MCE offers a unique collection of 405 macrocyclic compounds which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE Macrocyclic Compound Library is a useful tool for discovering new drugs, especially for “undruggable” targets and protein–protein interactions.
AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity .
Flubi-2 is a fluorescein-biotin based pH-ratio dye (Ex=480 nm, Em= 520-560 nm) with a pK value of 6.7. Flubi-2 is a hydrolysis product of Flubida-2 (non-fluorescent, membrane permeable). Flubi-2 can be used for pH determination of organelles of the secretory pathway (such as golgi apparatus and endoplasmic reticulum) in living cells .
AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity .
DNA-PK Substrate is a biological active peptide. (A substrate for DNA-dependent protein kinase (DNA-PK), phosphorylation. DNA-PK is essential for the repair of DNA double-strand breaks. This peptide corresponding to 11–24 amino acids of human p53 with threonine 18 and serine 20 changed to alanine is used as a substrate for the assay of DNA-PK activityPyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Kemptide (amide) is a heptapeptide with properties of a cytophilic substrate. Kemptide is a molecule preserving cell membrane intactness, is phosphorylated by PKI, the inhibitory protein specific for cAMP-dependent protein kinase (PK) .
Pheromonotropin (Pseudaletia separata) (Pss-PT) is an armyworm (Pseudaletia separata) pheromone with the C-terminal pentapeptide FXPRL-amide. Pheromonotropin (Pseudaletia separata) belongs to the PK/PBAN family and stimulates sex pheromone biosynthesis in moths, mediating feeding (intestinal muscle contraction), development (embryonic diapause, pupal diapause, and pupation), and defense against natural enemy insects wait .
Andrimid is a lipoacyl peptide with polyketide-nonribosomal peptide hybrid products (PK-NRPs). Andrimid can be widely applied in biomedical and biological agriculture .
Deoxytopsentin is a compound that can be found in marine sponges. It is an inhibitor of pyruvate kinase (PK) in methicillin-resistant Staphylococcus aureus (MRSA), with an IC50 value of 240 nM. Deoxytopsentin can be used in research in the field of anti-infection .
7-Ketositosterol is a phytosterol isolated from the fruits of the mulberry tree (Morus alba L.). 7-Ketositosterol can significantly inhibit Cisplatin (HY-17394)-induced apoptosis in LLC-PK1 cells and has the potential to improve Cisplatin-induced nephrotoxicity .
PKM2 protein catalyzes the final step of glycolysis, transferring a phosphoryl group from PEP to ADP to generate ATP.In the nucleus, transcriptional activation of PKM2 contributes to cancer progression, promoting cell proliferation and tumorigenesis.PKM2 is also involved in caspase-independent cell death in tumors.PKM2 Protein, Mouse (Baculovirus, His) is the recombinant mouse-derived PKM2 protein, expressed by Sf9 insect cells , with N-10*His labeled tag.
The PKLR protein is a key enzyme in cellular metabolism that acts as a pyruvate kinase, converting phosphoenolpyruvate to pyruvate. This process is an integral part of glycolysis, the fundamental pathway for cellular energy production. PKLR Protein, Human (HEK293, His) is the recombinant human-derived PKLR protein, expressed by HEK293 , with C-6*His labeled tag.
PIK3C3; Phosphatidylinositol 3-kinase catalytic subunit type 3; PI3-kinase type 3; PI3K type 3; PtdIns-3-kinase type 3; Phosphatidylinositol 3-kinase p100 subunit; Phosphoinositide-3-kinase class 3; hVps34
The PI3KC3 protein is the catalytic subunit of the PI3K complex and mediates the formation of phosphatidylinositol 3-phosphate. PI3KC3-C1 initiates autophagosomes, whereas PI3KC3-C2 promotes autophagosome maturation and endocytosis. PK3C3 Protein, Human (sf9, His, GST) is the recombinant human-derived PK3C3 protein, expressed by sf9 insect cells , with N-8*His, N-GST labeled tag.
The AKT1 protein is part of the AKT kinase family and is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage through inhibition of GSK3A/B. AKT1 Protein, Human (sf9, His) is the recombinant human-derived AKT1 protein, expressed by Sf9 insect cells , with C-10*His labeled tag.
The PKLR protein is a pyruvate kinase that plays a critical role in glycolysis, converting phosphoenolpyruvate to pyruvate and producing ATP.As a key enzyme, PKLR mediates the final steps of glycolysis, contributing to energy production.PKLR Protein, Rat (P.pastoris, His) is the recombinant rat-derived PKLR protein, expressed by P.pastoris , with N-6*His labeled tag.
The MAPKAPK3 protein is a stress-activated kinase involved in multiple cellular processes, including cytokine production and endocytosis. It is phosphorylated by p38-alpha/MAPK14 during stress, targets specific substrates, and has similarities to MAPKAPK2 but is less active. MAPKAPK3 Protein, Human (Active, sf9, GST) is the recombinant human-derived MAPKAPK3, expressed by Sf9 insect cells , with GST labeled tag. ,
MELK is a multifunctional serine/threonine protein kinase that regulates the cell cycle, stem cell self-renewal, apoptosis, and splicing. MELK phosphorylates BCL2L14, CDC25B, MAP3K5/ASK1 and ZNF622, activates apoptosis through MAP3K5/ASK1, helps CDC25B localize during mitosis, and inhibits BCL2L14, which may affect breast cancer occurrence. MELK Protein, Human is the recombinant human-derived MELK protein, expressed by E. coli , with tag free.
MELK is a multifunctional serine/threonine protein kinase that regulates the cell cycle, stem cell self-renewal, apoptosis, and splicing. MELK phosphorylates BCL2L14, CDC25B, MAP3K5/ASK1 and ZNF622, activates apoptosis through MAP3K5/ASK1, helps CDC25B localize during mitosis, and inhibits BCL2L14, which may affect breast cancer occurrence. MELK Protein, Human (His) is the recombinant human-derived MELK protein, expressed by E. coli , with N-6*His labeled tag.
PFKFB1 protein orchestrates the synthesis and degradation of fructose 2,6-bisphosphate, regulating cellular energy metabolism. Serving as a key enzyme, PFKFB1 modulates fructose 2,6-bisphosphate levels, impacting glycolysis and gluconeogenesis. Its dual role in both synthesis and breakdown is crucial for maintaining cellular energy homeostasis, ensuring adaptability to changing energy demands and environmental conditions. PFKFB1 Protein, Human (HEK293, His) is the recombinant human-derived PFKFB1 protein, expressed by HEK293 , with C-6*His labeled tag.
The AKT1 protein is part of the AKT kinase family and is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage through inhibition of GSK3A/B. AKT1 Protein, Human (Active, sf9, GST) is the recombinant human-derived AKT1, expressed by Sf9 insect cells , with GST labeled tag.
The AKT2 protein is a serine/threonine protein kinase in the AKT family that is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage. AKT2 Protein, Human (Active, sf9, GST) is the recombinant human-derived AKT2, expressed by Sf9 insect cells , with GST labeled tag.
The AKT3 protein, like AKT1 and AKT2, is an important member of the AKT kinase family and plays a central role in a variety of cellular processes, including metabolism, proliferation, survival, growth, and angiogenesis. AKT3 has more than 100 reported targets and coordinates complex signaling pathways that control glucose uptake, regulate glycogen storage, and influence neurogenesis. AKT3 Protein, Human (Active, sf9, GST) is the recombinant human-derived AKT3, expressed by Sf9 insect cells , with GST labeled tag.
Riluzole- 13C, 15N2 is the 13C and 15N labeled Riluzole . Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM .
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
Riluzole- 13C6 (PK 26124- 13C6) is 13C labeled Riluzole. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na + channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
Valiltramiprosate-d6 (ALZ-801-d6) is deuterium labeled Valiltramiprosate. ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound . ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
PKM2 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 58 kDa, targeting to PKM2. It can be used for WB,IHC-P,ICC/IF,FC assays with tag free, in the background of Human, Mouse, Rat.
Phospho-PKM2(Tyr105)Antibody is a rabbit-derived non-conjugated IgG antibody, targeting Phospho-PKM2(Tyr105)Antibody, with a predicted molecular weight of 58 kDa. Phospho-PKM2(Tyr105)Antibody can be used for IHC-P, IHC-F, ICC/IF, FC, ELISA experiments in human, rat backgrounds.
DNA PKcs Antibody (YA957) is a mouse-derived non-conjugated IgG1 antibody (Clone NO.: YA957), targeting DNA PKcs, with a predicted molecular weight of 469 kDa (observed band size: 450 kDa). DNA PKcs Antibody (YA957) can be used for WB, IHC-F, IHC-P, ICC/IF, IP experiment in human background.
DNA PKcs Antibody (YA959) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA959), targeting DNA PKcs, with a predicted molecular weight of 469 kDa (observed band size: 469 kDa). DNA PKcs Antibody (YA959) can be used for WB, IHC-P, ICC/IF experiment in human, mouse, rat background.
Phospho-DNA PKcs (Ser2056) Antibody (YA1823) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1823), targeting Phospho-DNA PKcs (Ser2056), with a predicted molecular weight of 469 kDa (observed band size: 469 kDa). Phospho-DNA PKcs (Ser2056) Antibody (YA1823) can be used for WB, IHC-P, ICC/IF experiment in human background.
AKT1; PKB; RAC; RAC-alpha serine/threonine-protein kinase; Protein kinase B; PKB; Protein kinase B alpha; PKB alpha; Proto-oncogene c-Akt; RAC-PK-alpha
ICC/IF, WB, IHC-F, IHC-P, ELISA
Human, Mouse, Rat
Phospho-AKT (Thr308) Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 56 kDa, targeting to Phospho-AKT (Thr308). It can be used for ICC/IF,WB,IHC-F,IHC-P,ELISA assays with tag free, in the background of Human, Mouse, Rat.
AKT1; PKB; RAC; RAC-alpha serine/threonine-protein kinase; Protein kinase B; PKB; Protein kinase B alpha; PKB alpha; Proto-oncogene c-Akt; RAC-PK-alpha
WB
Human, Mouse, Rat
Phospho-AKT1 (Ser473) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 56 kDa, targeting to Phospho-AKT (Ser473). It can be used for WB assays with tag free, in the background of Human, Mouse, Rat.
EG VEGF Antibody (YA2991) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2991), targeting EG VEGF, with a predicted molecular weight of 12 kDa (observed band size: 12 kDa). EG VEGF Antibody (YA2991) can be used for WB, FC experiment in human, mouse background.
DNA PKcs Antibody (YA958) is a mouse-derived non-conjugated IgG2b antibody (Clone NO.: YA958), targeting DNA PKcs, with a predicted molecular weight of 469 kDa (observed band size: 450 kDa). DNA PKcs Antibody (YA958) can be used for WB, ICC/IF, IP experiment in human background.
MELK; KIAA0175; Maternal embryonic leucine zipper kinase; hMELK; Protein kinase Eg3; pEg3 kinase; Protein kinase PK38; hPK38; Tyrosine-protein kinase MELK
WB
Human
MELK Antibody (YA1423) is a non-conjugated IgG antibody, targeting MELK, with a predicted molecular weight of 75 kDa (observed band size: 75 kDa). MELK Antibody (YA1423) can be used for WB experiment in human background.
MAPKAPK3; MAP kinase-activated protein kinase 3; MAPK-activated protein kinase 3; MAPKAP kinase 3; MAPKAP-K3; MAPKAPK-3; MK-3; Chromosome 3p kinase; 3PK
WB, IP
Human
MAPKAP Kinase 3 Antibody (YA3070) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3070), targeting MAPKAP Kinase 3, with a predicted molecular weight of 43 kDa (observed band size: 43 kDa). MAPKAP Kinase 3 Antibody (YA3070) can be used for WB, IP experiment in human background.
AKT 1 antibody; AKT antibody; AKT1 antibody; AKT1_HUMAN antibody; MGC99656 antibody; PKB antibody; PKB-ALPHA antibody; PRKBA antibody; Protein Kinase B Alpha antibody; Protein kinase B antibody; Proto-oncogene c-Akt antibody; RAC Alpha antibody; RAC antibody; RAC-alpha serine/threonine-protein kinase antibody; RAC-PK-alpha antibody;
WB, ICC/IF, IHC-P
Human, Mouse, Rat, Dog
Phospho-Akt1(Ser473) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 56 kDa, targeting to Phospho-Akt1(Ser473). It can be used for WB,ICC/IF,IHC-P assays with tag free, in the background of Human, Mouse, Rat, Dog.
PIK3CA Antibody is an unconjugated, approximately 110 kDa, rabbit-derived, anti-PIK3CA monoclonal antibody. PIK3CA Antibody can be used for: WB, ICC/IF, IP expriments in human, mouse, rat background without labeling.
PIK3CA Antibody is an unconjugated, approximately 110 kDa, rabbit-derived, anti-PIK3CA monoclonal antibody. PIK3CA Antibody can be used for: WB, ICC/IF, IP expriments in human, mouse, rat background without labeling.
Alpha CaMKII; Calcium calmodulin dependent protein kinase II; Calcium/calmodulin dependent protein kinase II alpha B subunit; Calcium/calmodulin dependent protein kinase type II alpha chain; Calcium/calmodulin-dependent protein kinase (CaM kinase) II alpha; Calcium/calmodulin-dependent protein kinase II alpha; Calcium/calmodulin-dependent protein kinase II-alpha; Calcium/calmodulin-dependent protein kinase type II subunit alpha; Calcium/calmodulin-dependent protein kinase type IIA; CaM kinase II alpha chain; CaM kinase II alpha subunit; CaM kinase II subunit alpha; CaMK II alpha subunit; CaMK-II subunit alpha; Camk2a; CAMKA; CaMKII; CaMKIINalpha; EC2.7.11.17; KCC2A_HUMAN; KIAA0968; MGC123320; MGC139375; MGC155201; mKIAA0968; PK2CDD; PKCCD; R74975; zgc:112538; zgc:123320;
WB, IP, FC, IHC-P
Human, Mouse, Rat
CaMKII alpha Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 54 kDa, targeting to CaMKII alpha. It can be used for WB,IP,FC,IHC-P assays with tag free, in the background of Human, Mouse, Rat.
phospho-PI3 Kinase p110 beta (Ser1070) Antibody is an unconjugated, approximately 110-123 kDa, rabbit-derived, anti-phospho-PI3 Kinase p110 beta (Ser1070) polyclonal antibody. phospho-PI3 Kinase p110 beta (Ser1070) Antibody can be used for: WB, IHC-P, IHC-F, IF expriments in human, mouse, rat, and predicted: chicken, dog, pig, cow, horse, guinea pig background without labeling.
Hexadecenyl-2-hydroxy-sn-glycero-3-PC (C16(Plasm) LPC) is a phosphatidylcholine. Hexadecenyl-2-hydroxy-sn-glycero-3-PC prolongs the lag-phase of α-syn aggregation, and can be used in Parkinson’s disease research .
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