Search results for: 'ur 144'
Catalog No.
Product Name
Application
Product Information
Product Citation
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URAT1 inhibitor
UR 1102, inhibitor of the renal urate transporter URAT1 with high selectivity to URAT1 over OAT1 and OAT3 in vitro (Ki values 0.057 uM, 7.2 uM, and 2.4 uM, respectively), capable of increasing the fractional excretion of urinary uric acid, and reducing plasma uric acid more effectively than Benzbromarone. -
irreversible EGFR inhibitor
ASP8273 is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. - Sec-O-glucosylhamaudol is one of the major bioactive compounds of the Saposhnikoviae Radix.
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ER stress inhibitor
Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is an endoplasmic reticulum (ER) stress inhibitor. -
EGFR inhibitor
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFRL858R, EGFRExon 19 deletion and EGFRT790M. -
Bilobalide, a biologically active terpenic trilactone (terpinoid), derived from geranylgeranyl pyrophosphate (GGPP) is an inducer of cytochrome P450 enzymes CYP3A1 and CYP1A2. May contain properties to stop apoptosis activation of the phosphatidylinositol 3-Kinase pathway in SH-SY5Y cells.
- TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.
- Anirudh Sattiraju, .et al. , Immunity, 2023, Aug 8;56(8):1825-1843 PMID: 37451265
- Anirudh Sattiraju, .et al. , bioRxiv, 2022, March 04
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BET inhibitor
GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family -
MEK1 inhibitor
Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. , Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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PI3Kα/δ inhibitor
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). -
HIV-1 integrase inhibitor
HIV-1 integrase inhibitor is uesful for anti-HIV. -
HIV-1 integrase inhibitor
HIV-1 integrase inhibitor 2, in the treatment of human immunodeficiency virus (HIV) infection. -
microtubule inhibitor
Ixabepilone is an epothilone B analog- Dong-Sheng Cao, .et al. , Eur J Med Chem, 2020, Aug 1;199:112421 PMID: 32428794
- Hoque M, .et al. , Pharmacol Res, 2018, Aug;134:166-178 PMID: 29944980
- APRIL L. RISINGER, .et al. , Anticancer Res, 2015, Nov; 35(11): 5845-5850 PMID: 26504006
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Thalidomide-based Cereblon ligand
Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
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NMDA receptors Blocker
Ro 25-6981 is a high-affinity, potent and selective blocker of N-methyl- D-aspartate (NMDA) receptors. -
XOR Inhibitor
Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM. -
Adenosine A3 receptor agonist
CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. -
HIF-PH inhibitor
Molidustat is a novel inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase (PH) which stimulates erythropoietin (EPO) production and the formation of red blood cells. -
FLT3/Axl inhibitor
Gilteritinib is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations.- Mohammad Azhar, .et al. , Blood Adv, 2022, Aug 31 PMID: 36044389
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FGFR1/2/3 inhibitor
Debio-1347 is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity. -
EGFR T790M inhibitor
EGF816 is a novel covalent inhibitor of mutant-selective EGFR; overcomes T790M-mediated resistance in NSCLC. -
c-Met inhibitor
Volitinib is an orally bioavailable inhibitor of the c-Met receptor tyrosine kinase with potential antineoplastic activity. -
Pan-PIM kinase inhibitor
LGB-321 HCl is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor).- Ricardo de Matos Simoes, .et al. , Nat Cancer, 2023, May;4(5):754-773 PMID: 37237081
- Andrea L. Casillas, .et al. , Clin Cancer Res, 2018, Jan 1; 24(1): 169-180 PMID: 29084916
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Mdm2 inhibitor
MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction. -
PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
CDK inhibitor
Palbociclib is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.- Kana Nakatani, .et al. , Int J Hematol, 2020, Oct 17 PMID: 33068248
- Ryohei Ogata, .et al. , Breast Cancer, 2020, Aug 28 PMID: 32860163
- Kishino E, .et al. , Breast Cancer, 2019, Dec 10 PMID: 31823286
- Hidemasa Matsuo, .et al. , Blood Adv, 2018, Nov 13; 2(21): 2879-2889 PMID: 30381403
- Zhihong Li, .et al. , J Med Chem, 2014, Apr 24;57(8):3430-49 PMID: 24641103
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NK1 receptor antagonist
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist. It competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). -
NOX1/4 inhibitor
GKT137831 is a first in class inhibitor targeting NOX1 and NOX4 enzymes.- Chia-Hui Huang, .et al. , Toxicol Appl Pharmacol, 2020, Apr 17;397:115013 PMID: 32305283
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5-HT2A receptor agonist
Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. -
NRT inhibitor
Elvucitabine is an experimental nucleoside reverse transcriptase inhibitor (NRTI).
