About 23 results found for searched term "GS87" (0.052 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M1932 | GSK1838705A | ALK |
| GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and the insulin receptor with IC50s of 2.0 and 1.6 nmol/L, respectively. | ||
| M2033 | GSK 3787 | PPAR |
| GSK3787 | ||
| GSK3787 is an orally available selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6). | ||
| M5212 | GSK2879552 | Histone demethylase |
| GSK2879552 is an effective, selective, bioactive and irreversible LSD1 inhibitor with Kiapp=1.7 μM. | ||
| M8648 | GS87 | Others |
| GS87 is a highly specific GSK3 (glycogen synthase kinase 3) inhibitor that induces extensive differentiation of AML cells. | ||
| M9074 | GSK872 | RIPK |
| GSK-872 | ||
| GSK872 is a receptor interacting protein kinase-3 (RIP3) inhibitor, which inhibits kinase activity with an IC50 of 1.3 nM. | ||
| M10625 | GSK2193874 | TRP Channel |
| GSK-2193874; GSK2193874A | ||
| GSK2193874 is a first-in-class orally bioavailable potent antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist with IC50 values of 2, 5, and 40 nM. GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor that demonstrated ability to improve pulmonary functions in a number of heart failure models. | ||
| M10637 | GSK3368715 2HCl | PRMTs |
| EPZ019997 2HCl | ||
| GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively. | ||
| M10921 | GSK2879552 dihydrochloride | Histone demethylase |
| GSK2879552 2HCl | ||
| GSK2879552 dihydrochloride is an oral, irreversible LSD1/KDM1A inhibitor with antitumor activity. | ||
| M13555 | GSK-872 hydrochloride | RIPK |
| GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. | ||
| M14280 | GSK2798745 | TRP Channel |
| GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. | ||
| M20799 | GS-9876 (lanraplenib) | Syk |
| GS-SYK | ||
| Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans. | ||
| M21259 | GSK2818713 | HCV Protease |
| GSK2818713 is an HCV NS5A replication complex inhibitor with an interesting biphenyl ligand. | ||
| M21394 | GSK3368715 3HCl | Others |
| GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8, corresponding to Kiapp values ranging from 1.5 nM to 81 nM. | ||
| M28389 | GSK2818713 | Anti-infection |
| GSK2818713 is a novel Hepatitis C NS5A replication complex inhibitor. | ||
| M28392 | GSK8175 | Anti-infection |
| GSK2878175 | ||
| GSK8175 is a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV). GSK8175 is a sulfonamide- N-benzoxaborole analog with low in vivo clearance across preclinical species and broad-spectrum activity against HCV replicons. | ||
| M28726 | GSK3368715 | Histone Methyltransferase |
| EPZ019997 | ||
| GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity. | ||
| M29155 | Tilpisertib | Serine/Threonine Protease |
| GS-4875 | ||
| Tilpisertib (GS-4875) is a serine/threonine kinase inhibitor (WO2017007689). | ||
| M29363 | GSK3395879 | TRP Channel |
| GSK3395879 is a selective and orally bioavailable transient receptor potential vanilloid-4 (TRPV4) antagonist with an IC50 of 1 nM for hTRPV4. | ||
| M29748 | GSK3987 | Liver X Receptor |
| GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation. | ||
| M30118 | Aplaviroc hydrochloride | CCR |
| AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride | ||
| Aplaviroc (AK 602) hydrochloride, a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW. | ||
| M30120 | Aplaviroc | CCR |
| AK 602; GSK 873140; GW 873140 | ||
| Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW. | ||
| M40947 | Inotersen | Transthyretin (TTR) |
| GSK-2998728; ISIS-420915 | ||
| Inotersen is an antisense oligonucleotide that inhibits the production of the hepatic transthyretin (TTR) protein. It can be used in studies related to TTR-mediated amyloidosis. | ||
| M49930 | Lanraplenib succinate | Syk |
| GS-9876 succinate | ||
| Lanraplenib succinate is a potent, highly selective and orally active splenic tyrosine kinase (SYK) inhibitor and inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor with an IC50 value of 9.5 nM. | ||
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