About 34 results found for searched term "SK1-IN-1" (0.082 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M9229 | GS-444217 | p38 MAPK |
| ASK1-IN-1 | ||
| GS-444217 is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87±0.85 nM. | ||
| M13395 | SK1-IN-1 | SPHK |
| Sk1-in-1 is an effective sphingosine kinase 1 (SPHK1) inhibitor with an IC50 value of 58 nM. | ||
| M20679 | SKLB4771 (FLT3-IN-1) | FLT3 |
| SKLB4771 is a potent and selective inhibitor of human receptor-type tyrosine-protein kinase FLT3 with IC50 of 10 nM. | ||
| M58401 | ASK1-IN-1 | MAPKAPK2/MAP3K/MAP4K |
| ASK1-IN-1 is a novel CNS-penetrant apoptosis signal-regulating kinase 1 (ASK1) inhibitor with good potency (cell IC50 = 138 nM), low clearance (rat Cl/Clu = 0.36/6.7 L h-1 kg-1) and good CNS penetration (rat K p,uu = 0.38). | ||
| M1717 | GSK1904529A | IGF-1R |
| GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity. | ||
| M1719 | GSK461364 | PLK |
| GSK461364A | ||
| GSK461364 is a potent and selective small molecule inhibitor of Polo-like kinase 1 (PLK1) with a Ki of 2.2 nM. | ||
| M1759 | GSK1120212 (Trametinib) | MEK |
| JTP-74057, GSK212 | ||
| Trametinib (GSK1120212; Jtp-74057) is an orally effective MEK inhibitor with IC50 of 2 nM against MEK1 and MEK2, respectively. Trametinib can activate autophagy and induce apoptosis. | ||
| 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. | ||
| M2730 | GSK-J1 | Histone demethylase |
| GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B. GSK J1 is selective for the H3K27 demethylases JMJD3 and UTX. | ||
| M2734 | GSK2606414 | PERK |
| GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. | ||
| M2826 | LY2090314 | GSK-3 |
| LY2090314 is a potent GSK-3 inhibitor for GSK-3α/β with IC50 of 1.5 nM/0.9 nM; may improve the efficacy of platinum-based chemotherapy regimens. Phase 1/2. | ||
| M3484 | Dolutegravir | Integrase |
| GSK1349572 | ||
| Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. | ||
| M3555 | GSK1070916 | Aurora Kinase |
| GSK-1070916A | ||
| GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. | ||
| M4831 | GSK2578215A | LRRK2 |
| GSK2578215A is a potent and selective LRRK2 kinase inhibitor with IC50 of 8.9 nM and 10.9 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively. | ||
| M4909 | GSK2801 | Epigenetic Reader Domain |
| GSK2801 is a selective bromodomains BAZ2A/B inhibitor with KD of 257 nM and 136 nM, respectively. | ||
| M5136 | GSK-LSD1 dihydrochloride | Histone demethylase |
| GSK-LSD1 2HCl | ||
| GSK-LSD1 2HCl is an irreversible, and selective LSD1 inhibitor with IC50 of 16 nM, > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B). | ||
| M5168 | GSK269962A | ROCK |
| GSK 269962 | ||
| GSK269962A is a potent ROCK inhibitor with IC50 values of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2, respectively. | ||
| M5209 | GSK481 | RIPK |
| GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM. | ||
| M5210 | GSK1325756 | CXCR |
| Danirixin | ||
| GSK1325756 (Danirixin) is a non-peptide, high affinity, selective and reversible CXCR2 antagonist, with IC50 of 12.5 nM for CXCL8. | ||
| M5212 | GSK2879552 | Histone demethylase |
| GSK2879552 is an effective, selective, bioactive and irreversible LSD1 inhibitor with Kiapp=1.7 μM. | ||
| M5239 | Batefenterol | Adrenergic Receptor |
| GSK961081; TD-5959 | ||
| Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. | ||
| M5269 | GSK180736A | ROCK |
| GSK180736 | ||
| GSK180736A, developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5. | ||
| M5271 | GSK6853 | Epigenetic Reader Domain |
| GSK6853 is a selective benzimidazolone BRPF1 inhibitor with pIC50 of 8.1(TR-FRET) showing greater than 1600-fold selectivity over all other bromodomains tested. | ||
| M5308 | Afuresertib | Akt |
| GSK2110183; LAE002 | ||
| Afuresertib (GSK2110183; LAE002) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. | ||
| M5325 | GSK 650394 | SGK |
| GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively. | ||
| M6044 | Uprosertib (GSK2141795) | Akt |
| GSK795; Uprosertib | ||
| Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180 nM for Akt1, 328 nM for Akt2, and 38 nM for Akt3 respectively (Clinical phase 1). | ||
| M6161 | GSK369796 Dihydrochloride | Potassium Channel |
| GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain. | ||
| M6770 | GSK 2830371 | Phosphatase |
| GSK 2830371 is a potent and selective allosteric inhibitor of Wip1 phosphatase. | ||
| M6772 | GSK 319347A | IκB/IKK |
| GSK319347A | ||
| GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. | ||
| M7305 | SKPin C1 | Others |
| SKPin-C1 | ||
| SKPin C1 is a inhibitor of Skp2-mediated p27 degradation. SKPin C1 induces p27 accumulation in metastatic melanoma cell lines. SKPin C1 promotes G1/S cell cycle arrest in T47D cells and LNCaP cells. SKPin C1 induces G2/M cell cycle arrest in MCF-7 cells. | ||
| M7545 | SKF-86002 | p38 MAPK |
| SKF-86002 is a potent inhibitor of p38 MAP kinase wit IC50 of 0.5-1 uM; inhibits LPS-induced IL-1 and TNF-α production in human monocytes. | ||
| M8631 | K6PC-5 | Others |
| K6PC-5 is a potent and selective sphingosine kinase 1 (SphK1 or SK1) activator that increases keratin 1 and involucrin expression in normal human epidermal keratinocytes cultured in vitro. | ||
| M8651 | GSK864 | Isocitrate Dehydrogenase (IDH) |
| GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. | ||
| M8758 | GW806742X | Necroptosis |
| GW806742X is an ATP site-targeing kinase inhibitor (IC50 in nM = 2/VEGFR2, 15/SRC, 47/C-FMS, 851/GSK3, 9016/ERBB2, 9120/FGFR) with potent antiproliferation activity against cancer cultures (IC50 in nM = 5/HUVEC-v, 424/HUVEC-b, 81/HEF, 453/MDA468, 470/A375P, 693/HT29, 734/PC3), GW806742X is now better known as Compound 1 for its anti-necroptosis activity via affinity interaction with ML | ||
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