About 8 results found for searched term "81-14-1" (0.118 seconds)
Cat.No. | Name | Target |
---|---|---|
M28909 | GGTI-286 hydrochloride | Ras |
GGTI-286 hydrochloride, a potent GGTase I inhibitor, is 25-fold more potent (IC50=2 μM) than the corresponding methyl ester of FTI-276. GGTI-286 hydrochloride selectively inhibits geranylgeranylation of Rap1A over farnesylation of H-Ras in NIH3T3 cells (IC50s =2 and >30 μM, respectively). GGTI-286 hydrochloride also potently inhibits oncogenic K-Ras4B stimulation with an IC50 of 1 μM. | ||
M58199 | Musk ketone | Cytochrome P450 (e.g. CYP17) |
Musk ketone is a widely used artificial fragrance. Musk ketone is also a cytochrome P450 enzyme inducer. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the PI3K/Akt signaling pathway. | ||
M9900 | Selpercatinib (LOXO-292) | RET |
LOXO-292; ARRY-192 | ||
Selpercatinib (LOXO-292) is a first-in-class, highly selective and potent small molecule RET inhibitor with good blood-brain barrier (BBB) penetration. and RET (G810R) with IC50 values of 14.0 nM, 24.1 nM and 530.7 nM, respectively. | ||
M27822 | JNJ-40411813 | GluR |
ADX-71149 | ||
JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM. | ||
M28154 | LY2812223 | GluR |
LY2812223 is a highly potent, functionally selective mGlu2 receptor agonist with mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively). | ||
M29048 | CD12681 | ROR |
CD12681 (compound 14) is a potent and selective RORγ inverse agonist with IC50 of 19 nM and 10 nM for RORγ GAL4 and CD4-IL-17 cells, respectively. CD12681 decreases the IL-17 inflammatory cell recruitment. CD12681 has the potential for the research of psoriasis. | ||
M29089 | GSK8814 | Epigenetic Reader Domain |
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1. | ||
M30111 | ABT-100 | Farnesyl Transferase |
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity. |
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