About 16 results found for searched term "ERK5-IN-2" (0.14 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M9688 | ERK5-IN-2 | ERK |
| ERK5-IN-2 is a selective, orally active, sub-micromolar ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. | ||
| 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. | ||
| M3668 | GDC-0994 | ERK |
| Ravoxertinib | ||
| Ravoxertinib (GDC-0994) is an orally active ERK kinase inhibitor with IC50 of 6.1 nM and 3.1 nM against ERK1 and ERK2, respectively. | ||
| M4819 | XMD17-109 | ERK |
| ERK5-IN-1 | ||
| XMD17-109 (ERK5-IN-1) is a novel, specific inhibitor of ERK-5 with an EC50 value of 4.2 μM in HEK293 cells. | ||
| M25612 | Elironrasib | Ras |
| RMC-6291 | ||
| Elironrasib is an orally active and covalent inhibitor of KRASG12C(ON). Elironrasib prevents KRASG12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRASG12C mutant cells with a median IC50 of 0.11 nM. | ||
| M9510 | JWG-071 | ERK |
| JWG-071 is the first reported kinase-selective chemical probe for ERK5, inhibits ERK5 and LRRK2 with IC50 of 88 and 109 nM, respectively. | ||
| M11529 | Temuterkib | ERK |
| LY3214996 | ||
| Temuterkib (LY3214996) is a selective, novel erK1/2 inhibitor with an IC50 of 5 nM against ERK1 and ERK2. It can effectively inhibit intracellular P-RSK1 in cancer cell lines with BRAF and RAS mutations. Temuterkib has strong antitumor activity in cancer models with altered MAPK pathways. | ||
| M14152 | ERK1/2 inhibitor 1 | ERK |
| ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively. | ||
| M14155 | Ulixertinib hydrochloride | ERK |
| BVD-523 hydrochloride; VRT752271 hydrochloride | ||
| Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. | ||
| M20811 | XMD8-85 (ERK5-IN-1) | ERK |
| XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively. | ||
| M21071 | MAP855 | MEK |
| MAP855 is a potent, selective and orally effective ATP-competitive MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 inhibits wild-type and mutant MEK1/2 equally. | ||
| M30754 | PT-262 | ROCK |
| PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity. | ||
| M42116 | ERK-IN-7 | ERK |
| ERK-IN-7, an analogue of SHR2415, is a potent ERK inhibitor with IC50 of 5 nM and 7 nM against ERK1 and ERK2, respectively. | ||
| M45287 | CK2/ERK8-IN-1 | Casein Kinase |
| CK2/ERK8-IN-1 is a dual inhibitor of casein kinase 2 (CK2) (Ki 0.25 µM) and ERK8 (MAPK15, ERK7), both with IC50s of 0.50 µM. In addition, CK2/ERK8-IN-1 binds to PIM1, HIPK2, and DYRK1A with Ki values of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. 15.25 µM and 11.9 µM, respectively, and also has pro-apoptotic activity. | ||
| M49702 | ERK1/2 inhibitor 4 | ERK |
| ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. | ||
| M49703 | ERK1/2 inhibitor 5 | ERK |
| ERK1/2 inhibitor 5 is a potent inhibitor of ERK1/2. | ||
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