active protein kinase

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.

EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.

LP-922761 is a potent, selective, and orally active AAK1 inhibitor with inhibitory effects on BMP-2 induced protein kinase (BIKE).

UR-13870 (Org 48762-0) is an orally active and selective inhibitor of p38 mitogen-activated protein kinase (MAPK), which prevents bone damage in collagen-induced arthritis in mice.

Emprumapimod (PF-07265803) is an orally active and specific inhibitor of mitogen-activated protein kinase p38α MAPK, inhibits LPS-induced production of IL-6, and can be used to study dilated cardiomyopathy induced by the LMNA gene.

TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK). It exhibits a strong selectivity for TNIK with an IC50 value of 0.026 μM. Additionally, TNIK-IN-3 demonstrates inhibitory activity against Flt4 (IC50 = 0.030 μM), Flt1 (IC50 = 0.191 μM), and DRAK1 (IC50 = 0.411 μM). This compound holds potential for carrying out research on colorectal cancer (CRC) [1].

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. Isolated from hyssop oil, it possesses antifungal, highly active whitening, and antioxidant properties, and it has potential applications in cosmeceutical materials. It downregulates proinflammatory cytokines in vitro and in vivo, reduces the number of total cells, neutrophils, and macrophages in BALF, attenuates histologic lung alterations, decreases the wet-to-dry weight ratio in BALF, and inhibits the activation of NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, and p38 mitogen-activated protein kinase.

Bufalin is an active ingredient and one of the glycosides in the traditional Chinese medicine ChanSu; it is also a bufadienolide toxin originally isolated from the venom of the Chinese toad Bufo gargarizans, with potential cardiotonic and antineoplastic a

GSK2606414 is a cell-permeable and orally active protein kinase R-like endoplasmic reticulum kinase(PERK)inhibitor with IC50 of 0.4 nM. GSK2606414 inhibits PERK activation in cells and suppresses the growth of human tumor xenografts in mice.

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

BAY-1816032 is a benzimidazole budding inhibition relieved homolog protein 1 kinase (BUB1) inhibitor with IC50 of 0.7 nM and is orally active and abolishes nocodazole-induced Thr-120 phosphorylation of histone H2A, a major BUB1 target protein, in HeLa cells with IC50 of 29 nM.

Takeda-6d, a novel, potent DFG-out RAF vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor, inhibits B-RAF and VEGFR2 with IC50 of 7.0nM and 2.2nM.

Pim-1 2 Kinase Inhibitor 1, an orally active inhibitor, impedes the action of Pim kinases by preventing their ability to phosphorylate peptides. It particularly inhibits the phosphorylation of 4E-BP1 and p27 Kip1 by Pim protein kinases. This compound is valuable in cancer research, with a notable application in studying prostate cancer [1].

BAY-8400 is a potent, selective, and orally active DNA-dependent protein kinase (DNA-PK) inhibitor (IC50 = 81 nM) that demonstrates synergistic efficacy when combined with targeted alpha therapies. BAY-8400 is applicable for cancer research [1].

ZIP acetate is a novel, cell-permeable inhibitor of protein kinase Mζ (PKMζ), a constitutively active, atypical PKC isozyme involved in LTP maintenance. Selectively blocks PKMζ-induced synaptic potentiation in hippocampal slices in vitro. Reverses late-ph

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Purine riboside-5'-O-triphosphate sodium is an active metabolite of Nebularine (HY-103694) and acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC50 values of 35 µM and 28 µM, respectively. It also inhibits calmodulin-dependent protein kinase II (CaMKII), with a Ki value of 590 µM.

Prostratin (12-Deoxyphorbol-13-acetate) is an orally active protein kinase C (PKC) activator with a Ki value of 12.5 nM.As an NF-κB activator, Prostratin activates HIV gene expression in T cells.Prostratin inhibits the growth of acute myeloid leukemia (AML) cell lines and enhances cytarabine-induced AML cell differentiation. In addition, Prostratin induced KRAS phosphorylation and inhibited the growth of KRAS-mutated tumors.

ONO-8130 is an orally available antagonist of EP1 receptor.

Plixorafenib (PLX8394) is an orally active inhibitor of the serine threonine protein kinase B-Raf (BRAF) protein.Plixorafenib can selectively bind to and inhibit the activity of wild-type and mutant forms of BRAF, inhibiting the proliferation of tumor cells expressing mutant forms of BRAF.