Cas No.: | 2173556-69-7 |
Chemical Name: | Cyclohexyl N-[5-(2-acetamido-1,3-benzothiazol-6-yl)-2-methylpyridin-3-yl]carbamate |
Synonyms: | PK68;BCP32187;Cyclohexyl N-[5-(2-acetamido-1,3-benzothiazol-6-yl)-2-methylpyridin-3-yl]carbamate |
SMILES: | S1C(N([H])C(C([H])([H])[H])=O)=NC2C([H])=C([H])C(=C([H])C1=2)C1C([H])=NC(C([H])([H])[H])=C(C=1[H])N([H])C(=O)OC1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] |
Formula: | C22H24N4O3S |
M.Wt: | 424.5160 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PK68 (RIPK1 inhibitor PK68) is a potent necroptosis inhibitor seletively targeting RIPK1 kinase activity, potently inhibits TNF-induced necroptosis (EC50, 23 and 13 nM in human and mouse cells, respectively).PK68 blocks cellular activation of RIPK1, RIPK3, and MLKL upon necroptotic stimuli.PK68 is a type II inhibitor of RIP1 kinase, highly selective inhibitor of RIPK1 kinase activity with IC50 of 90 nM, does not affect RIPK3 kinase activity at 1 uM, also demonstrated a reasonable selectivity against a panel of 369 kinases.PK68 exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.PK68 ameliorates TNF-induced systemic inflammatory response syndrome, and displays preventive suppression of tumor metastasis in the mouse cancer models. |
Target: | IC50: ~ 90 nM (RIPK1)[1] |
References: | [1]. Hou J, et al. Discovery of potent necroptosis inhibitors targeting RIPK1 kinase activity for the treatment of inflammatory disorder and cancer metastasis. Cell Death Dis. 2019 Jun 24;10(7):493. |