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首页-小分子抑制剂&激动剂-Apoptosis-Receptor Interacting Protein Kinase (RIPK)-PK68
PK68

Chemical Structure : PK68

CAS No.: 2173556-69-7

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PK68 (RIPK1 inhibitor PK68)

货号: PC-73017Not For Human Use, Lab Use Only.

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).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 424.519
分子式 C22H24N4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate

参考文献

1. Hou J, et al. Cell Death Dis. 2019 Jun 24;10(7):493.

2. Li Z, et al. Eur J Med Chem. 2022 Jan 15;228:114036.

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