staurosporine

Staurosporine (AM-2282) 是一种蛋白激酶抑制剂，对 PKC、PKA、c-Fgr、Phosphorylase kinase 和 TAOK2 均有抑制活性 (IC50=6 15 2 3 3000 nM)，具有 ATP 竞争性和非选择性。Staurosporine 也可以诱导凋亡。

7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.

5'-Hydroxy-staurosporine is an AMPK inhibitor with selective toxicity toward human colon tumor cells.

Staurosporine-Boc 是从放线菌（Streptomyces staurosporeus）中提取的一种天然产物，具有强效的非选择性蛋白激酶抑制特性。Staurosporine-Boc 能抑制多种蛋白激酶，包括蛋白激酶C (PKC)、酪氨酸激酶 (tyrosine kinase) 和丝氨酸 苏氨酸激酶。由于其广泛的抑制能力，该化合物在生物学研究中尤其是在细胞信号传导途径的研究中被广泛应用作为工具化合物。

Midostaurin (PKC412) 是一种多靶点蛋白激酶抑制剂，有抗肿瘤活性，对 PKCα β γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ和VEGFR1 2的IC50值范围为 22 到500 nM 之间。

Picroside I (6'-Cinnamoylcatalpol) 是胡黄连的一种天然产物，是有肝脏保护作用的代谢成分，可用于哮喘研究，有减轻炎症作用，还下调 pSTAT6 和 GATA3 表达。

NSC117079是一种新型的的PHLPP1 2（Pleckstrin homology domain and leucine rich repeat protein phosphatase）抑制剂，在神经元中能够激活神经元AKT并改善staurosporine诱导的细胞死亡。

K-252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi. K-252a inhibits protein kinase (IC50: 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+ calmodulin-dependent kinase type II, and phosphorylase kinase, respectively).

K-252c is a staurosporine analog isolated from Nocardiopsis sp. and is a cell-permeable PKC inhibitor (IC50: 2.45 μM). K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase. K-252c causes apoptosis in human chronic myelogenous leukemia cancer cells.

AFN941 is a staurosporine analog, acting as a Jak3-specific inhibitor.

Nardosinone 是一个 dbcAMP 和 staurosporine 的神经生成作用增强剂，分离自Nardostachys chinensis 中。Nardosinone 可能成为一种有用的药理学工具，不仅可用于研究神经生长因子 (NGF) 的作用机理，而且可用于研究神经毒性物质的作用机理。

NA 382 is a staurosporine derivative that inhibits multidrug resistance.

Co-treatment with Tanshinone IIB (TSB) significantly inhibits the DNA laddering, cytotoxicity and apoptosis of rat cortical neurons induced by staurosporine in a concentration-dependent manner; TSB also suppresses the elevated Bax protein and decreased bc

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) 作为一种有效的蛋白激酶抑制剂，展现了对PKC-α、ROCK、ASK1的强效抑制作用，其IC50分别为0.092, 0.26, 0.77 μM。此外，该化合物对PC-3癌细胞线具有显著的细胞毒性，其IC50为0.16 μM。

IP3RCYT 是一种 IP3R 的抑制肽，能够抑制细胞色素 C 与 IP3R 结合，IC50 约为 100 nM。IP3RCYT 可调节细胞内钙信号。在星形孢菌素或膜结合 Fas 配体 (FasL) 处理的 HeLa 和 Jurkat 细胞中，IP3RCYT 可抑制细胞凋亡 (apoptosis)。