pkc 9

PKC-9 is a PKC-zeta inhibitor 9.

Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2.7 µM, respectively). It reduces tumor growth in an HCCLM3 mouse xenograft model when administered at doses of 5 or 10 mg kg once per week. Formulations containing oxaliplatin have been used in the treatment of advanced colorectal cancer and as adjuvants in stage III colon cancer.

ML-9 suppresses MLCK, PKA, and PKC activity with Ki values of 4, 32, and 54 μM, respectively. ML-9 is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) activity. ML-9 causes autophagy by stimulating autophagosome formation and inhibiting their degradation.

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

CYC116 is a potent inhibitor of Aurora A B with Ki of 8.0 nM 9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt PKB, PKC, no effect on GSK-3α β, CK2, Plk1 and SAPK2A. Phase 1.

ML-9 (free base) suppresses MLCK, PKA, and PKC activity (Ki: 4, 32, and 54 μM, respectively). ML-9 (free base) is a selective and effective inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK), and stromal interaction molecule 1 (STIM1) acti

Bisindolylmaleimide XI hydrochloride is an orally active PKC inhibitor with inhibitory effects on PKCα, PKCβI, PKCβII, and PKCγ (IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM, respectively).

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.