BDP9066是肌强直性肌营养不良相关Cdc-42结合激酶MRCK的选择性有效抑制剂,其在SCC12细胞中测得对MRCKβ的IC50值为64nM,对MRCKα/β的Ki值分别为0.0136nM和0.0233nM。BDP9066通过降低底物磷酸化来治疗皮肤癌。
货号:ajcx13002
CAS:2226507-04-4
分子式:C20H24N6
分子量:348.44
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:
现货
Background:
BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinases MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells, Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.
BDP9066 shows antiproliferative effects with greatest activity in hematologic cancer cells. BDP9066 inhibits MLC phosphorylation and blocks SCC12 squamous cell carcinoma motility and invasion[1].
BDP9066 topical application significantly decreases phosphorylated MRCKα S1003 staining and tumor volumes[1].
[1]. Unbekandt M, et al. Discovery of Potent and Selective MRCK Inhibitors with Therapeutic Effect on Skin Cancer. Cancer Res. 2018 Apr 15;78(8):2096-2114.