CID 2011756

An inhibitor of protein kinase D

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库存: 现货

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5mg

￥437.00

350.00

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10mg

￥762.00

610.00

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50mg

￥3262.00

2610.00

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货号: ajci15678
CAS: 638156-11-3
别名:
分子式: C22H21ClN2O3
分子量: 396.87
纯度: >98%
溶解度: ≥ 39.7mg/mL in DMSO with gentle warming, ≥ 2.34 mg/mL in EtOH with ultrasonic and warming
储存: Store at RT
库存: 现货

Background

CID-2011756 is a novel and potent inhibitor of protein kinase D1 (PKD1), one of three PKD isoforms of a novel family of serine/threonine kinases involved in cell proliferation, survival, invasion and protein transport, with a value of 50% inhibition concentration IC₅₀ of 3.2 μM in vitro. CID-2011756 also exhibits pan-PKD inhibitory effects that ATP-competitively inhibits PKD2 and PDK3 with values of IC₅₀ of 0.6 μM and 0.7 μM respectively. Study results have shown that CID-2011756 is a cell active PKD1 inhibitor that concentration-dependently inhibits phorbolester-induced endogenous PKD1 activation in LNCap prostate cancer cells with a value of half maximal effective concentration EC₅₀of 10 μM.

Reference

[1].Sharlow ER, Mustata Wilson G, Close D, Leimgruber S, Tandon M, Reed RB, Shun TY, Wang QJ, Wipf P, Lazo JS. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.