CW-069

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Chemical Structure| 1594094-64-0 同义名 : -
CAS号 : 1594094-64-0
货号 : A719211
分子式 : C23H21IN2O3
纯度 : 99%+
分子量 : 500.329
MDL号 : MFCD28009372
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(99.93 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 HSET, encoded by KIFC1 in humans and Kifc5a in mice, is a minus-end microtubule motor protein which plays a critical role in the assembly of a functional mitotic spindle. CW069 is an allosteric inhibitor of HSET with IC50 value of 75 μM. CW069 treatment led to a significant increase in multipolar spindle formation in N1E-115 cells (control 30%, 100 mM 98%, 200 mM 86%), but not in normal human dermal fibroblast (NHDF) cells[2]. CW069 treatment dose-dependently suppressed cell viability in both the parental and docetaxel(DTX)-resistant prostate cancer cell lines DU145 and C4-2 cells. The combination of DTX and CW069(100μM) significantly reduced cell viability in the DTX-resistant cell lines while DTX alone had little effect, which demonstrated that CW069 re-sensitized DTX-resistant cell lines to DTX treatment[3].
作用机制 CW069 plays the role of HSET inhibitor by interacting with HSET loop 5 cleft.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.00mL

0.40mL

0.20mL

9.99mL

2.00mL

1.00mL

19.99mL

4.00mL

2.00mL
参考文献

[1]Watts CA, Richards FM, et al. Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes. Chem Biol. 2013 Nov 21;20(11):1399-410.

[2]Watts CA, Richards FM, Bender A, Bond PJ, Korb O, Kern O, Riddick M, Owen P, Myers RM, Raff J, Gergely F, Jodrell DI, Ley SV. Design, synthesis, and biological evaluation of an allosteric inhibitor of HSET that targets cancer cells with supernumerary centrosomes. Chem Biol. 2013 Nov 21;20(11):1399-410. doi: 10.1016/j.chembiol.2013.09.012. Epub 2013 Oct 24. PMID: 24210220; PMCID: PMC3898838.

[3]Sekino Y, Oue N, Koike Y, Shigematsu Y, Sakamoto N, Sentani K, Teishima J, Shiota M, Matsubara A, Yasui W. KIFC1 Inhibitor CW069 Induces Apoptosis and Reverses Resistance to Docetaxel in Prostate Cancer. J Clin Med. 2019 Feb 9;8(2):225. doi: 10.3390/jcm8020225. PMID: 30744126; PMCID: PMC6407017.