|(S)-2-(2-(苄基氨基)-3-苯基丙酰胺基)-5-碘苯甲酸|CsnPharm

CAS No.: 1594094-64-0

CW-069 Catalog No. CSN16978

Synonyms: CW069

CW069 is a selective and allosteric microtubule motor protein HSET inhibitor with IC50 value of 75 μM.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

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.
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9987 mL
- 9.9934 mL
- 19.9869 mL
- 5 mM
- 0.3997 mL
- 1.9987 mL
- 3.9974 mL
- 10 mM
- 0.1999 mL
- 0.9993 mL
- 1.9987 mL

技术信息

CAS号

1594094-64-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H21IN2O3

运输

蓝冰

分子量

500.33

别名

CW069

溶解度

DMSO	195.0 mg/mL (389.7 mM)
Water	insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

CW-069 Catalog No. CSN16978

靶点选择性

请登录您的专属账户

确认信息