|(3S,6S,9S,12S,15S)-甲基 3-苄基-1-(4-(叔丁基)苯基)-12-(4-(二乙基氨基)丁基)-15-(羟甲基)-9-异丁基-6-甲基-1,4,7,10,13-五氧代-2,5,8,11,14-五氮杂十六烷-16-油酸|CsnPharm

CAS No.: 1872382-47-2

UNC3866 Catalog No. CSN18843

Synonyms: UNC3866

UNC3866 is a high-affinity CBX4 and CBX7 inhibitor with Ki values of 94 and 97 nM, respectively.

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技术信息

生物活性

描述UNC3866 is an antagonist of the methyl-lysine (Kme) reading function of the Polycomb CBX and CDY families of chromodomains. It is a potent ligand for CBX4 and CBX7 with K_d values of 94 ± 17nM and 97 ± 2.4nM, respectively. UNC3866 is 65-fold selective for CBX4/7 over CDY1 (K_d = 6.3 ± 0.92µM) and 9-fold selective for CBX4/7 over CDYL1b (K_d = 0.91 ± 0.076µM) and CDYL2 (K_d = 0.85 ± 0.076µM). UNC3866 is also a potent antagonist of the CBX7-H3 interaction with an IC50 value of 66 ± 1.2nM. Treatment of PC3 cells with 30μM UNC3866 for 24 hours resulted in an intracellular concentration of 1.4 ± 0.3μM. UNC3866 treatment recued PC3 cell count with an EC50 values of 7.6 ± 2.5μM. UNC3866-treated PC cells also showed an enlarged and flattened morphology. UNC3866 (10mg/kg, intraperitoneal injection) showed 25% bioavailability and moderate clearance in male swiss albino mice^[2].
作用机制UNC3866 binds the chromodomains of CBX4 and CBX7. It participates in at least one hydrogen bond with the backbone of CBX7 and its N-terminal tert-butyl benzoyl cap primarily contacts the side chains of D50, R52, and L53^[2].
参考文献

[1] Stuckey JI, Dickson BM, et al. A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1. Nat Chem Biol. 2016 Mar;12(3):180-7.
[2] Stuckey JI, Dickson BM, Cheng N, Liu Y, Norris JL, Cholensky SH, Tempel W, Qin S, Huber KG, Sagum C, Black K, Li F, Huang XP, Roth BL, Baughman BM, Senisterra G, Pattenden SG, Vedadi M, Brown PJ, Bedford MT, Min J, Arrowsmith CH, James LI, Frye SV. A cellular chemical probe targeting the chromodomains of Polycomb repressive complex 1. Nat Chem Biol. 2016 Mar;12(3):180-7

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
- 1.2578 mL
- 6.2892 mL
- 12.5783 mL
- 5 mM
- 0.2516 mL
- 1.2578 mL
- 2.5157 mL
- 10 mM
- 0.1258 mL
- 0.6289 mL
- 1.2578 mL

技术信息

CAS号

1872382-47-2

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C43H66N6O8

运输

蓝冰

分子量

795.02

别名

UNC3866

溶解度

DMSO	410.0 mg/mL (515.7 mM)
Water	300.0 mg/mL (377.3 mM)

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