C646

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Chemical Structure| 328968-36-1 同义名 : -
CAS号 : 328968-36-1
货号 : A122218
分子式 : C24H19N3O6
纯度 : 99%+
分子量 : 445.42
MDL号 : MFCD01784780
存储条件：

Pure form Sealed in dry, 2-8°C

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

DMSO: 12 mg/mL(26.94 mM)，配合低频超声，并水浴加热至45℃助溶，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
生物活性
靶点

  • p300/CBP

    p300/CBP, Ki:400 nM
描述 The histone acetyltransferase p300/CBP is a transcriptional coactivator involved in many regulatory pathways during tumorigenesis. C646 is a selective and competitive p300 inhibitor with a Ki value of 400nM. Treatment of C3H 10T1/2 mouse fibroblasts with C646 (25μM) resulted in a reduction in the levels of histone H3 and H4 acetylation. C646 at a concentration of 25μM also inhibited TSA-induced acetylation in mouse fibroblasts. C646 at 10μM was capable of reducing 3H-thymidine incorporation in several human cancer cell lines. The IC50 value of C646 for the growth of melanoma cell line WM983A was 10-20μM[3] The suppression of P300 by C646 via intraperitoneal injection (30nmol/g/day for two weeks) reduced the level of blood glucose, rescued impaired autophagic flux, and resulted in an 18.5% increase in muscle mass in db/db mice.[4]
作用机制 C646 is a competitive, highly selective inhibitor of p300 versus other acetyltransferases.[3]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.23mL

2.25mL

1.12mL

22.45mL

4.49mL

2.25mL
参考文献

[1]Bowers EM, Yan G, Mukherjee C, Orry A, Wang L, Holbert MA, Crump NT, Hazzalin CA, Liszczak G, Yuan H, Larocca C, Saldanha SA, Abagyan R, Sun Y, Meyers DJ, Marmorstein R, Mahadevan LC, Alani RM, Cole PA. Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor. Chem Biol. 2010 May 28;17(5):471-82

[2]Fan Z, Wu J, Chen QN, Lyu AK, Chen JL, Sun Y, Lyu Q, Zhao YX, Guo A, Liao ZY, Yang YF, Zhu SY, Jiang XS, Chen B, Xiao Q. Type 2 diabetes-induced overactivation of P300 contributes to skeletal muscle atrophy by inhibiting autophagic flux. Life Sci. 2020 Oct 1;258:118243