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SGC-CBP30

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Chemical Structure| 1613695-14-9 同义名 : -
CAS号 : 1613695-14-9
货号 : A636668
分子式 : C28H33ClN4O3
纯度 : 99%+
分子量 : 509.04
MDL号 : MFCD26792586
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 65 mg/mL(127.69 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
动物实验配方：

2% DMSO+30% PEG 300+5% Tween 80+water 5 mg/mL

生物活性
靶点

  • p300/CBP

    EP300, IC50:38 nM

    CREBBP, IC50:21 nM
描述 CREBBP/EP300, two highly homologous transcriptional co-activators, are characterized by several zinc finger domains, a bromodomain, a plant homology domain, a HAT domain and a CREB binding domain. They bind to multiple partner proteins, mainly transcription factors and other co-activators and play essential roles in histone acetylation, mainly at histone H3 positions K18 and K27. SGC-CBP30, also called as CBP30, is a potent CREBBP/EP300 inhibitor with IC50 values of 69nM and 38nM for CREBBP (measured by Alphascreen assay) and EP300 (measured by ITC assay), respectively[1]. Treatment with 2μM SGC-CBP30 for 24h in Th17 cells can inhibit the binding of p300 and ac-H3K56, a known CBP/p300 mark, to the IL17A gene locus in CHIP experiment. SGC-CBP30 showed a broad anti-inflammatory activity in a panel of 12 stimulated primary human cell types treated with SGC-CBP30 (<10uM), shown as the down-regulation of the cytokines IL-17, TNFα, IL-8, IL-2, IL-6, IL-1α, and IL-10, VCAM-1 and MCP1. 2μM CBP30 inhibited IL-17A production by AS CD4 T cells by 77%, and an average reduced the secretion of IL-17A by 66.3% in cells from patients with AS and PSA and from HCs[2].
作用机制 SGC-CBP30 preferentially binds to the CBP/p300 Bromodomain and inhibited binding of p300 and of acetylated histone H3K56.[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.82mL

1.96mL

0.98mL

19.64mL

3.93mL

1.96mL
参考文献

[1]Hammitzsch A, Tallant C, et al. CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses. Proc Natl Acad Sci U S A. 2015 Aug 25;112(34):10768-73.