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CHIC35 Sale

目录号 : GC64255

CHIC35 是 EX-527 的结构类似物,是 SIRT1 (IC50=0.124 µM) 的有效选择性抑制剂。CHIC35 对 SIRT1 的选择性远大于对 SIRT2 (IC50=2.8 µM) 和 SIRT3 (IC50>100 µM)。CHIC35 具有抗炎作用,可用于 CHARGE 综合征的研究。

CHIC35 Chemical Structure

Cas No.:848193-72-6

规格 价格 库存 购买数量
5 mg
¥5,400.00
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10 mg
¥8,100.00
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25 mg
¥14,400.00
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产品描述

CHIC35, an analog of EX-527, is a potent and selective inhibitor of SIRT1 (IC50=0.124 µM). CHIC35 shows potential selective inhibition against SIRT1 over SIRT2 (IC50=2.8 µM) or SIRT3 (IC50>100 µM)[1]. CHIC35 has anti-inflammatory effects and can be used for CHARGE syndrome research[1][2].

CHIC-35 (0.5 μM; 16 hours) increases acetylation of histone H4 in BMDMs similar to Cambinol (200 μM)[1].CHIC-35 (5?μM; 72 hours) exhibits no significant difference in the survival of embryos at early stages[2]. Zebrafish embryos are microinjected with 2.4?ng of chd7 MO to develop to different stages of development. chd7 morphant embryos are treated with CHIC-35 from 8hpf to 24hpf. CHIC-35 (5?μM) is removed at 24hpf and embryos are incubated in fresh egg water until 4dpf. The chd7 morphant larvae has a severely reduced and disrupted pattern of cartilage elements in comparison to the control, CHIC-35 shows partial recovery in craniofacial cartilage elements[2].At 4dpf, zebrafish embryos show a well-formed lower jaw in controls, while chd7 morphants exhibits reduced lower jaw. Treatment with CHIC-35 (5?μM) rescues the expression of sox9a inchd7 morphants[2].Nearly 30% of chd7 morphant embryos (24hpf to 72hpf) shows a near complete loss of isl2a expression in the cranial region compared to 10% of the wildtype controls. CHIC-35 reduces this to 7.5% significantly. However, CHIC-35 shows no discernible effect on the enteric neurons marked by Tg[2].

[1]. JÉrÔme Lugrin, et al. The sirtuin inhibitor cambinol impairs MAPK signaling, inhibits inflammatory and innate immune responses and protects from septic shock. Biochim Biophys Acta. 2013 Jun;1833(6):1498-510
[2]. Zainab Asad, et al. Chemical screens in a zebrafish model of CHARGE syndrome identifies small molecules that ameliorate disease-like phenotypes in embryo. Eur J Med Genet. 2020 Feb;63(2):103661.

Chemical Properties

Cas No. 848193-72-6 SDF Download SDF
分子式 C14H15ClN2O 分子量 262.73
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1 mM 3.8062 mL 19.0309 mL 38.0619 mL
5 mM 0.7612 mL 3.8062 mL 7.6124 mL
10 mM 0.3806 mL 1.9031 mL 3.8062 mL
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Research Update

Chemical and genetic rescue of an ep300 knockdown model for Rubinstein Taybi Syndrome in zebrafish

Biochim Biophys Acta Mol Basis Dis 2018 Apr;1864(4 Pt A):1203-1215.PMID:29409755DOI:10.1016/j.bbadis.2018.01.029.

EP300 is a member of the EP300/CBP family of lysine acetyltransferases (KATs) with multiple roles in development and physiology. Loss of EP300/CBP activity in humans causes a very rare congenital disorder called Rubinstein Taybi Syndrome (RSTS). The zebrafish genome has two co-orthologs of lysine acetyltransferase EP300 (KAT3B) in zebrafish viz. ep300a and ep300b. Chemical inhibition of Ep300 with C646, a competitive inhibitor and morpholino-based genetic knockdown of ep300a and ep300b cause defects in embryonic development reminiscent of the human RSTS syndrome. Remarkably, overexpression of Ep300a KAT domain results in near complete rescue of the jaw development defects, a characteristic feature of RSTS in human suggesting the dispensability of the protein-interaction and DNA-binding domains for at least some developmental roles of Ep300. We also perform a chemical screen and identify two inhibitors of deacetylases, CHIC35 and HDACi III, that can partially rescue the RSTS-like phenotypes. Thus, modeling rare human genetic disorders in zebrafish allows for functional understanding of the genes involved and can also yield small molecule candidates towards therapeutic goals.

Seeding for sirtuins: microseed matrix seeding to obtain crystals of human Sirt3 and Sirt2 suitable for soaking

Acta Crystallogr F Struct Biol Commun 2015 Dec;71(Pt 12):1498-510.PMID:26625292DOI:10.1107/S2053230X15019986.

Sirtuins constitute a family of NAD(+)-dependent enzymes that catalyse the cleavage of various acyl groups from the ℇ-amino group of lysines. They regulate a series of cellular processes and their misregulation has been implicated in various diseases, making sirtuins attractive drug targets. To date, only a few sirtuin modulators have been reported that are suitable for cellular research and their development has been hampered by a lack of structural information. In this work, microseed matrix seeding (MMS) was used to obtain crystals of human Sirt3 in its apo form and of human Sirt2 in complex with ADP ribose (ADPR). Crystal formation using MMS was predictable, less error-prone and yielded a higher number of crystals per drop than using conventional crystallization screening methods. The crystals were used to solve the crystal structures of apo Sirt3 and of Sirt2 in complex with ADPR at an improved resolution, as well as the crystal structures of Sirt2 in complex with ADPR and the indoles EX527 and CHIC35. These Sirt2-ADPR-indole complexes unexpectedly contain two indole molecules and provide novel insights into selective Sirt2 inhibition. The MMS approach for Sirt2 and Sirt3 may be used as the basis for structure-based optimization of Sirt2/3 inhibitors in the future.