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编 号:F477855
分子式:C14H15ClN2O
分子量:262.73
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生物活性:
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). CHIC35 has anti-inflammatory?effects and can be used for CHARGE syndrome research.

体外研究:
CHIC-35 (0.5?μM; 16 hours) increases?acetylation?of?histone H4?in BMDMs similar to Cambinol (200?μM).CHIC-35 (5?μM; 72 hours) exhibits no significant difference in the survival of embryos at early stages. 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.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.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.
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