Domatinostat (4SC-202)

Chemical Structure : Domatinostat

CAS No.: 910462-43-0

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货号: PC-73192Not For Human Use, Lab Use Only.

Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20/1.12/0.57 uM for HDAC1/2/3, repectively.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥2980	In stock
100 mg		Get quote

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生物&药学活性

Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20/1.12/0.57 uM for HDAC1/2/3, repectively.
Domatinostat (4SC-202) weakly inhibits Class III (HDAC11, IC50=9.7 uM), does not inhibit HDAC4/6/7/8/9 (IC50>50 uM).
Domatinostat (4SC-202) potently inhibited survival and proliferation of primary human colon cancer cells and established CRC lines (HT-29, HCT-116, HT-15, and DLD-1).
4SC-202 provoked apoptosis activation, induced dramatic G2-M arrest in CRC cells. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to potently inhibit human HCC cells.
4SC-202 induces hyperacetylation of histone H3 in a dose dependent manner with a cellular potency EC50 of 1.1 uM.
4SC-202 shows a broad anti-proliferative/cytotoxic activity towards human cancer cell lines from various indications with mean IC50 of 0.7 uM.
4SC-202 showed pronounced and robust anti-tumor activity in various cancer cell lines and xenograft animal models.

物理化学性质&存储条件

分子量	447.51
分子式	C23H21N5O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	100 mM in DMSO
Chemical Name/SMILES	(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide

参考文献

1. Fu M, et al. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73.

2. Zhijun H, et al. Tumour Biol. 2016 Aug;37(8):10257-67.

3. Pinkerneil M, et al. Target Oncol. 2016 Dec;11(6):783-798.

4. von Tresckow B, et al. Eur J Haematol. 2019 Feb;102(2):163-173.