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Chemical Structure : Domatinostat
CAS No.: 910462-43-0
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $118 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $298 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 447.51 | |
| Formula | C23H21N5O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(E)-N-(2-aminophenyl)-3-(1-((4-(1-methyl-1H-pyrazol-4-yl)phenyl)sulfonyl)-1H-pyrrol-3-yl)acrylamide |
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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.
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