An HDAC1-3 and KDM1A inhibitor
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4SC-202

Item No. 26175

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-(2-aminophenyl)-3-[1-[[4-(1-methyl-1H-pyrazol-4-yl)phenyl]sulfonyl]-1H-pyrrol-3-yl]-2-propenamide, 4-methylbenzenesulfonate
CAS Number
1186222-89-8
Synonyms
  • Domatinostat
Molecular Formula
C23H21N5O3S • C7H8O3S
Formula Weight
619.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O=S(C1=CC=C(C2=CN(C)N=C2)C=C1)(N3C=C(/C=C/C(NC4=C(N)C=CC=C4)=O)C=C3)=O.CC5=CC=C(S(O)(=O)=O)C=C5
InChi Code
InChI=1S/C23H21N5O3S.C7H8O3S/c1-27-16-19(14-25-27)18-7-9-20(10-8-18)32(30,31)28-13-12-17(15-28)6-11-23(29)26-22-5-3-2-4-21(22)24;1-6-2-4-7(5-3-6)11(8,9)10/h2-16H,24H2,1H3,(H,26,29);2-5H,1H3,(H,8,9,10)/b11-6+;
InChi Key
IAVXAZDVNICKFJ-ICSBZGNSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $156

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    10 mg

    $279

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    25 mg

    $614

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    50 mg

    $1,077

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    Cayman Chemical
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    Product Description

    4SC-202 is an inhibitor of the class I histone deacetylases (HDACs) HDAC1-3 and the histone demethylase KDM1A.1 It reduces cell viability in a panel of colorectal cancer (CRC) cell lines when used at concentrations ranging from 1 to 10 µM and in patient-derived CRC cell lines when used at a concentration of 5 µM.2 4SC-202 (5 µM) induces cell cycle arrest at the G2/M phase in HT-29 cells and primary human CRC cells and increases apoptosis in HT-29 cells in a concentration-dependent manner, an effect that is enhanced by the Akt inhibitors perifosine (Item No. 10008112) and MK-2206 (Item No. 11593). 4SC-202 (100 mg/kg, p.o., every other day) reduces tumor growth in an HT-29 mouse xenograft model when administered alone and to an enhanced degree when co-administered with oxaliplatin (Item No. 13106).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maes, T., Carceller, E., Salas, J.A., et al. Advances in the development of histone lysine demethylase inhibitors. Curr. Opin. Pharmacol. 23, 52-60 (2015).

    2. Zhijun, H., Shusheng, W., Han, M., et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 37(8), 10257-10267 (2016).