A STAT3 inhibitor
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STAT3 Inhibitor 4m

Item No. 37352

Technical Information
Formal Name
(2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-N-(2-(thiophen-2-yl)ethyl)-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxamide
CAS Number
3033049-16-7
Synonyms
  • Signal Transducer and Activator of Transcription 3 Inhibitor 4m
Molecular Formula
C35H45NO3S
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
Chloroform: Soluble
SMILES
O=C(NCCC1=CC=CS1)[C@]2(C)CC[C@]3(C)CC[C@]4(C)C([C@@]5(C)CC[C@@]4(C)[C@]3([H])C2)=CC=C(C5=C6)C(C)=C(O)C6=O
InChi Code
InChI=1S/C35H45NO3S/c1-22-24-9-10-27-33(4,25(24)20-26(37)29(22)38)15-17-35(6)28-21-32(3,13-12-31(28,2)14-16-34(27,35)5)30(39)36-18-11-23-8-7-19-40-23/h7-10,19-20,28,38H,11-18,21H2,1-6H3,(H,36,39)/t28-,31-,32-,33+,34-,35+/m1/s1
InChi Key
JKWCCKBBTJGQQC-GTKRWHGSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    STAT3 inhibitor 4m is an inhibitor of STAT3 and a derivative of celastrol (Item No. 70950).1 It inhibits the phosphorylation of STAT3 and decreases levels of the STAT3 target proteins survivin and myeloid cell leukemia 1 (Mcl-1) in HCT116 cells when used at concentrations of 0.75 and 1 µM. STAT3 inhibitor 4m inhibits the proliferation of A549, HCT116, and HepG2 cells (IC50s = 0.93, 0.61, and 1.79 µM, respectively). It induces apoptosis and cell cycle arrest at both the S and G2/M phases in HCT116 cells when used at a concentration of 5 µM. STAT3 inhibitor 4m (1-10 µM) also reduces the viability of human colorectal cancer organoids (CCOs).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xu, S., Fan, R., Wang, L., et alSynthesis and biological evaluation of celastrol derivatives as potent antitumor agents with STAT3 inhibition. J. Enzyme Inhib. Med. Chem. 37(1), 236-251 (2022).