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SMI-4a (TCS PIM-1 4a) is a potent Pim1 inhibitor with an IC50 of 17 nM and is moderately effective against Pim-2, with no significant inhibition of other silk/threonine or tyrosine kinases.
Brand: BCM
Target: Pim
Signaling Pathways: Chromatin/Epigenetic; JAK/STAT signaling
In Vitro: One hour after oral administration of SMI-4a, p70S6K phosphorylation was reduced compared to the tumors of control mice, while total p70S6K expression was unchanged. SMI-4a treated with 60 mg/kg twice daily significantly reduced tumor size and was well tolerated.
pKa: 7.38±0.20(Predicted)
Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.
GHS: GHS07
Isomeric SMILES: C1=CC(=CC(=C1)C(F)(F)F)/C=C\2/C(=O)NC(=O)S2
InChIKey: NGJLOFCOEOHFKQ-YVMONPNESA-N
InChI: InChI=1S/C11H6F3NO2S/c12-11(13,14)7-3-1-2-6(4-7)5-8-9(16)15-10(17)18-8/h1-5H,(H,15,16,17)/b8-5-
Attribute [Chem Name] (5Z)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione [Synonym] SMI-4a; TCS PIM-1 4a [CAS No.] 438190-29-5 [EINECS] 200-256-5 [MDL No.] MFCD01152003 [Formula] C11H6F3NO2S [Molecular] 273.23 [Form] White to beige powder [Storage] Sealed in dry, 2-8°C
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