Description
SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9 μM in in vitro assay.
Product information
CAS Number: 1456632-41-9
Molecular Weight: 625.61
Formula: C29H28F5N3O5S
Chemical Name: 4-{N-[(4-cyclohexylphenyl)methyl]-2-(N-methyl2,3,4,5,6-pentafluorobenzenesulfonamido)acetamido}-N-hydroxybenzamide
Smiles: CN(CC(=O)N(CC1=CC=C(C=C1)C1CCCCC1)C1C=CC(=CC=1)C(=O)NO)S(=O)(=O)C1C(F)=C(F)C(F)=C(F)C=1F
InChiKey: QPSUYVALAOXFGL-UHFFFAOYSA-N
InChi: InChI=1S/C29H28F5N3O5S/c1-36(43(41,42)28-26(33)24(31)23(30)25(32)27(28)34)16-22(38)37(21-13-11-20(12-14-21)29(39)35-40)15-17-7-9-19(10-8-17)18-5-3-2-4-6-18/h7-14,18,40H,2-6,15-16H2,1H3,(H,35,39)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (79.92 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
SH5-07 is a hydroxamic acid analog of BP-1-102. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in in vitro assay. It preferentially inhibits Stat3:Stat3 DNA-binding activity, ahead of inhibiting Stat1:Stat3 activity, with minimal effects on Stat1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3 association with growth factor receptor, and thereby inhibits Stat3 phosphorylation. It induces antitumor cell effects against malignant cells harboring constitutively-active Stat3. SH5-07 inhibits the expression of known Stat3-regulated genes. Bcl-2, Bcl-xL, c-Myc, Survivin, Cyclin D1 and Mcl-1 expression is reduced in response to 24 h, 5 μM SH5-07 treatment.
In Vivo:
Tail vein injection or oral gavage delivery of SH5-07 or SH4-54 inhibits growth of 90-150 mm3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, associated with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity are observed.
Products are for research use only. Not for human use.
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