| Identification | Back Directory | [Name]
methyl 3-(4-methylphenylsulfonamido)benzoate | [CAS]
173436-66-3 | [Synonyms]
MSAB
GSK549
MSAB >=95% (HPLC)
methyl 3-(4-methylphenylsulfonamido)benzoate
Methyl 3-(4-Methylbenzenesulfonamido)benzoate
Benzoic acid, 3-[[(4-methylphenyl)sulfonyl]amino]-, methyl ester | [Molecular Formula]
C15H15NO4S | [MDL Number]
MFCD00994918 | [MOL File]
173436-66-3.mol | [Molecular Weight]
305.35 |
| Chemical Properties | Back Directory | [Melting point ]
152-154 °C | [Boiling point ]
456.5±55.0 °C(Predicted) | [density ]
1.312±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
Chloroform (Slightly), DMSO (Slightly) | [form ]
powder | [pka]
7.88±0.10(Predicted) | [color ]
off-white to purple | [InChIKey]
CVKBYFCJQSPBOI-UHFFFAOYSA-N | [SMILES]
CC1=CC=C(S(NC2=CC(C(OC)=O)=CC=C2)(=O)=O)C=C1 |
| Hazard Information | Back Directory | [Uses]
MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin and promotes its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells[1]. | [Biochem/physiol Actions]
A cell-permeable compound that targets β-catenin via direct affinity interaction within the C-terminal two thirds (a.a. 301-670) of the Armadillo repeat region (a.a. 136–686), inducing β-catenin ubiquitination and proteasomal degradation (Eff. conc. 1.25-5 μM in DLD-1, SW480 and LS174T cultures). MSAB selectively inhibits against Wnt sginaling-dependent proliferation of cancer cells (IC50 <6 μM), while exhibiting little efficacy in Wnt-independent cultures (<10% inhibition at 10 μM). Likewise, daily intraperitoneal injection (10-20 mg/kg/day) is efficacious in suppressing the expansion of established tumors from HCT116, HT115, and H23 xenografts in mice, while exhibiting little efficacy against the Wnt-independent H460 tumor growth. | [in vivo]
MSAB (10-20 mg/kg; i.p. daily for 2 weeks) inhibits tumor growth of Wnt-dependent cancer cells in mouse xenograft model[1].
MSAB (10-20 mg/kg; i.p. twice daily for 2 weeks) inhibits tumor growth of MMTV-Wnt1 transgenic mice[1]. | Animal Model: | Athymic nude mice (5-6 weeks) are injected HCT116, HT115, H23, or H460 cells[1] | | Dosage: | 10, 20 mg/kg | | Administration: | I.p. daily for 2 weeks | | Result: | Reduced the size and weight of various types of Wnt-dependent HCT116, HT115, and H23 tumors. |
| [References]
[1] Hwang SY, et, al. Direct Targeting of β-Catenin by a Small Molecule Stimulates Proteasomal Degradation and Suppresses Oncogenic Wnt/β-Catenin Signaling. Cell Rep. 2016 Jun 28;16(1):28-36. DOI:10.1016/j.celrep.2016.05.071 |
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| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Twochem Co.Ltd
|
| Telephone: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
|