TW-37

Catalog #

27775-1

$230 *

Size: 10 mg

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Description

TW-37 is a potent small-molecule inhibitor that attenuates Bcl-2 activation and inhibits multiple Bcl-2 family members including Bcl-xL and Mcl-1. TW-37 also inhibits in vivo and in vitro the activation of Jagged-1 and Notch-1.

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Synonyms

TW37; N-[4-(2-tert-butylphenyl)sulfonylphenyl]-2,3,4-trihydroxy-5-[(2-propan-2-ylphenyl)methyl]benzamide

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Product Info

Storage and Usage

Citations

Target(s)

Bcl2

Formula

C₃₃H₃₅NO₆S

573.7 Da

Solubility

Soluble in DMSO (100 mM), ethanol (5 mM), and water (<1 mg/ml).

Biological Activity

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 µM, 1.11 µM and 0.26 µM, respectively. Bcl-2: IC50 = 0.2 µM (human); Bcl-XL: IC50 = 6.58 µM (human); Mcl-1: IC50 = 1.03 µM

CAS Registry #

877877-35-5

Background

TW-37 is a Bcl-2 inhibitor that has been shown to inhibit the angiogenic potential of endothelial cells in vitro. S-phase arrest and apoptosis in pancreatic cancer cell lines have been observed to be induced by TW-37. It binds to the Bcl-2 homology domain 3 (BH3) groove of Bcl-2 preventing the heterodimerization of proapoptotic proteins (such as Bid, Bim, and Bad) with Bcl-2 and subsequently allowing them to induce apoptosis. Recent studies indicate TW-37 is able to inhibit the growth of a broad range of cancer cells (such as breast, prostate, lymphoma, and pancreatic cancer), since it induces S-phase cell cycle arrest with regulation of several important cell cycle related genes, including p27, p57, E2F-1, cdc25A, CDK4, cyclin A, cyclin D1 and cyclin E.

References

1. Wang, Z., et al. Cancer Res 2009;69:2757-2765.
2. Ashimori, N., et al. Mol Cancer Ther 2009;8:893-903.

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TW-37

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