Description
As a new inhibitor,TW-37 can recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 uM, 1.11 uM and 0.26 uM.
Storage
2 years at -20 centigrade
Targets
Bcl-2, Bcl-xL, Mcl-1
Molecular Formula
C33H35NO6S
Chemical Name
5-(2-isopropylbenzyl)-N-(4-(2-tert-butylphenylsulfonyl)phenyl)-2,3,4-trihydroxybenzamide
Solubility
DSMO 115 mg/mL Water
In vitro
As a potent inhibitor of Bcl-2, TW-37 can inhibit recombinant Bcl-2, Bcl-X(L), and Mcl-1 with Ki of 290 nM,110 nM and 260 nM. And TW-37 shows selectivity for Bcl-X(L). For cell lines, TW-37 showed significant antiproliferative effect to WSU-DLCL(2) lymphoma cell line and primary cells. TW-37 disrupted heterodimer formation between Bax and antiapoptotic proteins including Mcl-1, Bcl-2, and Bcl-X(L). TW-37 inhibited cell growth in a dose- and time-dependent manner. This was accompanied by increased apoptosis and concomitant attenuation of NF-kappaB, and downregulation of NF-kappaB downstream genes such as MMP-9 and VEGF, resulting in the inhibition of pancreatic cancer cell migration, invasion and angiogenesis in vitro. And TW-37 can cause apoptotic death.
In vivo
In Colo-357 human PC xenografts in SCID mice, TW-37 treatment signi?cantly inhibited tumor growth. TW-37 could affect the function of NF-kappaB in vivo, and the expression of VEGF, MMP-9, COX-2, Cyclin D1 and Survivin was also downregulated in TW-37-treated animals.
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