WT-161

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效、选择性和生物可利用的 HDAC6 抑制剂，IC50 为 0.4 nM。

A potent, selective, and bioavailable HDAC6 inhibitor with IC50 0.4 nM; displays >20-fold selectivity over HDAC1/2/3/8; selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin with little effect on global lysine acetylation in cells; reversibly and rapidly induces the accumulation of Ac-α-tubulin in MM cell lines, displays synergism with both BTZ and CFZ, caspase activation and apoptosis; demonstrates a significant antitumor effect in human MM cell xenograft mouse model combined with BTZ.

WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC50s between 1.5 and 4.7 μM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance.

WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined with WT161 demonstrates a significant antitumor effect.

WT 161 | WT161

Cell Cycle/DNA Damage

HDAC

HDAC

Cancer

——

1206731-57-8

458.55

C27H30N4O3

>98% (HPLC)

DMSO : ≥ 100 mg/mL 218.08 mM

O=C(NO)CCCCCCC(N/N=C/C1=CC=C(N(C2=CC=CC=C2)C3=CC=CC=C3)C=C1)=O

Octanoic acid, 8-(hydroxyamino)-8-oxo-, 2-[[4-(diphenylamino)phenyl]methylene]hydrazide

(-20℃)

With Ice Pack

≥ 2 years