|
|
|
| 【主 题】 ： |
Degrasyn |
| 【联系人名】 ： |
Linna Green |
| 【电子邮件】 ： |
account@bocsci.com |
| 【联系电话】 ： |
15166698109 |
| 【发布日期】 ： |
2016-9-6 |
| 【详细说明】 ： |
Degrasyn, also known as WP1130, is a small molecule
that specifically and rapidly down-regulates both
wild-type and mutant Bcr/Abl protein without
affecting bcr/abl gene expression in chronic
myelogenous leukemia (CML) cells and Hsp90/Hsp70
ratios within the cells. WP1130 was more effective
in reducing leukemic versus normal hematopoietic
colony formation and strongly inhibited colony
formation of cells derived from patients with T315I
mutant Bcr/Abl-expressing CML in blast crisis.
WP1130 suppressed the growth of K562
heterotransplanted tumors as well as both wild-type
Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3
cells transplanted into nude mice. WP1130 may be
useful in treating CML.
MM1: IC50 = 1 μM (human); U-266: IC50 = 1.3 μM
(human); USP9X: IC50 = 3 μM (human); UCH-L1: IC50 =
3 μM (human); USP5: IC50 = 3 μM (human)
In vitro: a partly selective DUB inhibitor, directly
inhibiting DUB activity of USP9x, USP5, USP14, and
UCH37, which are known to regulate survival protein
stability and 26S proteasome function;
In vivo: suppressed the growth of K562
heterotransplanted tumors as well as both wild-type
Bcr/Abl and T315I mutant Bcr/Abl-expressing BaF/3
cells transplanted into nude
mice.http://www.bocsci.com/degrasyn-cas-856243-80-6-
item-84-307702.html
|
|
|
|
|
English
