(S,R)-WT IDH1 Inhibitor 2 (Synonyms: GSK321) |
| Catalog No.GC65883 |
(S,R)-WT IDH1 Inhibitor 2 (GSK321) est un puissant inhibiteur IDH1 mutant sélectif avec des valeurs IC50 de 2,9, 3,8, 4,6 et 46 nM pour R132G, R132C, R132H et WT IDH1, respectivement, et >100 fois sélectivité sur IDH2. (S,R)-WT IDH1 Inhibitor 2 induit une diminution du 2-HG intracellulaire, l'abrogation du bloc de différenciation myéloÏde et l'induction de la différenciation granulocytaire au niveau des blastes leucémiques et des cellules souches plus immatures. (S,R)-WT IDH1 Inhibitor 2 peut être utilisé pour la recherche sur la leucémie myéloÏde aiguë (LMA) et d'autres cancers.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1816272-18-0
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
IC50: 2.9 (R132G), 3.8 (R132C), 4.6 (R132H) and 46 nM (WT IDH1)[1]
(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers[1].
(S,R)-WT IDH1 Inhibitor 2 (GSK321; 0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC50 value of 85 nM[1].
(S,R)-WT IDH1 Inhibitor 2 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2)[1].
(S,R)-WT IDH1 Inhibitor 2 (3 μM; 22 d) decreases intracellular 2-HG in a dose-dependent manner (R132G, 0.13-fold; R132C, 0.15-fold; R132H, 0.29-fold)[1].
(S,R)-WT IDH1 Inhibitor 2 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells[1].
(S,R)-WT IDH1 Inhibitor 2 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells[1].
Cell Viability Assay[1]
| Cell Line: | IDH1 mutant AML cells |
| Concentration: | 3 μM |
| Incubation Time: | 15 days |
| Result: | Increased in cell numbers (2-fold to 15-fold) in IDH1 mutant AML cells. |
Cell Cycle Analysis[1]
| Cell Line: | IDH1 mutant AML cells |
| Concentration: | 3 μM |
| Incubation Time: | 15 days |
| Result: | Decreased in quiescent (G0)-phase cells and increased in G1-phase in R132G IDH1. |
Western Blot Analysis[1]
| Cell Line: | HT1080 fibrosarcoma cells |
| Concentration: | 0, 0.5 and 5 μM |
| Incubation Time: | 48 hours |
| Result: | Induced markedly decreased H3K9me2 levels. |
(S,R)-WT IDH1 Inhibitor 2 (GSK321; 150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo[1].
| Animal Model: | Male CD-1 mice with IDH1 mutant AML xenograft[1] |
| Dosage: | 150 mg/kg |
| Administration: | Intraperitoneal injection; daily, for 15 days |
| Result: | Decreased in 2HG in IDH1-mutant AML cells. Decreased in the percentage of blast cells (SSClowCD45low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *