(S,R)-WT IDH1 Inhibitor 2
Modify Date: 2025-08-27 16:03:20
(S,R)-WT IDH1 Inhibitor 2 structure
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Common Name | (S,R)-WT IDH1 Inhibitor 2 | ||
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| CAS Number | 1816272-18-0 | Molecular Weight | 501.55 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H28FN5O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of (S,R)-WT IDH1 Inhibitor 2(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]. |
| Name | (S,R)-WT IDH1 Inhibitor 2 |
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| Description | (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]. |
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| Related Catalog | |
| Target |
IC50: 2.9 (R132G), 3.8 (R132C), 4.6 (R132H) and 46 nM (WT IDH1)[1] |
| In Vitro | (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. |
| In Vivo | (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. |
| References |
| Molecular Formula | C28H28FN5O3 |
|---|---|
| Molecular Weight | 501.55 |
| InChIKey | IVFDDVKCCBDPQZ-ZWKOTPCHSA-N |
| SMILES | CC(O)c1cccc(NC(=O)c2nn(Cc3ccc(F)cc3)c3c2CN(C(=O)c2ccc[nH]2)CC3C)c1 |