idh1- r132c

GSK864 is an IDH1 mutant inhibitor that inhibits IDH1 mutants R132C, R132H, and R132G, and is used in the study of cardiovascular and oncology diseases.

Mutant IDH1-IN-1 is a potent inhibitor of the mutant IDH1 R132 h, exhibiting an IC50 of less than 0.1 μM.

AGI-5198 (IDH-C35) is a potent and selective inhibitor of IDH1 R132H and R132C mutants, with IC50 values of 0.07 μM and 0.16 μM, respectively.

IDH1 Inhibitor 1 is an orally bioavailable, brain-penetrant, and selective mutant IDH1 inhibitor (IC50s: 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT).

IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. It is 200-fold more selective for mutant IDH1 isoforms than wild type, with IC50s of 27 nM, 28 nM, and 6.14 nM for IDH1R132H, IDH1R132C, and IDH1WT, respectively.

IDH889 is a brain penetrant, an allosteric and mutant specific IDH1 inhibitor. IDH889 has effective selectivity for IDH1 R132* mutations (IC50s: 0.02 μM, 0.072 μM, and 1.38 μM for IDH1R132H, IDH1R132C, and IDH1wt).

Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively).

BRD2879 is a potent and cell-active inhibitor of IDH1-R132H (IC50 = 50 nM).

TC-E 5008 is a selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1).

Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme.

(S,R)-WT IDH1 Inhibitor 2 is a selective and potent mutant IDH1 inhibitor that inhibits R132G (IC50: 2.9 nM), R132C (IC50: 3.8 nM), R132H (IC50: 4.6 nM) and WT IDH1 (IC50: 46 nM) with 100-fold higher selectivity than IDH2. 100-fold higher selectivity than IDH2. (S,R)-WT IDH1 Inhibitor 2 is investigated in acute myeloid leukemia (AML) and other cancers for its ability to induce intracellular 2-HG reduction, failure of myeloid differentiation block, and induction of granulocyte differentiation at the level of leukemia mother cells and more immature stem cells.

IDH1 Inhibitor 9 (compound 11S) (2, 4, 8, 10 µM) induces apoptosis and causes cell cycle arrest in the S phase in a dose-dependent manner.