Isocitrate Dehydrogenase (IDH)

AGI-5198, also know as IDH-C35, is the a very potent and selective mutant IDH1 inhibitor that was shown to potential anticancer activity.

AGI-6780 is a potent, selective inhibitor of mutant IDH2 with an IC50 value of 23 nM.

IDH-C227 is a potent and selective IDH1 R132H inhibitor.

AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.

Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).

Vorasidenib, also known as AG-881, is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type 2 (IDH2, isocitrate dehydrogenase [NADP+], mitochondrial) in the mitochondria, with potential antineoplastic activity.

IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.

BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1).

DH1 Inhibitor 2 is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC50 of 110 nM.

Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia.

Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ?? 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.

IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC50 of 45 nM for IDH1R132H.

IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1).

IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity.

GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.

Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.

Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.

DS-1001b is a mutant IDH-1 (Isocitrate Dehydrogenase-1) inhibitor extracted from patent WO2016052697A1, Example 168, and has antitumor activity.

GSK321 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), showing IC50 values of 2.9, 3.8, 4.6, and 46 nM for the R132G, R132C, R132H, and wild-type IDH1 variants, respectively, with over 100-fold selectivity for IDH2. This compound effectively reduces intracellular levels of α-Hydroxyglutaric acid (2-HG), disrupts the myeloid differentiation block, and promotes granulocytic differentiation in leukemic blasts and stem-like cells. GSK321 is valuable for research on acute myeloid leukemia (AML) and various other malignancies.

Alpha-Mangostin is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1-R132H), demonstrating a Ki of 2.85 μM. This dietary xanthone exhibits a diverse range of biological activities, including antioxidant, anti-inflammatory, antibacterial, and anticancer properties. It is valuable for research applications exploring metabolic pathways in cancer and the development of targeted therapies against IDH1-mutant tumors.

IDH1 Inhibitor 9 is a selective inhibitor targeting isocitrate dehydrogenase 1 (IDH1), exhibiting IC50 values of 124.4 nM and 95.7 nM for the R132H and R132C mutations, respectively. This compound effectively induces apoptosis and promotes cell cycle arrest at the S phase. Due to its anti-tumor properties, IDH1 Inhibitor 9 is valuable for research in cancer biology and the development of targeted therapies in IDH1-mutated cancers.

ZD-2767P is a reversible and competitive inhibitor of isocitrate dehydrogenase 1 (IDH1), with an IC50 value of 410 nM. This compound has been shown to effectively modulate IDH1 activity, making it a valuable tool for investigating metabolic pathways and oncogenic processes associated with IDH1 mutations. ZD-2767P is suitable for research applications focused on cancer biology and metabolic regulation.

Mutant IDH1/NAMPT-IN-1 is a dual inhibitor targeting mutant isocitrate dehydrogenase 1 (mutant IDH1) and nicotinamide phosphoribosyltransferase (NAMPT), with IC50 values of 14.93 nM and 12.56 nM, respectively. This compound effectively induces apoptosis, making it a valuable tool for research into cancer mechanisms and treatment strategies. Additionally, Mutant IDH1/NAMPT-IN-1 demonstrates the capability to cross the blood-brain barrier, enhancing its potential for applications in neurological studies and therapies.

(R)-IDHP is an isomer of isovaleryl-DL-3-hydroxybutyric acid, functioning primarily by inhibiting Ca2+ release and modulating Ca2+ inward flow in both voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. This compound exhibits vasorelaxant properties and is valuable in research focused on cardiovascular disease mechanisms and treatments. Its biological activity makes it a useful tool for investigating vascular dynamics and related pathophysiological conditions.