IDH
Isocitrate dehydrogenases (IDHs) are enzymes that catalyze the oxidative decarboxylation of isocitrate, producing α-ketoglutarate (αKG) and CO2. In humans, IDHs exist in three isoforms: IDH1, IDH2, and IDH3. IDH1 and IDH2 use nicotinamide adenine dinucleotide phosphate (NADP+) as a co-factor and function as homodimers. Even though IDH1/2 enzymes catalyze the equivalent isocitrate-to-αKG conversion, their reactions are coupled to NADP+ reduction and are reversible. The oxidative decarboxylation that converts αKG to isocitrate occurs predominantly in hypoxic conditions producing citrate and acetyl-CoA from glutamine and glutamate. This activity is critical to preserving lipids and cholesterol biosynthesis in hypoxic cells. Beyond their role in intermediary metabolism and energy production, IDH enzymes are involved also in redox status regulation. Indeed, NAD(P)+/NAD(P)H cofactors are essential for electron transfer in a plethora of cellular functions. This class of enzymes has received much attention, as mutations of IDH1 and IDH2 genes have been found in several malignancies. IDH1/2 mutations are heterozygous and result in amino acid changes that occur primarily at residue R132 in IDH1 and R140 or R172 in IDH2. The mutant proteins display a new enzymatic activity able to catalyze the NADPH-dependent reduction of αKG to D-2-hydroxyglutarate (D-2HG).
References
1.Bergaggio E,et al. Cancers (Basel). 2019 Apr 19;11(4). pii: E563.
References
1.Bergaggio E,et al. Cancers (Basel). 2019 Apr 19;11(4). pii: E563.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
IDH
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Mutant IDH1-IN-2
产品货号 : M26311
cas no: 1429176-69-1
Mutant IDH1-IN-2 是突变异柠檬酸脱氢酶 (IDH) 蛋白的抑制剂,荧光生化检测中的 IC50 为 16.6 nM,LS-MS 生化检测中的 IC50 <22 nM。 -
Olutasidenib
产品货号 : M12951
cas no: 1887014-12-1
Olutasidenib (FT-2102, FT2102) 是一种口服、高效、选择性小分子突变 IDH1 R132 抑制剂。 -
BAY-1436032
产品货号 : M12757
cas no: 1803274-65-8
BAY-1436032 (BAY1436032) 是一种有效的、选择性的、口服的泛突变 IDH1 抑制剂,对 IDH1 R132H 和 R132C 的 IC50 分别为 15 nM。 -
Vorasidenib
产品货号 : M12509
cas no: 1644545-52-7
Vorasidenib (AG-881) 是一种有效的、选择性的、口服生物可利用的泛 IDH(异柠檬酸脱氢酶)突变抑制剂,用于治疗 AML。 -
IDH305
产品货号 : M12434
cas no: 1628805-46-8
IDH 305 (IDH305) 是一种有效的、选择性的、脑渗透性突变 IDH1 抑制剂,对 IDH1 R132H 和 R132C 的 IC50 分别为 18 和 28 nM。