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Mutant IDH1 inhibitor

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By Targets:	Apoptosis (3) Bacterial (2) Fungal (2) Isocitrate Dehydrogenase (IDH) (28) NAMPT (1) Reactive Oxygen Species (2) Virus Protease (2)
By Research Areas:	Cancer (29) Inflammation/Immunology (1) Neurological Disease (1)

Inhibitors & Agonists

Natural
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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13972

**Mutant IDH1 inhibitor** 2 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC₅₀ of < 72 nM.

HY-12475

Mutant IDH1-IN-1 2 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
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.

HY-104036

IDH-305 1 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
IDH-305 is an orally available, mutant-selective and brain-penetrant *IDH1* inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC₅₀= 27 nM (IDH1 ^R132H), 28 nM (IDH1 ^R132C), 6.14 µM (IDH1 ^WT)) .

HY-112601

IDH1 Inhibitor 1	Isocitrate Dehydrogenase (IDH)	Cancer
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 IDH1 ^R132H, IDH1 ^R132C, and IDH1 ^WT, respectively . Anticancer activity .

HY-145594

Safusidenib AB-291; DS-1001	Isocitrate Dehydrogenase (IDH)	Cancer
Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant *IDH1* inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma . Safusidenib exhibits activity against *IDH1R132H, and IDH1R132C* with IC₅₀s of 15, and 130 nM in assays without any preincubation, respectively .

HY-149359

IHMT-IDH1-053	Isocitrate Dehydrogenase (IDH)	Cancer
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible *IDH1-mutant* inhibitor with an IC₅₀ of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC₅₀=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .

HY-158319

Mutant IDH1/NAMPT-IN-1	Apoptosis Isocitrate Dehydrogenase (IDH) NAMPT	Cancer
Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of **mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC₅₀=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC₅₀*=12.56 nM). Mutant* IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively .

HY-107977

IDH1 Inhibitor 3	Isocitrate Dehydrogenase (IDH)	Cancer
IDH1 Inhibitor 3 (compound 6f) is a mutant isocitric dehydrogenase 1 (IDH1) inhibitor, with an IC₅₀ of 45 nM for IDH1 ^R132H .

HY-131312

LY3410738 Mutant IDH1-IN-6	Isocitrate Dehydrogenase (IDH)	Cancer
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (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 mutant* enzymes*, respectively. Mutant* IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .

HY-143306

IDH1 Inhibitor 5	Isocitrate Dehydrogenase (IDH)	Cancer
IDH1 Inhibitor 5 (compound 2) is an *IDH1* (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC₅₀s of 64.4 and 34.9 nM, respectively .

HY-114459

Mutant IDH1-IN-4	Isocitrate Dehydrogenase (IDH)	Cancer
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 .

HY-19540

GSK864 4 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
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.

HY-18948

GSK321 1 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
GSK321 is a potent inhibitor of mutant *isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant* IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia .

HY-110144

TC-E 5008	Isocitrate Dehydrogenase (IDH)	Cancer
TC-E 5008 is a potent **mutant IDH1** inhibitor with K_i values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a K_i value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .

HY-112289

IDH889	Isocitrate Dehydrogenase (IDH)	Cancer
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC₅₀s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 ^R132H, IDH1 ^R132C and IDH1 ^wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC₅₀ of 0.014 μM .

HY-100020

BAY-1436032 3 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

HY-18717

Mutant IDH1-IN-2 2 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
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.

HY-N0328

alpha-Mangostin 3 Publications Verification α-Mangostin	Reactive Oxygen Species Apoptosis Bacterial Fungal Virus Protease	Cancer
alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a K_i of 2.85 μM.

HY-121736

AGI-12026 AGI-026	Isocitrate Dehydrogenase (IDH)	Neurological Disease
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .

HY-114226

Olutasidenib 1 Publications Verification FT-2102	Isocitrate Dehydrogenase (IDH)	Inflammation/Immunology Cancer
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of **mutant Isocitrate dehydrogenase 1 (IDH1), with IC₅₀** values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .

HY-112289B

(1R)-IDH889	Isocitrate Dehydrogenase (IDH)	Cancer
(1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC₅₀s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 ^R132H, IDH1 ^R132C and IDH1 ^wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC₅₀ of 0.014 μM .

HY-128888

(R,R)-GSK321	Isocitrate Dehydrogenase (IDH)	Cancer
(R,R)-GSK321 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC₅₀ value of 120 nM. (R,R)-GSK321 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity .

HY-104042

Vorasidenib 4 Publications Verification AG-881	Isocitrate Dehydrogenase (IDH)	Cancer
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC₅₀ ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .

HY-18082

AGI-5198 Maximum Cited Publications 15 Publications Verification IDH-C35	Isocitrate Dehydrogenase (IDH)	Cancer
AGI-5198 (IDH-C35) is a potent and selective mutant IDH1 ^R132H inhibitor with an IC₅₀ of 0.07 μM.

HY-N0328R

alpha-Mangostin (Standard) α-Mangostin (Standard)	Fungal Reactive Oxygen Species Bacterial Apoptosis Virus Protease	Cancer
alpha-Mangostin (Standard) is the analytical standard of alpha-Mangostin. This product is intended for research and analytical applications. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a K_i of 2.85 μM.

HY-129545

DS-1001b 1 Publications Verification	Isocitrate Dehydrogenase (IDH)	Cancer
DS-1001b is an orally active, blood-brain permeable, potent *IDH-1* (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity .

HY-N12390

Alternaphenol B2	Isocitrate Dehydrogenase (IDH)	Cancer
Alternaphenol B2 is a selective *IDH1* inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC₅₀ values of 41.9 μM .

HY-143234

mIDH1-IN-1	Isocitrate Dehydrogenase (IDH)	Cancer
mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC₅₀ of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC₅₀ of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC₅₀ of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .

HY-128888B

(S,R)-GSK321	Isocitrate Dehydrogenase (IDH)	Cancer
(S,R)-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)-GSK321 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)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .

HY-120181

AGI-14100	Isocitrate Dehydrogenase (IDH)	Cancer
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC₅₀=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .

alpha-Mangostin 3 Publications Verification α-Mangostin	Structural Classification other families Xanthones Classification of Application Fields Phenols Polyphenols Plants Disease Research Fields Cancer	Reactive Oxygen Species Apoptosis Bacterial Fungal Virus Protease
alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a K_i of 2.85 μM.

alpha-Mangostin (Standard) α-Mangostin (Standard)	Structural Classification other families Xanthones Classification of Application Fields Source classification Phenols Polyphenols Plants Disease Research Fields Cancer	Fungal Reactive Oxygen Species Bacterial Apoptosis Virus Protease
alpha-Mangostin (Standard) is the analytical standard of alpha-Mangostin. This product is intended for research and analytical applications. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a K_i of 2.85 μM.

Alternaphenol B2	Structural Classification Microorganisms Source classification Phenols Polyphenols	Isocitrate Dehydrogenase (IDH)
Alternaphenol B2 is a selective *IDH1* inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC₅₀ values of 41.9 μM .

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Mutant IDH1 inhibitor

Inhibitors & Agonists

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