Shopping Cart
- Remove All
Your shopping cart is currently empty
IHMT-IDH1-053
😃Good
Catalog No. T78758
IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].
IHMT-IDH1-053
IHMT-IDH1-053
😃Good
Catalog No. T78758
IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | Inquiry | Backorder | |
| 50 mg | Inquiry | Backorder |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "IHMT-IDH1-053"
Ivosidenib
AG-120
T36171448347-49-6
Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1) with potential antineoplastic activity. It specifically inhibits a mutated form of IDH1 in the cytoplasm, preventing the formation of the oncometabolite 2-hydroxyglutarate (2 hG), which may induce cellular differentiation and inhibit cellular proliferation in IDH1-expressing tumor cells.
- $42
Size
QTY
Mutant IDH1-IN-2
T121281429176-69-1In house
Mutant IDH1-IN-2 is an inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with an IC50 of 16.6 nM in fluorescence biochemical assay and an IC50 of <22 nM in LS-MS biochemical assay.
- $58
Size
QTY
Enasidenib
AG-221
T23461446502-11-9
Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity.
- $39
Size
QTY
AGI-6780
Cited
T18091432660-47-3
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.
- $31
Size
QTY
CitedMutant IDH1 inhibitor
T161611429180-08-4
Mutant IDH1 inhibitor is an effective inhibitor of mutant IDH1 R132H (IC50: < 72 nM).
- $35
Size
QTY
Olutasidenib
FT-2102
T163841887014-12-1
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).
- $56
Size
QTY
DS-1001b
T77411898207-64-1
DS-1001b is an inhibitor of mutant IDH-1 (Isocitrate Dehydrogenase-1)
- $31
Size
QTY
Mutant IDH1-IN-1
IDH1-IN-1
T20431355326-21-4
Mutant IDH1-IN-1 is a potent inhibitor of the mutant IDH1 R132 h, exhibiting an IC50 of less than 0.1 μM.
- $38
Size
QTY
Vorasidenib
PVM/MA, AG-881
T73071644545-52-7
Vorasidenib (PVM/MA) is an inhibitor of mutant isocitrate dehydrogenase (IDH; IC50s = 31.9 and 31.7 nM for IDH1R132H and IDH2R140Q, respectively)
- $48
Size
QTY
BAY-1436032
TQ00421803274-65-8
BAY-1436032 is a novel, selective and orally available inhibitor of pan-mutant isocitrate dehydrogenase 1 (IDH1).
- $31
Size
QTY
AGI-5198
IDH-C35
T21041355326-35-0
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.
- $31
Size
QTY
SH1573
T2002092376068-96-9
SH1573 is an orally active inhibitor of mutant isocitrate dehydrogenase 2 (mIDH2). It selectively targets the mIDH2 R140Q protein with a potent inhibitory effect (IC50=4.78 nmol/L), significantly reducing the production of the oncogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum, and tumors. SH1573 is utilized in the study of acute myeloid leukemia (AML).
- Inquiry Price
Size
QTY
Contact us for more batch information
Resource Download
Product Introduction
Bioactivity
Chemical Properties
| Description | IHMT-IDH1-053 (compound 16) is an irreversible inhibitor highly selective for the IDH1 R132H mutant, with an IC50 of 4.7 nM. It preferentially targets IDH1 mutants over wild-type IDH1 and IDH2, in both their wild-type and mutant forms. In 293T cells transfected with the IDH1 R132H mutant, IHMT-IDH1-053 reduces 2-hydroxyglutarate (2-HG) production with an IC50 of 28 nM. The compound binds to the R132H protein at an allosteric site near the NADPH binding region, forming a covalent linkage with Cys269. Additionally, IHMT-IDH1-053 inhibits the growth of both the HT1080 cell line and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutations [1]. |
| Targets&IC50 | R132H IDH1:4.7 μM |
| Molecular Weight | 532.63 |
| Formula | C25H33FN6O4S |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Keywords
Preview
Related Tags: buy IHMT-IDH1-053 | purchase IHMT-IDH1-053 | IHMT-IDH1-053 cost | order IHMT-IDH1-053 | IHMT-IDH1-053 formula | IHMT-IDH1-053 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.