2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Apoptosis
  3. Isocitrate Dehydrogenase (IDH) PDK-1 Apoptosis
  4. mIDH1-IN-2

mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma.

For research use only. We do not sell to patients.

mIDH1-IN-2

mIDH1-IN-2 Chemical Structure

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mIDH1-IN-2 Related Antibodies

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Description

mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma[1].

IC50 & Target[1]

R132H IDH1

80 nM (IC50)

R132C IDH1

58 nM (IC50)

In Vitro

mIDH1-IN-2 (Compound 27j) inhibits HT1080 and U87-MG cells proliferation all profile with EC50 values of 121.1 nM and 69.0 nM, respectively[1].
mIDH1-IN-2 (1-5 μM, 24-48 h) induces S phase arrest and apoptosis in U87-MG IDH1 R132H cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

mIDH1-IN-2 Related Antibodies

Immunofluorescence[1]

Cell Line: U87-MG IDH1 R132H cells
Concentration: 1, 2 and 5 μM
Incubation Time: 24 and 48 h
Result: Increased the proportion of apoptotic cells.
In Vivo

mIDH1-IN-2 (Compound 27j) (i.v.) is detectable in the brain tissues of mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

501.19

Formula

C18H15Br2NO4S
SMILES

O=C(C1=CC=C(SC2=CC=CC(OC3CCC3)=C2)C([N+]([O-])=O)=C1)C(Br)Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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mIDH1-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

mIDH1-IN-2Isocitrate Dehydrogenase (IDH)PDK-1Apoptosis3-Phosphoinositide-dependent protein kinase 1IDH1PDK1PDHHT1080U87-MGInhibitorinhibitorinhibit

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