2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. GSK321

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.

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

GSK321 Chemical Structure

GSK321 Chemical Structure

CAS No. : 1816331-63-1

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Based on 1 publication(s) in Google Scholar

Other Forms of GSK321:

GSK321 Related Antibodies

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1 Publications Citing Use of MCE GSK321

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Description

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[1][2].

IC50 & Target

IC50 for mutant IDH1 enzymes: 4.6 nM (R132H), 3.8 nM (R132C), 2.9 nM (R132G)[1].
In Vitro

GSK321 has high inhibitory for mutant IDH1 enzymes, with IC50 values of 4.6 nM against R132H, 3.8 nM against R132C and 2.9 nM against R132G, respectively[1].
GSK321 (0, 0.5, 5 μM; 48 h) induces markedly decreased H3K9me2 levels[1].
GSK321 decreases intracellular 2-HG and affects proliferation of primary IDH1 mutant AML cells[1].
GSK321 has inhibition activity for mutant IDH1 that overcomes the pathognomonic differentiation block of AML cells, and induces myeloid differentiation of IDH1 mutant cells at the level of leukemic blasts and more stem-like cells[1].
GSK321 leads to genome-wide DNA cytosine hypomethylation in IDH1-mutant AML cells[1].

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

GSK321 Related Antibodies

Western Blot Analysis[1]

Cell Line: HT-1080 cells
Concentration: 0, 0.5, 5 μM
Incubation Time: 48 h
Result: Lead to the reduction of histone H3K9 dimethylation (H3K9me2).

Cell Proliferation Assay[1]

Cell Line: IDH1 mutant AML cells
Concentration: 3 μM
Incubation Time: 15 days
Result: Showed a significant, initial increase in cell numbers (2-fold to 15-fold) in IDH1 mutant AML cells.

Cell Cycle Analysis[1]

Cell Line: IDH1 mutant AML cells
Concentration:
Incubation Time: 7 days
Result: Observed a reproducible and significant decrease in quiescent (G0)-phase cells in R132G IDH1 and R132C IDH1 AML cells.
Molecular Weight

501.55

Formula

C28H28FN5O3
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

O=C(C1=CC=CN1)N2C[C@@H](C)C(N(CC3=CC=C(F)C=C3)N=C4C(NC5=CC([C@H](C)O)=CC=C5)=O)=C4C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (498.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9938 mL 9.9691 mL 19.9382 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9938 mL 9.9691 mL 19.9382 mL 49.8455 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL 9.9691 mL
10 mM 0.1994 mL 0.9969 mL 1.9938 mL 4.9845 mL
15 mM 0.1329 mL 0.6646 mL 1.3292 mL 3.3230 mL
20 mM 0.0997 mL 0.4985 mL 0.9969 mL 2.4923 mL
25 mM 0.0798 mL 0.3988 mL 0.7975 mL 1.9938 mL
30 mM 0.0665 mL 0.3323 mL 0.6646 mL 1.6615 mL
40 mM 0.0498 mL 0.2492 mL 0.4985 mL 1.2461 mL
50 mM 0.0399 mL 0.1994 mL 0.3988 mL 0.9969 mL
60 mM 0.0332 mL 0.1662 mL 0.3323 mL 0.8308 mL
80 mM 0.0249 mL 0.1246 mL 0.2492 mL 0.6231 mL
100 mM 0.0199 mL 0.0997 mL 0.1994 mL 0.4985 mL
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GSK321 Related Classifications

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:

GSK3211816331-63-1GSK 321GSK-321Isocitrate Dehydrogenase (IDH)mutantisocitrate dehydrogenase 1 (IDH1)R132HR132CR132Gacute myeloid leukemiaInhibitorinhibitorinhibit

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