GSK321
Based on 1 publication(s) in Google Scholar
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. GSK321 induces decrease in intracellular α-Hydroxyglutaric acid (2-HG) (HY-113038B), abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers.
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- Pureza: 99.87%
- No. CAS: 1816331-63-1
- Fòrmula: C28H28FN5O3
- Peso molecular:501.55
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Publications Citing Use of MedChemExpress (MCE) GSK321
More
Actividad biológica
IC50 for mutant IDH1 enzymes: 4.6 nM (R132H), 3.8 nM (R132C), 2.9 nM (R132G)[1].
GSK321 (0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC50 value of 85 nM[1].
GSK321 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2)[1].
GSK321 (3 μM; 22 d) decreases intracellular 2-HG in a dose-dependent manner (R132G, 0.13-fold; R132C, 0.15-fold; R132H, 0.29-fold)[1].
GSK321 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells[1].
GSK321 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080 cells
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Concentration:0, 0.5, 5 μM
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Incubation Time:48 h
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Result:Lead to the reduction of histone H3K9 dimethylation (H3K9me2).
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Cell Line:IDH1 mutant AML cells
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Concentration:3 μM
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Incubation Time:15 days
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Result:Showed a significant, initial increase in cell numbers (2-fold to 15-fold) in IDH1 mutant AML cells.
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Cell Line:IDH1 mutant AML cells
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Concentration:3 μM
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Incubation Time:15 days
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Result:Decreased in quiescent (G0)-phase cells and increased in G1-phase in R132G IDH1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD-1 mice with IDH1 mutant AML xenograft[1]
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Dosage:150 mg/kg
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Administration:Intraperitoneal injection; daily, for 15 days
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Result:Decreased in 2HG in IDH1-mutant AML cells. Decreased in the percentage of blast cells (SSClowCD45low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.
Chemical Information
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No. CAS 1816331-63-1
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Appearance Solid
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Peso molecular 501.55
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Fòrmula C28H28FN5O3
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Color Off-white to light brown
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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EMBO Rep
HDAC6 deacetylates IDH1 to promote the homeostasis of hematopoietic stem and progenitor cells. [Abstract]2023 Oct 9;24(10):e56009. PMID: 37642636
Solvente y solubilidad
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)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
| 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 |
GSK321 Related Classifications
HY-18948 Related Classifications
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