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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- Pureté: 99.87%
- CAS No.: 1816331-63-1
- Formule: C28H28FN5O3
- Masse moléculaire:501.55
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Stockage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK321
More
Activité biologique
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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CAS No. 1816331-63-1
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Appearance Solid
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Masse moléculaire 501.55
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 |
GSK321 Related Classifications
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