Cat. No.: HY-18948

GSK321

1 Cited Publications

Customer Review

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.

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

Purity: 99.87%
CAS No.: 1816331-63-1
Formula: C₂₈H₂₈FN₅O₃
Molecular Weight:501.55

Storage:

4°C, protect from light

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

GSK321 Chemical Structure

CAS No.: 1816331-63-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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

All Isocitrate Dehydrogenase (IDH) Isoforms :

IDH1
IDH2

In Vitro

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.

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:

3 μM
Incubation Time:

15 days
Result:

Decreased in quiescent (G0)-phase cells and increased in G1-phase in R132G IDH1.

In Vivo

GSK321 (150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo^[1].

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

Animal Model:

Male CD-1 mice with IDH1 mutant AML xenograft^[1]
Dosage:

150 mg/kg
Administration:

Intraperitoneal injection; daily, for 15 days
Result:

Decreased in 2HG in IDH1-mutant AML cells. Decreased in the percentage of blast cells (^SSClowCD45^low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.

Chemical Information

CAS No. 1816331-63-1
Appearance Solid
Molecular Weight 501.55
Formula C₂₈H₂₈FN₅O₃
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)

Publications (1)

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Journal Impact Factor

EMBO Rep

HDAC6 deacetylates IDH1 to promote the homeostasis of hematopoietic stem and progenitor cells. [Abstract]

2023 Oct 9;24(10):e56009. PMID: 37642636

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9938 mL

9.9691 mL

19.9382 mL

5 mM

0.3988 mL

1.9938 mL

3.9876 mL

10 mM

0.1994 mL

0.9969 mL

1.9938 mL

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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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ujunwa C Okoye-Okafor, et al. New IDH1 mutant inhibitors for treatment of acute myeloid leukemia. Nat Chem Biol. 2015 Nov;11(11):878-86. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

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GSK321

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Glutamine Metabolism Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK321

All Isocitrate Dehydrogenase (IDH) Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK321

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Glutamine Metabolism Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Mitochondria-Targeted Compound Library

Glucose Metabolism Compound Library

Metabolic Enzyme Compound Library

TCA Cycle Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GSK321

All Isocitrate Dehydrogenase (IDH) Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GSK321 Related Classifications

HY-18948 Related Classifications