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

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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GSK321

GSK321 構造式

CAS 番号 : 1816331-63-1

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 166 在庫あり
Solution
10 mM * 1 mL in DMSO USD 166 在庫あり
Solid
5 mg $150 在庫あり
10 mg $250 在庫あり
25 mg $550 在庫あり
50 mg $950 在庫あり
100 mg $1550 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

Other Forms of GSK321:

GSK321 関連抗体

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Isocitrate Dehydrogenase (IDH) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
IDH1 IDH2

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製品説明

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[1].

IC50 & Target

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

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.

GSK321 関連抗体

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.
体内実験

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 (SSClowCD45low/+) and a relative increase in mature lymphoid and granulocytic/monocytic cells.
分子量

501.55

分子式

C28H28FN5O3
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, protect from light

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

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
10 mM 0.1994 mL 0.9969 mL 1.9938 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)

一般には略語で表示されます：C1V1 = C2V2

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純度とドキュメンテーション

純度: 99.87%

COA (256 KB) RP-HPLC (225 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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