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

GSK321 是突变异柠檬酸脱氢酶 1 (IDH1) 酶的有效抑制剂。GSK321 对突变的 IDH1 酶具有高抑制性和选择性。GSK321 可用于急性髓性白血病的研究。

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GSK321 Chemical Structure

GSK321 Chemical Structure

CAS No. : 1816331-63-1

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规格 价格 是否有货 数量
1 mg ￥681
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5 mg ￥1500
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10 mg ￥2500
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25 mg ￥5500
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50 mg ￥9500
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Customer Review

Other Forms of GSK321:

GSK321 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Isocitrate Dehydrogenase (IDH) 亚型特异性产品:

查看所有亚型
IDH1 IDH2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].
体外研究
(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].

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

GSK321 相关抗体:

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:
Incubation Time: 7 days
Result: Observed a reproducible and significant decrease in quiescent (G0)-phase cells in R132G IDH1 and R132C IDH1 AML cells.
分子量

501.55

Formula

C28H28FN5O3
CAS 号
性状

固体

颜色

Off-white to light brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

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

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (498.45 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

GSK321 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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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