1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. JG-231

JG-231 是一种热休克蛋白 70 (Hsp70) 的变构抑制剂。JG-231 可以抑制 Hsp70BAG 家族蛋白的结合,其中抑制 Hsp70BAG1Ki 为 0.11μM。JG-231 能抑制肿瘤细胞的增殖,并诱导细胞凋亡 (apoptosis)。JG-231 具有抗肿瘤的活性。

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JG-231 Chemical Structure

JG-231 Chemical Structure

CAS No. : 1627126-59-3

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4906
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1 mg ¥1300
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5 mg ¥3600
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10 mg ¥4700
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a Ki of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity[1][2].

IC50 & Target[2]

HSP70

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
0.12 μM
Compound: 42; JG-231
Antiproliferative activity against human MCF7 cells by MTT assay
Antiproliferative activity against human MCF7 cells by MTT assay
[PMID: 29953808]
MDA-MB-231 IC50
0.25 μM
Compound: 42; JG-231
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
[PMID: 29953808]
MEF IC50
2.5 μM
Compound: 42; JG-231
Antiproliferative activity against MEF cells by MTT assay
Antiproliferative activity against MEF cells by MTT assay
[PMID: 29953808]
体外研究
(In Vitro)

JG-231 (0.31-5 μM;4-10 天) 在三维培养的 TT 和 MZ-CRC-1 细胞中,以剂量和时间依赖方式抑制细胞球生长[1]
JG-231 (0-10 μM;12-24 小时) 在 MCF-7 细胞中,可破坏 Hsp70 与 BAG3 的相互作用,影响与 Hsp70 相关的信号通路,并诱导细胞凋亡[2]

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

Western Blot Analysis[2]

Cell Line: MCF-7
Concentration: 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 24 h
Result: Reduced the levels of Akt, c-Raf , CDK4, IAP-1 and HuR.
Did not change the levels of Hsp72 and Hsp90.
体内研究
(In Vivo)

JG-231 (4 mg/kg;腹腔注射;一周三次;4 周) 在乳腺癌异种移植小鼠模型中具有抗肿瘤的作用[2]
在小鼠中的药代动力学分析[1]

Route Dose (mg/kg) Cmax (nM) Tmax (h) t1/2 (h) AUC0-∞ (nM·h)
i.p. 5 159 2 21.6 3401

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

Animal Model: Four-week-old female athymic mice (Charles River) bearing xenografted MDA-MB-231 cells[2]
Dosage: 4 mg/kg
Administration: Intraperitoneal injection (i.p.); 3 days a week for 4 weeks
Result: Inhibited tumor growth.
Did not significantly change the weight of mice.
分子量

619.47

Formula

C22H18BrCl2N3OS4

CAS 号
性状

固体

颜色

Orange to reddish brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 2 mg/mL (3.23 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 1.6143 mL 8.0714 mL 16.1428 mL
5 mM --- --- ---
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 (sealed storage, away from moisture and 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

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

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 (sealed storage, away from moisture and 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 1.6143 mL 8.0714 mL 16.1428 mL 40.3571 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.

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产品名称:
JG-231
目录号:
HY-124611
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