2. Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Apoptosis HSP
  4. Hsp90-Cdc37-IN-3

Hsp90-Cdc37-IN-3 

目录号: HY-144650 纯度: 98.09%
COA 产品使用指南

摩尔计算器

Hsp90-Cdc37-IN-3 (Compound 9) 是一种具有抗癌活性 (anticancer) 的新型 celastrol−imidazole 衍生物。Hsp90-Cdc37-IN-3 通过共价结合抑制 Hsp90−Cdc37，诱导细胞凋亡 (apoptosis)。

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Hsp90-Cdc37-IN-3 Chemical Structure

Hsp90-Cdc37-IN-3 Chemical Structure

CAS No. : 2361009-68-7

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1 mg ￥1580
In-stock
5 mg ￥4400
In-stock
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100 mg   询价  

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Hsp90-Cdc37-IN-3 相关抗体

Top Publications Citing Use of Products

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].

IC50 & Target

Hsp90-Cdc37

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: 9
Antiproliferative activity against human A549 cells expressing Hsp90-Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing Hsp90-Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
A549 IC50
> 100 μM
Compound: 9
Antiproliferative activity against human A549 cells expressing Hsp90 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing Hsp90 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
A549 IC50
> 100 μM
Compound: 9
Antiproliferative activity against human A549 cells expressing Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells expressing Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
A549 IC50
0.54 μM
Compound: 9
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
HCT-116 IC50
0.59 μM
Compound: 9
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
MDA-MB-231 IC50
0.57 μM
Compound: 9
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
U2OS IC50
0.57 μM
Compound: 9
Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
[PMID: 35238566]
体外研究
(In Vitro)

Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values of 0.54, 0.59, 0.57, and 0.57 µM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively[1].
Hsp90-Cdc37-IN-3 (0-5 µM, 12 h) inhibits Hsp90−Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37[1].
Hsp90-Cdc37-IN-3 (0-0.8 µM, 48 h) induces apoptosis significantly in A549 cells[1].
Hsp90-Cdc37-IN-3 (0-0.4 µM, 24 h) arrests the cell cycle in the G0/G1 phase in a dose-dependent manner[1].

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

Hsp90-Cdc37-IN-3 相关抗体:

Western Blot Analysis[1]

Cell Line: A549
Concentration: 1.25, 2.5, and 5 µM
Incubation Time: 12 h
Result: Downregulated the levels of Hsp90−Cdc37 clients (p-Akt and Cdk4) in a dose-dependent manner, and the levels of apoptosis-related proteins (Bax, Bcl-2, cleaved caspase-3, and cleaved PARP) were significantly regulated.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 0.2, 0.4, and 0.8 μM
Incubation Time: 48 h
Result: Induced apoptosis significantly.

Cell Cycle Analysis[1]

Cell Line: A549
Concentration: 0.1, 0.2, and 0.4 μM
Incubation Time: 24 h
Result: Arrested the cell cycle in the G0/G1 phase in a dose-dependent manner.
体内研究
(In Vivo)

Hsp90-Cdc37-IN-3 (Compound 9) (0-1 mg/kg; i.p.; once a day, 21 days) shows strong antitumor activity with no significant toxicity[1].

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

Animal Model: Female BALB/c nude mice at 6 weeks old[1].
Dosage: 0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107 in 100 μL of PBS for each mouse).
Administration: Intraperitoneal injection, once a day, 21 days
Result: Decreased tumor weight and enhanced TIR without show toxicity.
分子量

638.19

Formula

C35H44ClN3O6
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (156.69 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 1.5669 mL 7.8347 mL 15.6693 mL
5 mM 0.3134 mL 1.5669 mL 3.1339 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。-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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (3.92 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

Hsp90-Cdc37-IN-3 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。-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 1.5669 mL 7.8347 mL 15.6693 mL 39.1733 mL
5 mM 0.3134 mL 1.5669 mL 3.1339 mL 7.8347 mL
10 mM 0.1567 mL 0.7835 mL 1.5669 mL 3.9173 mL
15 mM 0.1045 mL 0.5223 mL 1.0446 mL 2.6116 mL
20 mM 0.0783 mL 0.3917 mL 0.7835 mL 1.9587 mL
25 mM 0.0627 mL 0.3134 mL 0.6268 mL 1.5669 mL
30 mM 0.0522 mL 0.2612 mL 0.5223 mL 1.3058 mL
40 mM 0.0392 mL 0.1959 mL 0.3917 mL 0.9793 mL
50 mM 0.0313 mL 0.1567 mL 0.3134 mL 0.7835 mL
60 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6529 mL
80 mM 0.0196 mL 0.0979 mL 0.1959 mL 0.4897 mL
100 mM 0.0157 mL 0.0783 mL 0.1567 mL 0.3917 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:

Hsp90-Cdc37-IN-32361009-68-7ApoptosisHSPHeat shock proteinsA549HTC116U2OSMDA-MB231celastrol?imidazoleInhibitorinhibitorinhibit

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