1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. YK5

YK5 是一种有效的选择性 Hsp70 抑制剂。YK5 在癌细胞中选择性地,紧密地与胞质 Hsp70s 结合。YK5 通过干扰活性致癌 Hsp70/Hsp90/ 配体蛋白复合物的形成而发挥其生物活性。

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YK5 Chemical Structure

YK5 Chemical Structure

CAS No. : 1268273-23-9

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规格 价格 是否有货 数量
1 mg ¥2450
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YK5 is a potent and selective Hsp70 inhibitor. YK5 selectively and tightly binds to the cytosolic Hsp70s in cancer cells. YK5 has biological activity partly by interfering with the formation of active oncogenic Hsp70/Hsp90/client protein complexes[1].

IC50 & Target

HSP70

 

HSP90

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Kasumi 1 IC50
0.9 μM
Compound: 17a
Growth inhibition of human Kasumi-1 cells expressing p-gp/MDR1 after 72 hrs by Alamar Blue assay
Growth inhibition of human Kasumi-1 cells expressing p-gp/MDR1 after 72 hrs by Alamar Blue assay
[PMID: 24548207]
MOLM-13 IC50
1.2 μM
Compound: 17a
Induction of apoptosis in human MOLM13 assessed as caspase 3/7 activation using Z-DEVD-R110 as substrate pretreated for 16 hrs followed by substrate addition by fluorescence-based assay
Induction of apoptosis in human MOLM13 assessed as caspase 3/7 activation using Z-DEVD-R110 as substrate pretreated for 16 hrs followed by substrate addition by fluorescence-based assay
[PMID: 24548207]
SK-BR-3 IC50
> 500 μM
Compound: 17a
Displacement of GM-cy3B from Hsp90 in human SKBR3 cells after 24 hrs by fluorescence polarization assay
Displacement of GM-cy3B from Hsp90 in human SKBR3 cells after 24 hrs by fluorescence polarization assay
[PMID: 24548207]
SK-BR-3 IC50
0.7 μM
Compound: 17a
Inhibition of Hsp70 in human SKBR3 cells assessed as HER2 protein degradation by Western blotting analysis
Inhibition of Hsp70 in human SKBR3 cells assessed as HER2 protein degradation by Western blotting analysis
[PMID: 24548207]
SK-BR-3 IC50
0.8 μM
Compound: 17a
Growth inhibition of human SKBR3 cells after 72 hrs by Alamar Blue assay
Growth inhibition of human SKBR3 cells after 72 hrs by Alamar Blue assay
[PMID: 24548207]
SK-BR-3 IC50
1.7 μM
Compound: 17a
Inhibition of Hsp70 in human SKBR3 cells assessed as RAF1 protein degradation by Western blotting analysis
Inhibition of Hsp70 in human SKBR3 cells assessed as RAF1 protein degradation by Western blotting analysis
[PMID: 24548207]
SK-BR-3 IC50
2 μM
Compound: 17a
Induction of apoptosis in human SKBR3 cells assessed as PARP cleavage by Western blotting analysis
Induction of apoptosis in human SKBR3 cells assessed as PARP cleavage by Western blotting analysis
[PMID: 24548207]
体外研究
(In Vitro)

YK5 shows selectively and tightly binds to the cytosolic Hsp70s[1].
YK5 (0.5, 1, 5 µM; 72 h) degrades the expression of Hsp90/Hsp70-onco-client proteins and also leads to the inhibition of cell proliferation in SKBr3 cells[1].
YK5 (0.5, 1, 5 µM; 24 h) induces the degradation of HER2, Raf-1, Akt kinases, and also induces apoptosis in SKBr3 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: SKBr3 cells
Concentration: 0.5, 1, 5 µM
Incubation Time: 72 h
Result: Degraded the expression of Hsp90/Hsp70-onco-client proteins and also led to the inhibition of cell proliferation in SKBr3 cells.

Western Blot Analysis[1]

Cell Line: SKBr3 cells
Concentration: 0.5, 1, 5 µM
Incubation Time: 24 h
Result: Induced the degradation of HER2, Raf-1, Akt kinases, and also induced apoptosis in SKBr3 cells.
分子量

432.50

Formula

C18H24N8O3S

CAS 号
性状

固体

颜色

White to off-white

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 (231.21 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 2.3121 mL 11.5607 mL 23.1214 mL
5 mM 0.4624 mL 2.3121 mL 4.6243 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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.78 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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
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

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 2.3121 mL 11.5607 mL 23.1214 mL 57.8035 mL
5 mM 0.4624 mL 2.3121 mL 4.6243 mL 11.5607 mL
10 mM 0.2312 mL 1.1561 mL 2.3121 mL 5.7803 mL
15 mM 0.1541 mL 0.7707 mL 1.5414 mL 3.8536 mL
20 mM 0.1156 mL 0.5780 mL 1.1561 mL 2.8902 mL
25 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3121 mL
30 mM 0.0771 mL 0.3854 mL 0.7707 mL 1.9268 mL
40 mM 0.0578 mL 0.2890 mL 0.5780 mL 1.4451 mL
50 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9634 mL
80 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7225 mL
100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 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:
YK5
目录号:
HY-120909
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