YK5
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 1268273-23-9
- Formula: C18H24N8O3S
- Molecular Weight:432.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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HSP70 |
HSP90 |
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Cell Line
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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] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKBr3 cells
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Concentration:0.5, 1, 5 µM
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Incubation Time:72 h
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Result:Degraded the expression of Hsp90/Hsp70-onco-client proteins and also led to the inhibition of cell proliferation in SKBr3 cells.
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Cell Line:SKBr3 cells
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Concentration:0.5, 1, 5 µM
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Incubation Time:24 h
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Result:Induced the degradation of HER2, Raf-1, Akt kinases, and also induced apoptosis in SKBr3 cells.
Chemical Information
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CAS No. 1268273-23-9
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Appearance Solid
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Molecular Weight 432.50
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Formula C18H24N8O3S
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Color White to off-white
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SMILES
C=CC(NC1=NC(SC2=C(OC)N=C(N3CCN(C)CC3)N=C2OC)=NC(N)=C1)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (231.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Rodina A, et al. Identification of an allosteric pocket on human hsp70 reveals a mode of inhibition of this therapeutically important protein. Chem Biol. 2013 Dec 19;20(12):1469-80. [Content Brief]
[2]. Taldone T, Kang Y, Patel HJ, et al. Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014;57(4):1208-1224. [Content Brief]
[3]. Kang Y, Taldone T, Patel HJ, et al. Heat shock protein 70 inhibitors. 1. 2,5'-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014;57(4):1188-1207. [Content Brief]
[4]. Hu YT, Lin YW, Guo SY, et al. Disrupting the protein-protein interaction network of Hsp72 inhibits adipogenic differentiation and lipid synthesis in adipocytes. Cell Signal. 2024;124:111431. [Content Brief]
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. 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 | 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 |