Art. -Nr.: HY-120909

YK5

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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.

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Reinheit: 99.66%
CAS. Nr.: 1268273-23-9
Formel: C₁₈H₂₄N₈O₃S
Molecular Weight:432.50

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

YK5 Chemical Structure

CAS. Nr.: 1268273-23-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

HSP70

HSP90

Alle HSP Isoform-spezifische Produkte anzeigen :

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]

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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 1268273-23-9

Appearance Solid

Molecular Weight 432.50

Formel C₁₈H₂₄N₈O₃S

Color White to off-white

SMILES

C=CC(NC1=NC(SC2=C(OC)N=C(N3CCN(C)CC3)N=C2OC)=NC(N)=C1)=O

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3121 mL

11.5607 mL

23.1214 mL

5 mM

0.4624 mL

2.3121 mL

4.6243 mL

10 mM

0.2312 mL

1.1561 mL

2.3121 mL

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.

Molaritätsrechner

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

Mass Mass

=
Konzentration Konzentration

×
Volumen Volumen

×
Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

×

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

=

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

×

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg

Animal Weight (Per Animal) Animal Weight (Per Animal)
g

Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL

Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

%
+

+
%
Tween-80 + +

%
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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact
MedChemExpress (MCE) .

Tel: 609-228-6898
E-mail: [email protected]
Technical Support: [email protected]

Method for preparing in vivo working solution for animal experiments:
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Saline .

Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)

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)

COA (2659 KB)

Elemental Analysis Report (2659 KB)

HNMR (2659 KB)

CNMR (2659 KB)

RP-HPLC (2659 KB)

NP-HPLC (2659 KB)

MS (2659 KB)

LCMS (2659 KB)

IR (2659 KB)

GC (2659 KB)

OR (2659 KB)

SDS-PAGE (2659 KB)

SEC-HPLC (2659 KB)

Other Report (2659 KB)

Handling Instructions (2659 KB)

Verweise

[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]

View More

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

YK5 Related Classifications

HY-120909 Related Classifications

Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis

HSP Apoptosis

Disease Areas

Cancer Inflammation or Immune System Disease Urogenital Disease Digestive System Disease

Prostate Cancer Urogenital Cancer Digestive System Inflammation

Cancer

Cancer Targeted Therapy Cancer Metabolism and Metastasis

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Keywords

YK5
1268273-23-9
YK 5
YK-5
HSP
Apoptosis
Cytosolic
selective
Hsp70/Hsp90/client protein
SKBr3 cells
cell proliferation
Inhibitor
inhibitor
inhibit

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Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	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

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YK5

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High-Throughput Bioactive Compound Library

Alle HSP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table