Cat. No.: HY-15984

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VER-50589

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VER-50589 is a Hsp90 inhibitor, with an IC₅₀ of 21 nM and a K_d of 4.5 nM.

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Pureté: 99.76%
CAS No.: 747413-08-7
Formule: C₁₉H₁₇ClN₂O₅
Masse moléculaire:388.80

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

VER-50589 Chemical Structure

CAS No.: 747413-08-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

VER-50589 is a Hsp90 inhibitor, with an IC₅₀ of 21 nM and a K_d of 4.5 nM.

IC₅₀ & Target^[1]

HSP90

21 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform HSP :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	223.48 nM Compound: VER-50589	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	[PMID: 37315698]
DU-145	GI₅₀	0.23 μM Compound: 33	Growth inhibition of human DU145 cells by SRB assay Growth inhibition of human DU145 cells by SRB assay	[PMID: 18020435]
ES-2	IC₅₀	50.4 nM Compound: VER-50589	Cytotoxicity against human ES2 cells by MTT assay Cytotoxicity against human ES2 cells by MTT assay	[PMID: 37315698]
HCT-116	GI₅₀	0.12 μM Compound: 33	Growth inhibition of human HCT116 cells after 24 hrs by SRB assay Growth inhibition of human HCT116 cells after 24 hrs by SRB assay	[PMID: 18020435]
HeLa	IC₅₀	219 nM Compound: VER-50589	Cytotoxicity against human HeLa cells by MTT assay Cytotoxicity against human HeLa cells by MTT assay	[PMID: 37315698]
MCF7	IC₅₀	69.57 nM Compound: VER-50589	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 37315698]
MDA-MB-231	IC₅₀	75.84 nM Compound: VER-50589	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	[PMID: 37315698]
PC-3M	GI₅₀	0.22 μM Compound: 33	Growth inhibition of human PC3M cells by SRB assay Growth inhibition of human PC3M cells by SRB assay	[PMID: 18020435]
SF-268	GI₅₀	0.034 μM Compound: 33	Growth inhibition of human SF268 cells by SRB assay Growth inhibition of human SF268 cells by SRB assay	[PMID: 18020435]
SK-MEL-28	GI₅₀	0.045 μM Compound: 33	Growth inhibition of human SKMel28 cells by SRB assay Growth inhibition of human SKMel28 cells by SRB assay	[PMID: 18020435]
U-87MG ATCC	GI₅₀	0.028 μM Compound: 33	Growth inhibition of human U87MG cells by SRB assay Growth inhibition of human U87MG cells by SRB assay	[PMID: 18020435]

In Vitro

VER-50589 is a Hsp90 inhibitor, with an IC₅₀ of 21 nM and a K_d of 4.5 nM. VER-50589 inhibits intrinsic ATPase of full-length recombinant yeast Hsp90, with an IC₅₀ of 143 ± 23 nM in the presence of 400 μM ATP. VER-50589 shows antiproliferative activities against various human cancer cells, with the lowest GI₅₀ of 32.7 ± 0.2 nM for CH1 human ovarian cells, and mean GI₅₀ of 78 ± 15 nM. VER-50589 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI₅₀ value of 19 ± 2.4 nM, and shows higher GI₅₀s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. Furthermore, VER-50589 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression. VER-50589 also causes G1 and G2-M block (115 or 575 nM) and induces cytostasis in HCT116 colon cancer cells. In addition, VER-50589 causes great uptake in HCT116 cells^[1].

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

In Vivo

VER-50589 (4 mg/kg, i.p.) exerts a complete HSP90 inhibition in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors. VER-50589 (100 mg/kg, i.p.) shows reduced tumor volume and tumor weights in the HCT116 colon carcinoma xenografts compared to the control mice group^[1].

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

Chemical Information

CAS No. 747413-08-7
Appearance Solid
Masse moléculaire 388.80
Formule C₁₉H₁₇ClN₂O₅
Color White to off-white
SMILES

O=C(C1=NOC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)C=C3)NCC
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Theranostics

Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]

2019 Aug 12;9(20):5769-5783. PMID: 31534518

Solvant et solubilité

In Vitro:

DMSO : ≥ 48 mg/mL (123.46 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.5720 mL

12.8601 mL

25.7202 mL

5 mM

0.5144 mL

2.5720 mL

5.1440 mL

10 mM

0.2572 mL

1.2860 mL

2.5720 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Protocole

Cell Assay^[1]

HCT116 and HT29 human colon cancer cells are seeded and left to attach overnight. Vehicle control or compound (VER-50589) is added for 1, 4, and 24 h. Attached cells are collected and counted by hemacytometer. Incubation medium (1 mL) and cell pellets are frozen at −80°C until mass spectrometry analysis^[1].

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

Animal Administration^[1]

HCT116 cells (2-5 million cells per site) are injected s.c. in the flanks of 6- to 8-week-old female NCr athymic mice. Dosing commenced when tumors are well established (∼5-6 mm diameter). For combined therapy and pharmacokinetic and pharmacodynamic studies, mice bearing HCT116 xenografts are administered 100 mg/kg VER-50589 i.p. per day for 9 days. Tumor volumes are calculated. On study termination, blood samples are taken, and plasma is separated and stored −80°C. Tumors are excised, weighed, and snap frozen at −80°C^[1].

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[1]. Sharp SY, et al. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther. 2007 Apr;6(4):1198-211. [Content Brief]

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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5720 mL	12.8601 mL	25.7202 mL	64.3004 mL
	5 mM	0.5144 mL	2.5720 mL	5.1440 mL	12.8601 mL
	10 mM	0.2572 mL	1.2860 mL	2.5720 mL	6.4300 mL
	15 mM	0.1715 mL	0.8573 mL	1.7147 mL	4.2867 mL
	20 mM	0.1286 mL	0.6430 mL	1.2860 mL	3.2150 mL
	25 mM	0.1029 mL	0.5144 mL	1.0288 mL	2.5720 mL
	30 mM	0.0857 mL	0.4287 mL	0.8573 mL	2.1433 mL
	40 mM	0.0643 mL	0.3215 mL	0.6430 mL	1.6075 mL
	50 mM	0.0514 mL	0.2572 mL	0.5144 mL	1.2860 mL
	60 mM	0.0429 mL	0.2143 mL	0.4287 mL	1.0717 mL
	80 mM	0.0322 mL	0.1608 mL	0.3215 mL	0.8038 mL
	100 mM	0.0257 mL	0.1286 mL	0.2572 mL	0.6430 mL

Keywords

VER-50589

1 Cited Publications

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VER-50589

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Extracellular Vesicles (EVs) Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VER-50589

Voir tous les produits spécifiques à Isoform HSP

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

VER-50589

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Extracellular Vesicles (EVs) Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) VER-50589

Voir tous les produits spécifiques à Isoform HSP

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

VER-50589 Related Classifications

HY-15984 Related Classifications