VER155008


Catalog No. size PriceQuantity
M6451-2 2mg solid $104
M6451-10 10mg solid $401

Description

VER155008 is an inhibitor of HSP70. It acts by inhibiting reactivation of firefly luciferase.

Product information

CAS Number: 1134156-31-2

Molecular Weight: 556.40

Formula: C25H23Cl2N7O4

Synonym:

VER-155008

VER 155008

VER155008

Chemical Name: 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine

Smiles: NC1=NC=NC2=C1N=C(NCC1=CC(Cl)=C(Cl)C=C1)N2[C@@H]1O[C@H](COCC2C=CC(=CC=2)C#N)[C@@H](O)[C@H]1O

InChiKey: ZXGGCBQORXDVTE-UMCMBGNQSA-N

InChi: InChI=1S/C25H23Cl2N7O4/c26-16-6-5-15(7-17(16)27)9-30-25-33-19-22(29)31-12-32-23(19)34(25)24-21(36)20(35)18(38-24)11-37-10-14-3-1-13(8-28)2-4-14/h1-7,12,18,20-21,24,35-36H,9-11H2,(H,30,33)(H2,29,31,32)/t18-,20-,21-,24-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

VER155008 is an inhibitor of Hsc70 and Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, a with a Kd of 0.3 μM for Hsp70, but shows no activities against Hsp90, with an IC50 of >200 μM. VER155008 inhibits the proliferation of a variety of human colon and breast tumor cell lines, such as BT474, MB-468, HCT116 and HT29 cells, with GI50s of 10.4 μM, 14.4 μM, 5.3 μM, and 12.8 μM, respectively. VER155008 (5-40 μM) induces client protein degradation in HCT116 and BT474 carcinoma cells. VER155008 also induces apoptosis in human tumor cell lines. VER155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons. VER155008 (10 μM or 25 μM) inhibits Hsp70 and suppresses the proliferation of LNCaP95 cells. VER155008 also reduces full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7) protein expression.

In Vivo:

VER155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice. VER155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice.

References:

  1. Tian Y, Xu H, Farooq AA, Nie B, Chen X, Su S, Yuan R, Qiao G, Li C, Li X, Liu X, Lin X. Maslinic acid induces autophagy by down-regulating HSPA8 in pancreatic cancer cells. Phytother Res. 2018 Mar 8. doi: 10.1002/ptr.6064. [Epub ahead of print] PubMed PMID: 29516568.
  2. Yang X, Tohda C. Heat Shock Cognate 70 Inhibitor, VER-155008, Reduces Memory Deficits and Axonal Degeneration in a Mouse Model of Alzheimer's Disease. Front Pharmacol. 2018 Jan 30;9:48. doi: 10.3389/fphar.2018.00048. eCollection 2018. PubMed PMID: 29441022; PubMed Central PMCID: PMC5797615.
  3. Morey TM, Winick-Ng W, Seah C, Rylett RJ. Chaperone-Mediated Regulation of Choline Acetyltransferase Protein Stability and Activity by HSC/HSP70, HSP90, and p97/VCP. Front Mol Neurosci. 2017 Dec 12;10:415. doi: 10.3389/fnmol.2017.00415. eCollection 2017. PubMed PMID: 29311808; PubMed Central PMCID: PMC5733026

Products are for research use only. Not for human use.

Payment & Security

PayPal Venmo

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed