VER155008 is an inhibitor of HSP70. It acts by inhibiting reactivation of firefly luciferase.
CAS Number: 1134156-31-2
Molecular Weight: 556.40
Chemical Name: 5'-O-[(4-Cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-adenosine
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
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.
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.
- 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.
- 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.
- 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
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