VH101-OH small molecule (tool compound)

Hydroxyl functionalized VHL ligand

Contributors

Inventor	Institute
Alessio Ciulli	University of Dundee

Cat. #:	158374
Research Fields:	Drug development

Product description:	Hydroxyl functionalized VHL ligand
Molecular weight:	532.63

References:	Farnaby et al. 2019. Nat Chem Biol. 15(7):672-680. PMID: 31178587. Girardini et al. 2019. Bioorg Med Chem. 27(12):2466-2479. PMID: 30826187. Zoppi et al. 2019. J Med Chem. 62(2):699-726. PMID: 30540463. Maniaci et al. 2017. Nat Commun. 8(1):830. PMID: 29018234.

Unfortunately this tool is not available through our online checkout process. Please contact our team directly to obtain further information on accessing this tool.

Enquire about this Tool

If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.

Request a license

Get technical support

New to CancerTools?

We are a trusted, non-profit platform for cancer research products, part of Cancer Research UK – by sourcing your cancer research tools from us you help fund future cancer research.

Find out more

Related Tools for Small molecules

Cat. #

Tool Name

151712

CDK7 inhibitor BS-181 Small Molecule (Tool Compound)

Key Info

Cat. #:	151712
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	BS-181 is stable in vivo with a plasma elimination half-life in mice of 405 minutes after i.p. administration of 10 mg/kg. BS-181 inhibits the growth of MCF-7 xenografts in the nude mice model in a dose-dependent manner, with 25% and 50% reduction in tumor growth after 2 weeks of treatment at 10 mg/kg/day and 20 mg/kg/day, respectively without apparent toxicity. BS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 ÎźM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 ÎźM, and only shows inhibition for several kinases from other classes at high concentrations (>10 ÎźM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5-37 ÎźM. In MCF-7 cells, BS-181 inhibits the phosphorylation of the CDK7 substrate RNA polymerase II COOH-terminal domain (CTD), and promotes cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines.

View Tool

151831

Protein Kinase D inhibitor CRT0066101 Small Molecule (Tool Compound)

Key Info

Cat. #:	151831
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	In Panc-1 subcutaneous xenograft model, orally administration of CRT0066101 at the dosage of 80 mg/kg/d for 24 days significantly suppressed pancreatic cancer growth. Moreover, when CRT0066101 reached its peak concentration (12 Îźmol/L) in tumor model, the expression of activated PKD1/2 in the treated tumor explants was substantially decreased. It was concluded that CRT0066101 given orally at 80 mg/kg/d for 21 days in Panc-1 orthotropic model suppressed tumor growth potently in vivo. Clinical…

View Tool

151843

AKR1C3 inhibitor CRT0036521 Small Molecule (Tool Compound)

Key Info

Cat. #:	151843
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	The compounds showed good cellular potency, as measured by inhibition of AKR1C3 metabolism of a known dinitrobenzamide substrate, with a broad rank order between enzymic and cellular activity, but amide analogues were more effective than predicted by the cellular assay. displays potency in a cellular assay, blocking the ability of AKR1C3 to metabolize a proven substrate.

View Tool

152789

Glucose-6-phosphate Dehydrogenase inhibitor G6PD Small Molecule (Collaborative Toolkit)

Key Info

Cat. #:	152789
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing

View Tool

153334

HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)

Key Info

Cat. #:	153334
Sub-type:	Fluorescent Probe
Availability:	Please enquire for quantities and pricing
Application:	2-FAM-InsP5 [2-FAM-Ins(1,3,4,5,6)P5] is a fluorescent derivative of Ins(1,3,4,5,6)P5. 2-FAM-InsP5 activates the HDAC3:SMRT complex in a similar manner to the natural ligand, Ins(1,4,5,6)P4. The binding constant (Kd) for binding of 2-FAM-InsP5 to HDAC3:SMRT measured by a direct binding assay, 0.3 Âą 0.01 ÎźM, was approximately 10-fold lower than the Kdapp for activation of the catalytic activity of HDAC3:SMRT by Ins(…

View Tool

By Category

By Cancer Type

More

VH101-OH small molecule (tool compound)

Contributors

Related Tools for Small molecules

Tool enquiry