ASCT2 Inhibitor

Lc-BPE is the highest affinity novel chemical tool for characterizing the role of Alanine-Serine-Cysteine Transporter 2 (ASCT2), a sodium-dependent transporter in a variety of tissues, in cancer and other diseases from this study.

Contributors

Inventor	Institute
Christof Grewer	Binghamton University

Cat. #:	160702
Tool sub type:	Inhibitor
Research Fields:	Genetics
Application:	molecular docking, electrophysiology, transport assays in proteoliposomes and cryo-EM structure determination of ASCT2
Purpose:	Inhibitor

Alternate name:	L-cis hydroxyproline biphenyl ester (Lc-BPE)
Selectivity:	Stereoselective

Primary target:	NA

Shipping conditions:	Dry Ice

References:	doi: https://doi.org/10.1101/2020.05.29.124305

Unfortunately this tool is not currently 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 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

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

151880

AKR1C3 inhibitor CRT0093964 Small Molecule (Tool Compound)

Key Info

Cat. #:	151880
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing

View Tool

153255

Autotaxin Inhibitor (CRT0273750) Small Molecule (Collaborative Toolkit)

Key Info

Cat. #:	153255
Availability:	3-4 weeks

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

ASCT2 Inhibitor

Contributors

Related Tools for Small molecules

Tool enquiry