SGK3-PROTAC1 small molecule (tool compound)

Contributors

Inventor	Institute
Alessio Ciulli	University of Dundee

Cat. #:	158378
Research Fields:	Drug development

Shipping conditions:	Dry Ice

References:	Tovell et al. 2019. ACS Chem Biol. 14(9):2024-2034. PMID: 31461270.

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 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

151834

Antitumoral Quinol1h Small Molecule (Tool Compound)

Key Info

Cat. #:	151834
Sub-type:	Antitumoral
Availability:	Please enquire for quantities and pricing
Application:	Antitumor activity observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM), and in breast cancer cell lines. Potent inhibitory effect in NCI 60 cells (GI50 =16 nM and LC50 = 2.24 ÂľM).

View Tool

151839

Antitumoral Phortress Small Molecule (Tool Compound)

Key Info

Cat. #:	151839
Sub-type:	Antitumoral
Availability:	Please enquire for quantities and pricing
Application:	Active against breast, ovarian and renal carcinomas. Taken up into sensitive cells followed by aryl hydrocarbon receptor binding and translocation into the nucleus. Requires metabolic activation by cytochrome P450 to generate cytotoxic species. Induces expression of CYP1A1 and generates adducts in the DNA of sensitive MCF7 and IGROV-1 cells.

View Tool

151889

DNA-PK inhibitor NU7441 Small Molecule (Tool Compound)

Key Info

Cat. #:	151889
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. NU7441 increases the persistence of ÎłH2AX foci after ionizing radiationâinduced or etoposide-induced DNA damage. NU7441 (0.5 ÎźM or 1 ÎźM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. NU7441 causes persistence of d…

View Tool

152544

Protein Kinase D inhibitor CRT5 (CRT0066051) Small Molecule (Tool Compound)

Key Info

Cat. #:	152544
Sub-type:	Inhibitor
Availability:	Please enquire for quantities and pricing
Application:	PLEASE NOTE THAT THIS COMPOUND IS TOXIC IN VIVO. CRT5 blocks phosphorylation of PKD1 on Ser916 and PKD2 on Ser876, but does not affect PKC-dependent PKD phosphorylation or PKD autophosphorylation.1 It also decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis.

View Tool

By Category

By Cancer Type

More

SGK3-PROTAC1 small molecule (tool compound)

Contributors

Related Tools for Small molecules

Tool enquiry