Cat. No. 2907
Chemical Name: (Z)-1,3-Dihydro-3-(1H-imidazol-4-yl
Biological ActivityPotent, selective cdk2 inhibitor (IC50 values are 0.022, 0.04, 0.2, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G1 and G2-M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Gao et al (2006) The three-substituted indolinone cyclin-dependent kinase 2 inhibitor 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one (SU9516) kills human leukemia cells via down-regulation of Mcl-1 through a transcriptional mechanism. Mol.Pharmacol. 70 645. PMID: 16672643.
Yu et al (2002) SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells. Biochem.Pharmacol. 64 1091. PMID: 12234612.
Lane et al (2001) A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells. Cancer Res. 61 6170. PMID: 11507069.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for SU 9516 include:
Shi et al (2014) The FGF-1-specific single-chain antibody scFv1C9 effectively inhibits breast cancer tumour growth and metastasis. J Cell Mol Med 18 2061. PMID: 25124967.
Do you know of a great paper that uses SU 9516 from Tocris? If so please let us know.
View Related Products by Product Action
Keywords: SU 9516, supplier, Potent, cdk2, inhibitors, Transcriptionally, downregulates, Mcl-1, proapoptotic, Cyclin-Dependent, Protein, Kinases, Bcl-2, Family, SU9516, Tocris Bioscience, Cyclin-Dependent Protein Kinase Inhibitor products
Find multiple products by catalog number
New Products in this Area
Selective ATP competitive SphK1 and 2 inhibitor; cell permeableAkti-1/2
Potent and selective dual Akt1 and 2 inhibitorVX 680
High affinity and selective Aurora kinase inhibitorImatinib mesylate
Potent and selective v-Abl tyrosine kinase inhibitor; also inhibits PDGFR and c-kitTGX 221
Potent and selective PI 3-kinase β inhibitorPF 543 hydrochloride
Potent and selective SphK1 inhibitorJX 06
Potent and selective PDK1/2/3 inhibitorMRT 68601 hydrochloride
Potent TBK1 inhibitorAzoramide
Unfolded protein response (UPR) modulatorLCB 03-0110 dihydrochloride
Potent c-SRC kinase inhibitor; also inhibits DDR2, BTK and SykCCT 241533 dihydrochloride
Potent Chk2 inhibitorIRAK1/4 Inhibitor I
IRAK4 and IRAK1 inhibitorCentrinone
High affinity and selective PLK4 inhibitorAZD 3147
Potent and selective dual mTORC1 and 2 inhibitor; orally bioavailableTilfrinib
Potent and selective breast tumor kinase (Brk) inhibitorProstratin
PKC activator; also NF-κB activator
July 29 - 31, 2016