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HomeProduct name listSU 9516

SU 9516

SU 9516 Structural

What is SU 9516?

The Uses of SU 9516

SU 9516 is a 3-substituted indolinone CDK inhibitor with potent and selective inhibition towards cyclin-dependant kinases.

What are the applications of Application

SU 9516 is a cell permeable, potent, selective and ATP-competitive inhibitor

Definition

ChEBI: 3-(1H-imidazol-5-ylmethylidene)-5-methoxy-1H-indol-2-one is a member of indoles.

Biological Activity

Potent, selective cdk2 inhibitor (IC 50 values are 0.022, 0.04, >10, >10, 18 and >100 μ M for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively). Inhibits pRb phosphorylation causing enhanced pRB/E2F complex formation and induces G 1 and G 2 -M cell cycle arrest. Transcriptionally downregulates Mcl-1 and has antiproliferative, cytostatic and pro-apoptotic effects in vitro .

References

[1]. lane me, yu b, rice a, et al. a novel cdk2-selective inhibitor, su9516, induces apoptosis in colon carcinoma cells. cancer res, 2001, 61(16): 6170-6177.
[2]. yu b, lane me, wadler s. su9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight e2f complexes in human colon carcinoma cells. biochem pharmacol, 2002, 64(7): 1091-1100.
[3]. gao n, kramer l, rahmani m, et al. 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, 2006, 70(2): 645-655.

Properties of SU 9516

storage temp.  Store at +4°C
solubility  DMSO: ~17 mg/mL
form  crystalline
color  brown

Safety information for SU 9516

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for SU 9516

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