SR 7826 - CAS 1219728-20-7
Category: Inhibitor
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Molecular Formula:
C22H21N5O2
Molecular Weight:
387.43
COA:
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Targets:
LIM Kinase(LIMK)
Description:
SR 7826 is a potent and selective LIMK inhibitor (IC50 = 43, 5536 and 6565 nM for LIMK1, ROCKI and ROCKII, respectively). SR 7826 was shown to inhibit cofilin phosphorylation in A7r5 cells and suppress migration and invasion of PC-3 cells in vitro.
Brife Description:
LIMK inhibitor
Purity:
≥98% by HPLC
Synonyms:
SR7826; SR-7826; SR 7826; N-(2-Hydroxyethyl)-N'-[4,5-methyl-7H-pyrrolo[2,3-d]pyrimidine-4-yl)phenyl]-N-phenylurea; 1-(2-hydroxyethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)phenyl]-1-phenylurea
MSDS:
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InChIKey:
WQAGVQVBDHOHRD-UHFFFAOYSA-N
InChI:
InChI=1S/C22H21N5O2/c1-15-13-23-21-19(15)20(24-14-25-21)16-7-9-17(10-8-16)26-22(29)27(11-12-28)18-5-3-2-4-6-18/h2-10,13-14,28H,11-12H2,1H3,(H,26,29)(H,23,24,25)
Canonical SMILES:
CC1=CNC2=NC=NC(=C12)C3=CC=C(C=C3)NC(=O)N(CCO)C4=CC=CC=C4
1.Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3.
Yu Q;Gratzke C;Wang Y;Herlemann A;Sterr CM;Rutz B;Ciotkowska A;Wang X;Strittmatter F;Stief CG;Hennenberg M Br J Pharmacol. 2018 Jun;175(11):2077-2096. doi: 10.1111/bph.14201. Epub 2018 Apr 29.
BACKGROUND AND PURPOSE: ;In men with benign prostatic hyperplasia, increased smooth muscle tone in the prostate may lead to bladder outlet obstruction and subsequent lower urinary tract symptoms. Consequently, medical treatment aims to inhibit prostate smooth muscle contraction. However, the efficacy of the treatment options available is limited, and improved understanding of mechanisms of prostate smooth muscle contraction and identification of new targets for medical intervention are mandatory. Several studies suggest that LIM kinases (LIMKs) promote smooth muscle contraction; however, this has not yet been examined. Here, we studied effects of the LIMK inhibitors on prostate smooth muscle contraction.;EXPERIMENTAL APPROACH: ;Human prostate tissues were obtained from radical prostatectomy. Phosphorylation of cofilin, a LIMK substrate, was examined using a phospho-specific antibody. Smooth muscle contractions were studied in organ bath experiments.;KEY RESULTS: ;Real-time PCR, Western blot and immunofluorescence suggested LIMKs are expressed in smooth muscle cells of prostate tissues. Two different LIMK inhibitors, SR7826 (1 μM) and LIMKi3 (1 μM), inhibited contractions of prostate strips, which were induced by electrical field stimulation, α;1; -adrenoceptor agonists phenylephrine and methoxamine and the TXA;2; analogue, U46619.
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SR 7826 is a potent and selective LIMK inhibitor (IC50 = 43, 5536 and 6565 nM for LIMK1, ROCKI and ROCKII, respectively). SR 7826 was shown to inhibit cofilin p...

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CAS 1219728-20-7 SR 7826

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