SLx-2119

  • CAT Number: I005432
  • CAS Number: 911417-87-3
  • Molecular Formula: C26H24N6O2
  • Molecular Weight: 452.5
  • Purity: ≥95%
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<p>
SLx-2119(KD-025, cas 911417-87-3) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; &gt; 200 fold selecivity over ROCK1(IC50 =24 uM).&nbsp;
</p>
<p>
In humans, oral KD 025 diminishes STAT3 phosphorylation and pro-inflammatory cytokine production in CD4+ T cells while up-regulating phosphorylation of STAT5 in regulatory T cells, altering the immune response.
</p>

Catalog Number I005432
CAS Number 911417-87-3
Molecular Formula

C26H24N6O2

Purity 95%
Target ROCK
Solubility DMSO: ≥ 29 mg/mL
Storage Store at -20°C
IC50 105 nM(ROCK2); 24 μM(ROCK1)
InChI InChI=1S/C26H24N6O2/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31)
InChIKey GKHIVNAUVKXIIY-UHFFFAOYSA-N
SMILES O=C(NC(C)C)COC1=CC=CC(C2=NC3=CC=CC=C3C(NC4=CC(C=NN5)=C5C=C4)=N2)=C1
Reference

1: De Silva TM, Kinzenbaw DA, Modrick ML, Reinhardt LD, Faraci FM. Heterogeneous
Impact of ROCK2 on Carotid and Cerebrovascular Function. Hypertension. 2016
Sep;68(3):809-17. doi: 10.1161/HYPERTENSIONAHA.116.07430. Epub 2016 Jul 18.
PubMed PMID: 27432870; PubMed Central PMCID: PMC4982851.

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2: Lee JH, Zheng Y, von Bornstadt D, Wei Y, Balcioglu A, Daneshmand A, Yalcin N,
Yu E, Herisson F, Atalay YB, Kim MH, Ahn YJ, Balkaya M, Sweetnam P, Schueller O,
Poyurovsky MV, Kim HH, Lo EH, Furie KL, Ayata C. Selective ROCK2 Inhibition In
Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. PubMed
PMID: 24466563; PubMed Central PMCID: PMC3900310.

<br>
3: Boerma M, Fu Q, Wang J, Loose DS, Bartolozzi A, Ellis JL, McGonigle S,
Paradise E, Sweetnam P, Fink LM, Vozenin-Brotons MC, Hauer-Jensen M. Comparative
gene expression profiling in three primary human cell lines after treatment with
a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul Fibrinolysis. 2008
Oct;19(7):709-18. doi: 10.1097/MBC.0b013e32830b2891. PubMed PMID: 18832915;
PubMed Central PMCID: PMC2713681.

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