An allosteric antagonist of CXCR1 and CXCR2
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SCH 527123

Item No. 27800

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-hydroxy-N,N-dimethyl-3-[[2-[[(1R)-1-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]-benzamide
CAS Number
473727-83-2
Synonyms
  • MK-7123
Molecular Formula
C21H23N3O5
Formula Weight
397.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleMethanol: slightly soluble
λmax
215, 296, 347 nm
SMILES
OC1=C(C(N(C)C)=O)C=CC=C1NC(C2=O)=C(N[C@@H](C3=CC=C(C)O3)CC)C2=O
InChi Code
InChI=1S/C21H23N3O5/c1-5-13(15-10-9-11(2)29-15)22-16-17(20(27)19(16)26)23-14-8-6-7-12(18(14)25)21(28)24(3)4/h6-10,13,22-23,25H,5H2,1-4H3/t13-/m1/s1
InChi Key
RXIUEIPPLAFSDF-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    SCH 527123 is an allosteric antagonist of C-X-C chemokine receptor type 1 (CXCR1; IC50 = 43 nM in Ba/F3 cells) and CXCR2 (IC50 = 0.97 nM in HTS cells).1 It inhibits calcium flux induced by CXCL8 in Ba/F3 cells expressing human recombinant CXCR1 or CXCR2. SCH 527123 (3 nM) inhibits CXCL8-induced chemotaxis of Ba/F3 cells expressing human recombinant CXCR2 and CXCL1-induced chemotaxis of isolated human polymorphonuclear cells (PMNs). It also inhibits LPS-induced neutrophil infiltration into the lung (ED50 = 1.8 mg/kg) and increases mucin levels in bronchoalveolar lavage fluid (BALF) in a rat model of airway inflammation.2 SCH 527123 inhibits proliferation of wild-type (IC50s = 28.95 and 18.78 µM, respectively) and IL-8 overexpressing HCT116 and Caco-2 cells (IC50s = 39.45 and 25.45 µM, respectively).3 It reduces tumor growth in an HCT116 mouse xenograft model when administered at a dose of 50 mg/kg per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gonsiorek, W., Fan, X., Hesk, D., et al. Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist. J. Pharmacol. Exp. Ther. 322(2), 477-485 (2007).

    2. Chapman, R.W., Minnicozzi, M., Celly, C.S., et al. A novel, orally active CXCR1/2 receptor antagonist, Sch527123, inhibits neutrophil recruitment, mucus production, and goblet cell hyperplasia in animal models of pulmonary inflammation. J. Pharmacol. Exp. Ther. 322(2), 486-493 (2007).

    3. Ning, Y., Labonte, M.J., Zhang, W., et al. The CXCR2 antagonist, SCH-527123, shows antitumor activity and sensitizes cells to oxaliplatin in preclinical colon cancer models. Mol. Cancer Ther. 11(6), 1353-1364 (2012).