SB-3CT

A selective inhibitor of MMP-2 and MMP-9

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5mg

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880.00

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1300.00

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货号: ajci17396
CAS: 292605-14-2
别名: Matrix Metalloproteinase-2/9 Inhibitor IV, MMP-2/MMP-9 Inhibitor IV
分子式: C15H14O3S2
分子量: 306.4
纯度: >98%
溶解度: ≥ 30.6mg/mL in DMSO
储存: Desiccate at -20°C
库存: 现货

Background

SB-3CT is a potent and selective inhibitor of gelatinases with Ki values of 13.9 and 600 nM for MMP-2 and MMP-9, respectively.

Gelatinases A (MMP-2) and B (MMP-9) belong to matrix metalloproteinases family and are involved in tumor metastasis and angiogenesis by hydrolyzing extracellular matrix [1].

SB-3CT is a potent and selective gelatinases inhibitor. SB-3CT was a novel mechanism-based inhibitor that directly bound to the catalytic zinc ion of MMP-2 [1]. SB-3CT inhibited purified mouse MMP-9 with Ki value of 120 nM [2].

In mice bearing T-cell lymphoma L-CI.5s cells, SB-3CT reduced the number of liver metastases in a dose dependent way and reduced the number of tumor colonies by >70% at 50 mg/kg/d. SB-3CT (50 mg/kg/d) also significantly reduced colony size and the number of PCNA positive tumor cells in the livers. These results suggested that SB-3CT effectively inhibited tumor cell extravasation and exhibited an antiproliferative effect. SB-3CT completely inhibited MMP-mediated gelatinolytic activity through the inhibition of both MMP-2 and MMP-9. Also, SB-3CT increased survival [2]. In a transient focal cerebral ischemia mice model, SB-3CT inhibited laminin cleavage mediated by MMP-9 and then rescued neurons from apoptosis [3].

参考文献:
[1].? Kleifeld O, Kotra LP, Gervasi DC, et al. X-ray absorption studies of human matrix metalloproteinase-2 (MMP-2) bound to a highly selective mechanism-based inhibitor. comparison with the latent and active forms of the enzyme. J Biol Chem, 2001, 276(20): 17125-17131.
[2].? Krüger A, Arlt MJ, Gerg M, et al. Antimetastatic activity of a novel mechanism-based gelatinase inhibitor. Cancer Res, 2005, 65(9): 3523-3526.
[3].? Gu Z, Cui J, Brown S, et al. A highly specific inhibitor of matrix metalloproteinase-9 rescues laminin from proteolysis and neurons from apoptosis in transient focal cerebral ischemia. J Neurosci, 2005, 25(27): 6401-6408.