SB-3CT

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Chemical Structure| 292605-14-2 同义名 : Matrix Metalloproteinase-2/9 Inhibitor IV; MMP-2/MMP-9 Inhibitor IV
CAS号 : 292605-14-2
货号 : A332833
分子式 : C15H14O3S2
纯度 : 99%+
分子量 : 306.4
MDL号 : MFCD09836266
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(163.19 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • MMP

    MMP-9, Ki:600 nM

    MMP-2, Ki:13.9 nM
描述 SB-3CT is a selective MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively, with much less potency to the other MMPs with Ki values of 206μM, 15μM and 96μM for MMP-1, 3 and 7, respectively[1]. SB-3CT also works as an inhibitor of gelatinase, a member of MMP family. Daily intraperitoneal administration of SB-3CT at dose of 50 mg/kg potently inhibited the liver metastasis and increased survival in an aggressive mouse model of T-cell lymphoma[2]. Treatment with 0.1 or 1μM SB-3CT inhibited capillary-like tubule formation by BMEC-1 cells and the ability of BMEC-1 cells to invade filters coated with Matrigel, but not the cell proliferation up to 10μM. Intraperitoneal injection with SB-3CT at dose of 50 mg/kg potently inhibited intraosseous tumor growth, bone degradation, and intratumoral angiogenesis of human PC3 cells within the marrow of human fetal femur fragments previously implanted in SCID mice[3]. SB-3CT is blood-brain barrier permeable as it can be rapidly absorbed and readily distributed to the brain, and also shows neuroprotective effect[4].
作用机制 SB-3CT directly binds the catalytic zinc ion of MMP-2.[5]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.26mL

0.65mL

0.33mL

16.32mL

3.26mL

1.63mL

32.64mL

6.53mL

3.26mL
参考文献

[1]Stephen Brown, M. Margarida Bernardo, et al. Potent and Selective Mechanism-Based Inhibition of Gelatinases. J. Am. Chem. Soc., 2000, 122 (28), pp 6799–6800.

[2]Krüger A, Arlt MJ, et al. Antimetastatic activity of a novel mechanism-based gelatinase inhibitor. Cancer Res. 2005 May 1;65(9):3523-6.

[3]Bonfil RD, Sabbota A, et al. Inhibition of human prostate cancer growth, osteolysis and angiogenesis in a bone metastasis model by a novel mechanism-based selective gelatinase inhibitor. Int J Cancer. 2006 Jun 1;118(11):2721-6.

[4]Gooyit M, Suckow MA, et al. Selective gelatinase inhibitor neuroprotective agents cross the blood-brain barrier. ACS Chem Neurosci. 2012 Oct 17;3(10):730-6.

[5]Kleifeld O, Kotra LP, 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 May 18;276(20):17125-31. Epub 2001 Jan 30.