| Cat. No. |
Product Name |
CAS No. |
Information |
| H9048 |
RF036
|
2108097-04-5 |
RF036 is a potent matrix metalloproteinase 13 (MMP-13) inhibitor with IC50 values of 2.7 nM. |
| H8774 |
Aldumastat
|
1957278-93-1 |
Aldumastat is a novel ADAMTS inhibitor, for the treatment of osteoarthritis and their preparation. |
| H5265 |
MMP13-IN-31f
|
935759-55-0 |
MMP13-IN-31f is a highly potent, selective, orally bioavailable MMP-13 inhibitor with IC50 of 0.036 nM; exhibits 5,000-fold selectivity for MMP-13 over MMP-2, >1,500-fold selectivity over MMP-10, and >27,000-fold selectivity over MMP-1, 3, 7, 8, 9, 14, and TACE; prevents IL-1/OSM induced in vitro degradation of BNC (70.8% inhibition of cartilage degradation at 1 ¦ÌM).
|
| H5254 |
CGS 27023A
|
161314-82-5 |
CGS 27023A (MMI 270) is a potent, orally active MMP inhibitor with Ki of 8-43 nM for MMP1/2/3/9; shows growth-inhibitory effects in breast carcinoma, prostate, bladder, colon, lung adenocarcinoma, glioblastoma, and ovarian carcinoma cell line;.protects the cartilage proteoglycan matrix in a partial meniscectomy model of osteoarthritis in rabbits. |
| H5277 |
UK 356618
|
230961-08-7 |
UK 356618 (UK356618) is a potent and selective MMP3 inhibitor with IC50 of 5.9 nM, shows >140-fold less potent against MMP-1 (IC50=51000 nM), MMP-2 (IC50=1790 nM), MMP-9 (IC50=840 nM) and MMP-14 (IC50=1900 nM); significantly reduces hemorrhagic transformation and improves functional outcomes in hyperglycemic stroke. |
| H5276 |
TAPI-2
|
187034-31-7 |
A broad-spectrum inhibitor of TNF-α converting enzyme (TACE;ADAM17), ADAMs, and other MMPs, inhibits ADAM8, 10, 12, and TACE with Ki values of 10, 3, 100, and 0.12 uM, respectively; inhibits PMA-induced shedding of cell surface proteins, such as TGF-α, β amyloid precursor protein, L-selectin, and IL-6 receptor α subunit in CHO cells with IC50 of 10 uM; reverses the malignant phenotype in a breast cancer cell line by preventing mobilization of the growth factors TGF-α and amphiregulin. |
| H5275 |
Tanomastat
|
179545-77-8 |
Tanomastat (BAY 129566) is a potent,orally available, non-peptidic inhibitor of MMP-2, MMP-3 and MMP-9 with 11, 143 and 301 nM, respectively; inhibits extracellular matrix degradation and potentially inhibiting angiogenesis, tumor growth and invasion, and metastasis both in vitro and in vivo. |
| H5274 |
SB-3CT
|
292605-14-2 |
SB-3CT is a potent, selective gelatinase inhibitor that dually inhibits MMP2/9 with Ki of 13.9 and 600 nM, display little to no affinity for MMP-3, 7 and 1 (Ki=15, 96 and 206 uM); also poorly inhibits the closely related zinc-dependent metalloprotease ADAM-17; demonstrates antitumor activity in a mouse model of T-cell lymphoma and shows significant reduction in the growth and number of experimental liver metastases and to an increase in survival; blocks MMP-9 activity, including MMP-9-mediated laminin cleavage, thus rescuing neurons from apoptosis in transient focal cerebral ischemia |
| H5273 |
RO 28-2653
|
261956-22-3 |
RO 28-2653 is a potent, selective and orally active matrix-metalloproteinases (MMPs) MMP2, MMP9 and MMP14 inhibitor with IC50 of 10, 12 and 10 nM, shows no activity against MMP3 and MMP1 (IC50>1 uM); reduces the growth of tumors induced by the inoculation of different cell lines producing MMPs and inhibits the tumor-promoting effect of fibroblasts on breast adenocarcinoma cells; reduces tumor growth and prolongs survival in a prostate cancer standard rat model. |
| H5272 |
proMMP9-IN-3c
|
2138321-18-1 |
proMMP9-IN-3c is a potent and specific inhibitor of the hemopexin-like domain of MMP-9 (proMMP-9) with Kd of 320 nM; disrupts MMP-9 homodimerization, prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in dissociation of EGFR; decreases phosphorylation of Src and its downstream target proteins FAK and paxillin in cancer cells; blocks cancer cell invasion of the basement membrane and reduces angiogenesis at 500 nM. |
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