品質等級
化驗
≥98% (HPLC)
形狀
solid
製造商/商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
light yellow
溶解度
DMSO: 10 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
InChI
1S/C22H20F2N4O2/c1-13-7-15(3-5-17(13)23)10-25-21(29)19-9-20(28-12-27-19)22(30)26-11-16-4-6-18(24)14(2)8-16/h3-9,12H,10-11H2,1-2H3,(H,25,29)(H,26,30)
InChI 密鑰
PYFRREJCFXFNRR-UHFFFAOYSA-N
一般說明
MMP-13活性的强效抑制剂(IC50=8 nM),并通过构象结构分析确定对MMP-1,-2,-3,-7,-8,-9,-10,-12,-14和-16具有预期的选择性。显示与MMP-13催化结构域结合并充当非锌螯合抑制剂。
一种嘧啶二甲酰胺化合物,可有效抑制MMP-13活性(IC50=8 nM),并通过构象结构分析确定对MMP-1,-2,-3,-7,-8,-9,-10,-12,-14和-16具有预期的选择性。显示与MMP-13催化结构域结合并充当非锌螯合抑制剂。
生化/生理作用
主要靶标
MMP-13活性
MMP-13活性
产物不与ATP竞争。
可逆:否
细胞渗透性:否
靶标IC50:MMP-13为8 nM
包裝
用惰性气体包装
警告
毒性:标准处理(A)
準備報告
使用前立即用缓冲液进一步稀释。
重構
复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多6个月。
其他說明
Engel, C.K., et al. 2005.Chem. Biol.12, 181.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 1
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Chemistry & biology, 12(2), 181-189 (2005-03-01)
Inhibitors for matrix metalloproteinases (MMPs) are under investigation for the treatment of cancer, arthritis, and cardiovascular disease. Here, we report a class of highly selective MMP-13 inhibitors (pyrimidine dicarboxamides) that exhibit no detectable activity against other MMPs. The high-resolution X-ray
eLife, 11 (2022-06-07)
Precise developmental control of jaw length is critical for survival, but underlying molecular mechanisms remain poorly understood. The jaw skeleton arises from neural crest mesenchyme (NCM), and we previously demonstrated that these progenitor cells express more bone-resorbing enzymes including Matrix
The Journal of investigative dermatology (2021-11-11)
Cutaneous squamous cell carcinoma (cSCC) is the most common metastatic skin cancer with increasing incidence worldwide. Previous studies have demonstrated the role of complement system in cSCC progression. In this study we have investigated the mechanistic role of serine protease
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