L 006235
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 0.25 nM
L-006235是一种强效的和选择性的组织蛋白酶K抑制剂。
体外:L-006235稀释至0.05 nM后,组织蛋白酶K的酶活性开始被抑制,但缓慢恢复,第一阶速率常数为0.023 s-1。最终的稳态酶活性为对照组的80%-90%,表明L-006235-组织蛋白酶K复合物的完全可逆性。L-006235不是组织蛋白酶K腈水解酶活性的底物。
体内:L-006235在大鼠中具有口服生物可利用度,终末半衰期超过3小时。去势雌性恒河猴每天一次持续7天口服给药L-006235。结果表明,胶原分解产物剂量依赖性减少达76%。L-006235的血浆浓度在24小时后高于骨吸收IC50值,表明功能性细胞和体内试验之间的相关性。这些结果表明,通过组织蛋白酶K抑制剂(如L-006235)抑制胶原分解,可能对骨质疏松症和其他涉及骨吸收的适应症有用[1]。
临床试验:N/A
参考文献:
[1] Palmer JT,Bryant C,Wang DX et al. Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J Med Chem.2005 Dec 1;48(24):7520-34.
Physical Appearance | White solid |
Storage | Store at 4°C |
M.Wt | 466.6 |
Cas No. | 294623-49-7 |
Formula | C24H30N6O2S |
Solubility | <46.66mg/ml in DMSO |
Chemical Name | N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide |
SDF | Download SDF |
Canonical SMILES | CN1CCN(CC1)C2=NC(=CS2)C3=CC=C(C=C3)C(=O)NC4(CCCCC4)C(=O)NCC#N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. | ||||||
Targets | cathepsin K | |||||
IC50 | 0.25nM |