958772-66-2
958772-66-2 结构式
基本信息
化合物SID 26681509
SID 26681509
SID26681509
SID-26681509
N-[(1,1-Dimethylethoxy)carbonyl]-L-tryptophan-2-[[[2-[(2-ethylphenyl)amino]-2-oxoethyl]thio]carbonyl]hydrazide
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] [2-[(2S)-3-(1H-indol-3-yl)-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoyl]hydrazinyl]methanethioate
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/08/19 | HY-103353 | SID26681509; SID-26681509 SID 26681509 | 958772-66-2 | 1mg | 720元 |
| 2024/08/19 | HY-103353 | SID26681509; SID-26681509 SID 26681509 | 958772-66-2 | 5mg | 1800元 |
| 2024/08/19 | HY-103353 | SID26681509; SID-26681509 SID 26681509 | 958772-66-2 | 10 mM * 1 mLin DMSO | 2137元 |
常见问题列表
IC50: 56 nM (Human cathepsin L), 0.5 μM (Cathepsin V), 15.4 μM ( Plasmodium falciparum ), 12.5 μM ( Leishmania major )
After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an
IC
50
of 1.0 nM. SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M
-1
s
-1
and koff = 2.2 × 10
-5
s
-1
(K
i
= 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148.
SID 26681509 inhibits papain and cathepsins B, K, S, and V with
IC
50
values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G.
SID 26681509 inhibits cathepsin V activity with an IC
50
value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability.
SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models.