SID 26681509

Research use only, not for human use.

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).

SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM).(In Vitro):After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent(IC50 : 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-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 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 IC50 values determined after one hour ranging from 618 nM to 8.442 μM.(In Vivo):survival in murine models of sepsis significantly improved SID 26681509 by and reduces liver damage following warm liver ischemia/reperfusion (I/R) models.

After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an IC50 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-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 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 IC50 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 IC50 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.

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Proteasome/Ubiquitin

Cysteine Protease

Hormone-sensitive lipase (HSL)

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958772-66-2

539.65

C27H33N5O5S

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (92.65 mM)

CCc1ccccc1NC(=O)CSC(=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C

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(-20℃)

With Ice Pack

≥ 2 years