SID 26681509

SKU: orb1708525

Description

SID 26681509 is a potent, reversible, and competitive inhibitor of human cathepsin L, exhibiting an IC50 value of 56 nM. This small molecule is a valuable research tool for studying cathepsin L function in various pathological contexts, including cancer metastasis and viral entry, in both cellular and biochemical assay systems.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 958772-66-2
• MW: 539.65
• Purity: 98.16% (May vary between batches)
• Formula: C₂₇H₃₃N₅O₅S
• SMILES: CCc1ccccc1NC(=O)CSC(=O)NNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)OC(C)(C)C
• Target: Parasite,Cysteine Protease
• Solubility: DMSO:55 mg/mL (101.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.85 mM)

Bioactivity

• Target IC50:
  P. falciparum:15.4 μM |Cathepsin L (human):56 nM |Leishmania major:12.5 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.
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• In Vitro:
  After a 4-hour preincubation with cathepsin L, SID 26681509 becomes more potent (IC50: 1.0 nM). SID 26681509 acts as a slow-binding, slowly reversible competitive inhibitor with inhibition rate constants kon = 24,000 M^-1s^-1 and koff = 2.2 × 10^-5 s^-1 (Ki = 0.89 nM), as determined through transient kinetic analysis for single-step reversibility. Molecular docking studies, using the X-ray crystal structure of papain/CLIK-148, show that SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC50 values ranging from 618 nM to 8.442 μM after one hour.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CysteineProtease, Cysteine Protease, Cathepsin L, Cathepsin, inhibit, Inhibitor, Parasite, falciparu, Human cathepsin L, malaria, major, Leishmania, Leishmania major, SID 26681509, SID26681509, SID-26681509, P. falciparum, Thiocarbazate, reversible, propagation, Plasmodium falciparum, Plasmodium, slow-binding

Compound Identifiers

PubChem CID

16725315