1. Metabolic Enzyme/Protease
    Anti-infection
  2. Cathepsin
    Parasite
  3. SID 26681509

SID 26681509 

Cat. No.: HY-103353 Purity: >97.0%
Handling Instructions

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.

For research use only. We do not sell to patients.

SID 26681509 Chemical Structure

SID 26681509 Chemical Structure

CAS No. : 958772-66-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 689 In-stock
Estimated Time of Arrival: December 31
1 mg USD 195 In-stock
Estimated Time of Arrival: December 31
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G[1].

IC50 & Target

IC50: 56 nM (Human cathepsin L), 15.4 μM (Plasmodium falciparum), 12.5 μM (Leishmania major)[1]

In Vitro

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[1].
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[1].

In Vivo

SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models[2].

Molecular Weight

539.65

Formula

C₂₇H₃₃N₅O₅S

CAS No.

958772-66-2

SMILES

O=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[[email protected]](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >97.0%

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Keywords:

SID 26681509SID26681509SID-26681509CathepsinParasiteThiocarbazateslow-bindingpropagationmalariaLeishmaniamajorreversiblePlasmodiumfalciparuInhibitorinhibitorinhibit

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SID 26681509
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