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

SID 26681509 quarterhydrate 

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

SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows no inhibitory activity against cathepsin G.

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

SID 26681509 quarterhydrate Chemical Structure

SID 26681509 quarterhydrate Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 712 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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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of SID 26681509 quarterhydrate:

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  • Biological Activity

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Description

SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate 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 quarterhydrate shows no inhibitory activity against cathepsin G[1].

IC50 & Target

IC50: 56 nM (Human cathepsin L), 0.5 μM (Cathepsin V), 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].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

544.16

Formula

C₂₇H₃₃N₅O₅S.₁/₄H₂O

SMILES

O=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[[email protected]](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O.[1/4].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
Solvent & Solubility
In Vitro: 

DMSO : 27 mg/mL (49.62 mM; Need ultrasonic and warming)

Ethanol : 5 mg/mL (9.19 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8377 mL 9.1885 mL 18.3769 mL
5 mM 0.3675 mL 1.8377 mL 3.6754 mL
10 mM 0.1838 mL 0.9188 mL 1.8377 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: ≥97.0%

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Keywords:

SID 26681509 quarterhydrateCathepsinParasiteThiocarbazateslow-bindingpropagationmalariaLeishmaniamajorreversiblePlasmodiumfalciparumInhibitorinhibitorinhibit

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Product Name:
SID 26681509 quarterhydrate
Cat. No.:
HY-103353A
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