| Name | SID 26681509 |
| Description | SID 26681509 is a selective, reversible and competitive human cathepsin L inhibitor (IC50 of 56 nM). |
| 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[1], 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[1]. |
| 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[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.85 mM), Sonication is recommended.
DMSO : 55 mg/mL (101.92 mM), Sonication is recommended.
|
| Keywords | Thiocarbazate | slow-binding | SID-26681509 | SID26681509 | SID 26681509 | reversible | propagation | Plasmodium falciparum | Plasmodium | Parasite | P. falciparum | malaria | major | Leishmania major | Leishmania | Inhibitor | inhibit | Human cathepsin L | falciparu | CysteineProtease | Cysteine Protease | Cathepsin L | Cathepsin |
| Inhibitors Related | Flubendazole | Gum arabic | Kojic acid | Urethane | Hydroxychloroquine | Metronidazole | Avermectin B1a | 2-Amino-2-methyl-1-propanol | Doxycycline | Fenpyroximate | Methylene Blue trihydrate | Coumaran |
| Related Compound Libraries | Anti-Parasitic Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Protease Inhibitor Library | Multi-Target Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Infection Compound Library |
United States
