Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis. Necrosulfonamide significantly decreases BV6/DAC-induced cell death in MV4-11 cells. Necrosulfonamide is also an effective inhibitor of the necroptotic pathway induced by STS in the presence of caspase inhibitor.
JACC-BASIC TRANSL SC. 2023 May 31.
PCSK9 Promotes Hypoxia-Induced Endothelial Cell Pyroptosis by Regulating Smac Mitochondrion-Cytoplasm Translocation in Critical Limb Ischemia
Necrosulfonamide purchased from AbMole
| Molecular Weight | 461.47 |
| Formula | C18H15N5O6S2 |
| CAS Number | 1360614-48-7 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Bae JH, et al. Arch Pharm Res. Chemical regulation of signaling pathways to programmed necrosis.
| Related Necroptosis Products |
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TP4 (Nile tilapia piscidin) is an orally active piscidin-like antimicrobial peptide. |
| TC13172
TC13172 is an inhibitor of MLKL and necroptosis that acts on HT-29 cells with an EC50 value of 2 nM. |
| GW806742X hydrochloride
GW806742X hydrochloride is an ATP mimetic and potent inhibitor of MLKL and necroptosis, slowing down MLKL membrane translocation and binding to the MLKL pseudokinase domain with a Kd value of 9.3 μM. GW806742X hydrochloride has anti-VEGFR2 activity (IC50=2 nM). GW806742X hydrochloride has anti-VEGFR2 activity (IC50=2 nM). |
| GSK-843
GSK-843 is a potent receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. |
| PK68
PK68 is a potent and selective type II RIPK1 inhibitor with an IC50 value of approximately 90 nM that inhibits RIPK1-dependent necroptosis. It can be used in studies related to inflammatory diseases and cancer metastasis. |
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