SZM-1209
SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects.
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- CAS No.: 2919801-86-6
- Formule: C31H29F5N4O5S2
- Masse moléculaire:696.71
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Help & FAQs
Activité biologique
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RIPK1 85 nM (Kd) |
RIPK3 >10000 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| HT-29 | CC50 |
>100 μM
Compound: 21; SZM-1209
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Cytotoxicity against human HT-29 cells incubated for 16 to 24 hrs measured by cell-titre glo luminescent cell viability assay
Cytotoxicity against human HT-29 cells incubated for 16 to 24 hrs measured by cell-titre glo luminescent cell viability assay
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[PMID: 36908007] |
| HT-29 | EC50 |
22.4 nM
Compound: 21; SZM-1209
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Anti-necroptotic activity in human HT-29 cells assessed as inhibition of human TNFalpha/Smac mimetic/Z-VAD-FMK induced necroptosis preincubated with compound for 16 to 24 hrs followed by TSZ stimulation for 12 hrs measured by cell-titre glo luminescent ce
Anti-necroptotic activity in human HT-29 cells assessed as inhibition of human TNFalpha/Smac mimetic/Z-VAD-FMK induced necroptosis preincubated with compound for 16 to 24 hrs followed by TSZ stimulation for 12 hrs measured by cell-titre glo luminescent ce
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[PMID: 36908007] |
SZM-1209 blocks necroptosis in a dose-dependent manner[1].
SZM-1209 (0-1 μM, 6 h) specifically inhibits phosphorylation of RIPK1-RIPK3-MLKL necroptosis signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 cells
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Concentration:0.1, 0.5, and 1 μM
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Incubation Time:6 h
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Result:SZM-1209 at 1 μM completely inhibited phosphorylation of both RIPK1 and RIPK3 in 2-6 h, and subsequently inhibited the phosphorylation of downstream MLKL.
SZM-1209 (25-100 mg/kg, IP) significantly alleviates ALI (acute lung injury) by reducing pulmonary edema and pathological damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (female, 6-8 weeks old, mTNF-α (intravenous injection)-induced SIRS model)[1]
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Dosage:25, 50, and 100 mg/kg
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Administration:Intragastric administration
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Result:Dose-dependently improved survival rates of the SIRS mice to 30, 90, and 100%. Could effectively protect against mTNFα-induced SIRS in vivo. Serum levels of IL-6 and IL-1β were significantly decreased.
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Animal Model:C57BL/6J mice (female, 6-8 weeks old, NNK (HY-126477) (65 mg/kg) short-term intratracheal exposure-induced ALI model)[1]
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Dosage:25, 50, and 100 mg/kg
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Administration:IP
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Result:Exhibited lower levels of IL-6 and TNF-α in BALF than those of model mice. Inhibited the expression of inflammatory genes of IL-6 and TNF-α in lung tissues of mice at a mRNA level. Significant reduced phosphorylation of RIPK1, and also completely blocked at a high dose of 100 mg/kg in lung tissue of ALI model mice.
Chemical Information
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CAS No. 2919801-86-6
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Masse moléculaire 696.71
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Formule C31H29F5N4O5S2
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SMILES
CCS(=O)(NC1CCC(CC1)C(NC2=NC3=C(S2)C=C(C(F)=C3)OC4=CC=C(C(NC(CC5=CC=CC(C(F)(F)F)=C5)=O)=C4)F)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SZM-1209 Related Classifications
HY-149052 Related Classifications
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