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.
For research use only. We do not sell to patients.
- CAS No.: 2919801-86-6
- Formula: C31H29F5N4O5S2
- Molecular Weight:696.71
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
RIPK1 85 nM (Kd) |
RIPK3 >10000 nM (Kd) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | CC50 |
>100 μM
Compound: 21; SZM-1209
|
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
|
[PMID: 36908007] |
| HT-29 | EC50 |
22.4 nM
Compound: 21; SZM-1209
|
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
|
[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.
-
Cell Line:HT-29 cells
-
Concentration:0.1, 0.5, and 1 μM
-
Incubation Time:6 h
-
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.
-
Animal Model:C57BL/6J mice (female, 6-8 weeks old, mTNF-α (intravenous injection)-induced SIRS model)[1]
-
Dosage:25, 50, and 100 mg/kg
-
Administration:Intragastric administration
-
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.
-
Animal Model:C57BL/6J mice (female, 6-8 weeks old, NNK (HY-126477) (65 mg/kg) short-term intratracheal exposure-induced ALI model)[1]
-
Dosage:25, 50, and 100 mg/kg
-
Administration:IP
-
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
-
CAS No. 2919801-86-6
-
Molecular Weight 696.71
-
Formula C31H29F5N4O5S2
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SZM-1209 Related Classifications
HY-149052 Related Classifications
Powered by Bioz