2. Apoptosis
  3. RIP kinase
  4. SZM679

SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD).

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SZM679 Chemical Structure

SZM679 Chemical Structure

CAS No. : 3027645-52-6

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5 mg USD 648 In-stock
10 mg USD 1033 In-stock
25 mg USD 2083 In-stock
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Based on 1 publication(s) in Google Scholar

SZM679 Related Antibodies

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Description

SZM679 is a potent, orally active and selective RIPK1 inhibitor with Kd values of 8.6 nM and >5000 nM for RIPK1 and RIPK3, respectively. SZM679 reverses the tumor necrosis factor-induced systemic inflammatory response. SZM679 decreases the Tau hyperphosphorylation, neuroinflammation, and the RIPK1 phosphorylation level in the hippocampus and cortex. SZM679 can be used in research of Alzheimer's disease (AD)[1].

IC50 & Target[1]

RIPK1

8.6 nM (Kd)

RIPK3

>5000 nM (Kd)

In Vitro

SZM679 (0-10 μM; 24 h; necrotic L929 and HT-29 cells) has an anti-necrosis activity by Inhibiting the RIPK1 pathway with an EC50 value of 2 nM. SZM679 also protects against TNF-α, cycloheximide, and z-VAD-fmk (TCZ)-induced necroptosis. SZM679 protects against necroptosis induced by TZ in a dose dependent manner[1].
SZM679 (1 μM; 6 h; necrotic HT-29 cells) selectively inhibits the expression of RIPK1 but not RIPK3 or MLKL. SZM679 blocks necrosome formation by inhibiting TSZ-induced phosphorylation of RIPK1[1].

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

SZM679 Related Antibodies

Western Blot Analysis[1]

Cell Line: Necrotic HT-29 cells
Concentration: 1 μM
Incubation Time: 6 hours
Result: Inhibited the phosphorylation of RIPK1 at 1 μM, resulting in the inhibition of the downstream phosphorylation of RIPK3 and MLKL.
In Vivo

SZM679 (10-40 mg/kg; i.p.; male C57BL/6 J mice with TNF-induced SIRS models) protects against necroptosis-specific TNF-induced systemic inflammatory response syndrome (SIRS) in vivo[1].
SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) improves cognitive function in STZ-induced AD mice[1].
SZM679 (1 mg/kg; administered intragastrically; once daily for 7 days) rescues brain structure damage with no obvious toxicity and decreases AD biomarkers and decreases the expression levels of inflammatory cytokines and inhibits RIPK1 phosphorylation in the brain tissues of AD mice[1].

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

Animal Model: Male C57BL/6 J mice with TNF-induced SIRS models[1]
Dosage: 10, 20, and 40 mg/kg
Administration: Intraperitoneal injection
Result: Protected mice in a dose-dependent manner from hypothermia and death.
Animal Model: Male C57BL/6 J mice with AD models[1]
Dosage: 1 mg/kg
Administration: Administered intragastrically; once daily for 7 days
Result: Improved the anxiety, behavior, and exploratory ability of AD mice.
Improved the learning and memory ability of AD mice.
Animal Model: Male C57BL/6 J mice with AD models[1]
Dosage: 1 mg/kg
Administration: Administered intragastrically; once daily for 7 days
Result: Rescued the damaged hippocampal structure of AD mice and restored the cell number and morphology.
Down-regulated the expression of the inflammatory cytokines, the IL-1β and TNF-α levels.
Molecular Weight

591.51

Formula

C27H18F5N3O5S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1CC(C1)=O)NC2=NC3=CC(F)=C(OC4=CC=C(F)C(NC(CC5=CC=CC(OC(F)(F)F)=C5)=O)=C4)C=C3S2
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 : 125 mg/mL (211.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6906 mL 8.4529 mL 16.9059 mL
5 mM 0.3381 mL 1.6906 mL 3.3812 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6906 mL 8.4529 mL 16.9059 mL 42.2647 mL
5 mM 0.3381 mL 1.6906 mL 3.3812 mL 8.4529 mL
10 mM 0.1691 mL 0.8453 mL 1.6906 mL 4.2265 mL
15 mM 0.1127 mL 0.5635 mL 1.1271 mL 2.8176 mL
20 mM 0.0845 mL 0.4226 mL 0.8453 mL 2.1132 mL
25 mM 0.0676 mL 0.3381 mL 0.6762 mL 1.6906 mL
30 mM 0.0564 mL 0.2818 mL 0.5635 mL 1.4088 mL
40 mM 0.0423 mL 0.2113 mL 0.4226 mL 1.0566 mL
50 mM 0.0338 mL 0.1691 mL 0.3381 mL 0.8453 mL
60 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7044 mL
80 mM 0.0211 mL 0.1057 mL 0.2113 mL 0.5283 mL
100 mM 0.0169 mL 0.0845 mL 0.1691 mL 0.4226 mL
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SZM679 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SZM6793027645-52-6SZM 679SZM-679RIP kinaseReceptor-interacting protein kinasesRIPKtumor necrosis factorinflammatorynecrosisTauphosphorylationhippocampuscortexAlzheimer's diseaseInhibitorinhibitorinhibit

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