2. Apoptosis MAPK/ERK Pathway
  3. RIP kinase Mixed Lineage Kinase Necroptosis
  4. SZM-1209

SZM-1209 是一种口服有效且特异性的 RIPK1 抑制剂，Kd 为 85 nM。 SZM-1209 表现出高抗坏死性凋亡(necroptosis) 活性 (EC50=22.4 ± 8.1 nM)。 SZM-1209 具有抗 SIRS (全身炎症反应综合征)和抗 ALI (急性肺损伤)作用。

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SZM-1209 Chemical Structure

SZM-1209 Chemical Structure

CAS No. : 2919801-86-6

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SZM-1209 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

IC50 & Target

RIPK1

85 nM (Kd)

RIPK3

>10000 nM (Kd)

体外研究
(In Vitro)

SZM-1209 以剂量依赖的方式阻断坏死性凋亡[1]。
SZM-1209 (0-1 μM, 6 h) 特异性抑制 RIPK1-RIPK3-MLKL 坏死性凋亡信号的磷酸化[1]。

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

SZM-1209 相关抗体:

Western Blot Analysis[1]

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.
体内研究
(In Vivo)

SZM-1209 (25-100 mg/kg, 灌胃) 在 mTNF-α 诱导的全身炎症反应综合征 (SIRS) 模型中具有显著的抗炎作用，可以逆转小鼠死亡[1]。
SZM-1209 (25-100 mg/kg, 腹腔注射) 通过减少肺水肿和病理损伤显着减轻 ALI (急性肺损伤)[1]。

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.
分子量

696.71

Formula

C31H29F5N4O5S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SZM-1209 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

SZM-12092919801-86-6SZM1209SZM 1209RIP kinaseMixed Lineage KinaseNecroptosisReceptor-interacting protein kinasesRIPKMLKsAcute lung injuryacute respiratory distress syndromeALI/ARDSHT-29 cellsSIRSsystemic inflammatory response syndromeMLKL phosphorylationL929 cellsInhibitorinhibitorinhibit

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