2. Membrane Transporter/Ion Channel Anti-infection Immunology/Inflammation Apoptosis
  3. Sec61 SARS-CoV Interleukin Related TNF Receptor IFNAR
  4. KZR-8445

KZR-8445 是一种环状缩酚酸肽，是一种底物选择性 Sec61 抑制剂。KZR-8445 结合完全开放的 Sec61 侧门，阻断管腔塞结构域的结合，稳定侧门螺旋，捕获特定信号肽，并破坏分泌蛋白和膜蛋白的生物合成。KZR-8445 可抑制原代免疫细胞中促炎细胞因子的分泌。KZR-8445 能够抑制 SARS-CoV-2 复制、病毒诱导的细胞毒性以及刺突蛋白的生物合成。KZR-8445 可阻断类风湿性关节炎小鼠模型的疾病进展。KZR-8445 可用于类风湿性关节炎和 SARS-CoV-2 感染的相关研究。

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KZR-8445

KZR-8445 Chemical Structure

CAS No. : 2377734-91-1

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Other Forms of KZR-8445:

KZR-8445 相关抗体

Top Publications Citing Use of Products

查看 Interleukin Related 亚型特异性产品:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KZR-8445, a cyclic depsipeptide, is a client-selective Sec61 inhibitor. KZR-8445 binds to the fully opened Sec61 lateral gate, blocks lumenal plug domain access, stabilizes lateral gate helices, traps select signal peptides, and disrupts secretory and membrane protein biogenesis. KZR-8445 inhibits pro-inflammatory cytokine secretion in primary immune cells. KZR-8445 inhibits SARS-CoV-2 replication, virus-induced cytotoxicity, and spike protein biogenesis. KZR-8445 blocks disease progression in a mouse model of rheumatoid arthritis. KZR-8445 can be used for the researches of rheumatoid arthritis and SARS-CoV-2 infection[1].

IC50 & Target[1]

IL-2

 

IL-1β

 

IL-6

 

IL-23

 

体外研究
(In Vitro)

KZR-8445 (0.1-10000 nM; 24 h) 可直接靶向 Sec61α，在表达野生型 Sec61α 的 HEK293 Flp-In T-REx 细胞中强效抑制 IL-2-GLuc 和 TNFα-GLuc 的分泌，其 IC50 约为 100 nM[1]。
KZR-8445 (24 h) 可抑制 HEK293 Flp-In T-REx 细胞中融合 HER3、催乳素、PD1、TNFα 和 IL-2 信号肽的 GLuc 报告蛋白的分泌，其 IC50 值范围为 32 nM 至 1068 nM[1]。
KZR-8445 可强效抑制活化人外周血单个核细胞 (PBMCs) 中 Sec61 依赖性促炎细胞因子的分泌，其 IC50 值为亚微摩尔级别；同时在浓度高达 20 µM 时，对细胞活力无影响[1]。
KZR-8445 (0.01-10 µM; 2 h) 可抑制 Vero E6 细胞中 SARS-CoV-2 的复制及刺突蛋白的生物合成，且在浓度高达 10 µM 时仍能维持细胞存活率在 50% 以上[1]。

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

KZR-8445 相关抗体:
体内研究
(In Vivo)

KZR-8445 (10-20 mg/kg；静脉注射；每周 3 次/每周 1 次；持续 2 周) 可在类风湿关节炎小鼠模型中呈剂量依赖性地阻断疾病进展[1]。

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

Animal Model: BALB/c (female, 7-8 weeks old, rheumatoid arthritis induced via intravenous anti-type II collagen antibody cocktail on day 0 + intraperitoneal LPS (HY-D1056) on day 3)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v.; weekly/weekly; 2 weeks
Result: Blocked disease progression with a statistically significant effect at 10 and 20 mg/kg thrice weekly.
Significantly blocked disease progression at 20 mg/kg weekly.
Showed no significant toxicity, with body weight changes comparable to or greater than vehicle-treated mice across all treatment groups.
分子量

1083.95

Formula

C49H61BrF6N8O8
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

KZR-8445 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:

KZR-84452377734-91-1KZR8445KZR 8445Sec61SARS-CoVInterleukin RelatedTNF ReceptorIFNARSec61 complex, SecY, Sec61 channel SARS coronavirusILTumor Necrosis Factor ReceptorTNFRInterferon-α/β receptorInterferon-alpha/beta receptormouse modelprimary immune cellsSec61α subunitSARS-CoV-2HEK293 Flp-In T-REx cellsrheumatoid arthritisVero E6 cellsribosome-Sec61 complexT-cell acute lymphoblastic leukemia cellshuman PBMCsInhibitorinhibitorinhibit

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