2. Immunology/Inflammation NF-κB GPCR/G Protein
  3. STING IKK IFNAR Interleukin Related CXCR
  4. STING agonist-50

STING agonist-50 是一种口服有效的 STING 激动剂，IC50 为 3.457 μM。STING agonist-50 可激活 STING 信号通路，促进下游 TBK1 和 IRF3 的磷酸化。STING agonist-50 可诱导 IFN-β、CXCL10 和 IL-6 的表达。STING agonist-50 可抑制同源小鼠模型中的肿瘤生长。STING agonist-50 可用于结直肠癌的研究。

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STING agonist-50

STING agonist-50 Chemical Structure

CAS No. : 3058842-90-0

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STING agonist-50 相关抗体

Top Publications Citing Use of Products

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IKK-α IKK-β IKK IKKε TBK1

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

STING agonist-50 is an orally active STING agonist with an IC50 of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

TBK1

 

IL-6

 

体外研究
(In Vitro)

STING agonist-50 (Compound X41) 可激活 THP1-Dual 细胞中的 STING 信号通路，其诱导 IRF3 调控的荧光素酶活性的 EC50 值为 13.60 μM，诱导 NF-κB 调控的荧光素酶活性的 EC50 值为 17.52 μM[1]。
STING agonist-50 (12.5-50 μM; 3 h) 可通过 STING 依赖型机制在 THP1-Dual 细胞中诱导 IFN-β、CXCL10 和 IL-6 mRNA 呈浓度依赖性上调，但对 STING 敲除的 THP1 细胞中 IFN-β mRNA 无影响[1]。
STING agonist-50 (20-40 μM; 1-12 h) 可在 THP1-Dual 细胞中诱导 STING、TBK1 和 IRF3 发生时间依赖性及浓度依赖性的磷酸化，且在处理后 3 h 观察到最大激活水平[1]。

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

STING agonist-50 相关抗体:

Real Time qPCR[1]

Cell Line: THP1-Dual cells, THP1-STING^KO^ cells
Concentration: 12.5, 25 and 50 μM
Incubation Time: 3 h
Result: Induced concentration-dependent upregulation of IFN-β, CXCL10, and IL-6 mRNA in THP1-Dual cells.
Did not increase IFN-β mRNA transcription in THP1-STING^KO^ cells even at 50 μM.

Western Blot Analysis[1]

Cell Line: THP1-Dual cells
Concentration: 20, 30 and 40 μM (3 h incubation); 30 μM (1, 3, 6, 12 h incubation)
Incubation Time: 1, 3, 6, 12 h (30 μM); 3 h (20, 30, 40 μM)
Result: Induced maximal phosphorylation of STING, TBK1, and IRF3 at 3 h post-treatment.
Promoted phosphorylation of these downstream proteins in a concentration-dependent manner.
药代动力学
(Parmacokinetics)
Species Dose Route AUCINF_obs T1/2 Vz CL Tmax Cmax F
Rat[1] 1 mg/kg i.v. 72.91 μg·h/mL 4.43 h 87.78 mL/kg 0.23 mL/min/kg / / /
Rat[1] 5 mg/kg i.p. 141.42 μg·h/mL 4.11 h 209.71 mL/kg 0.59 mL/min/kg 0.26 h 82.37 μg/mL 39.57 %
Rat[1] 8 mg/kg p.o. 60.08 mg·h/L 9.92 h 1904.93 mL/kg 2.24 mL/min/kg 0.33 h 8.32 μg/mL 10.51 %
体内研究
(In Vivo)

STING agonist-50 (Compound X41) (10-100 mg/kg; i.p., p.o.; 第 1, 3, 5, 8 天给药) 在小鼠 MC38 结直肠癌模型中展现出强效的剂量依赖性抗肿瘤功效[1]。

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

Animal Model: C57BL/6 (female; subcutaneous MC38 colorectal carcinoma model)[1]
Dosage: 10 mg/kg (i.p.); 20 mg/kg (i.p.); 50 mg/kg (p.o.); 100 mg/kg (p.o.)
Administration: i.p.; days 1, 3, 5, 8; p.o.; days 1, 3, 5, 8
Result: Achieved complete tumor regression in 2 out of 6 mice (10 mg/kg i.p.).
Achieved complete tumor regression in 3 out of 6 mice, and drastically reduced final tumor volumes and weights relative to controls (20 mg/kg i.p.).
Significantly reduced final tumor volumes and weights compared to saline controls, with robust tumor growth inhibition and no complete regression (50 mg/kg p.o.).
Significantly reduced final tumor volumes and weights compared to saline controls (100 mg/kg p.o.).
Showed no significant body weight changes relative to controls, indicating good tolerability (all doses).
Induced significantly higher plasma IFN-β levels 4 hours post-administration than 10 mg/kg Compound 22 (10 mg/kg i.p.).
Induced measurable plasma IFN-β levels (50 mg/kg p.o.).
Caused no significant histopathological alterations in kidney, lung, spleen, liver, and heart tissue (all doses).
分子量

395.80

Formula

C20H14ClN3O4
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

STING agonist-50 相关分类

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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:

STING agonist-503058842-90-0STING agonist50STING agonist 50STINGIKKIFNARInterleukin RelatedCXCRStimulator of Interferon GenesTMEM173MITAERISMPYSIκB kinaseI kappa B kinase Interferon-α/β receptorInterferon-alpha/beta receptor ILCXC chemokine receptorsC-X-C motif chemokine receptorsTBK1MC38 colorectal carcinomasyngeneic mouse modelsIRF3STING signaling pathwayIL-6human STINGCXCL10IFN-βTHP1-Dual cellsInhibitorinhibitorinhibit

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