1. Autophagy Metabolic Enzyme/Protease
  2. Autophagy Phosphatase
  3. SMIP-031

SMIP-031 是一种强效且具有口服活性的 PPM1A 抑制剂,其 IC50 值为 180 nM。SMIP-031 可诱导自噬 (autophagy)。SMIP-031 可抑制小鼠中的 Mycobacterium tuberculosis 感染。

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SMIP-031 Chemical Structure

SMIP-031 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SMIP-031 is a potent and orally active PPM1A inhibitor with an IC50 value of 180 nM. SMIP-031 induces autophagy. SMIP-031 inhibits Mycobacterium tuberculosis infect in mice[1].

IC50 & Target

IC50: 180 nM (PPM1A)[1]

体外研究
(In Vitro)

SMIP-031 (0.5, 1, 2.5,5 µM; 5 days) 以剂量依赖性方式减少受感染的 THP-1 细胞中的 Mycobacterium tuberculosis (Mtb) 的负担[1]
SMIP-031 (0.25, 0.5, 1, 2, 4, 8 µM) 通过降低 Mtb 感染的 THP-1 巨噬细胞中 S403-p62 的蛋白表达来诱导自噬[1]

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

Western Blot Analysis[1]

Cell Line: THP-1 macrophages (Mtb-infected)
Concentration: 0.25, 0.5, 1, 2, 4, 8 µM (bafilomycin 100 nM)
Incubation Time:
Result: Iecreased the protein expression of S403-p62 in a dose-dependent manner.
体内研究
(In Vivo)

SMIP-031 (12.5, 50 mg/kg; i.p.; daily for 8 days) 可降低受感染小鼠脾脏中的细菌负担[1].
药代动力学分析 (ICR (CD-1) mice; i.v. for 2 mg/kg; p.o. for 10 mg/kg)[1].

administration T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h*ng/mL) AUCINF-obs (h*ng/mL) CL obs (mL/min/kg) F (%)
p.o. 0.771 0.250 908 759 761 - 73.7
i.v. 0.634 - - 206 208 >170 -

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

Animal Model: BALB/c mice (Mtb mc26206 strain)[1]
Dosage: 12.5, 50 mg/kg
Administration: I.p.; daily for 14 days
Result: Reduced the Mtb burden and no weight loss or visible signs of toxicity were observed during the experiment.
分子量

366.22

Formula

C17H17BrFNO2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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SMIP-031
目录号:
HY-163782
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