2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation
  3. SHP1 Phospholipase ERK Interleukin Related
  4. SHP1-IN-2

SHP1‑IN‑2 是一种具有口服活性的 SHP1 选择性抑制剂。SHP1‑IN‑2 可与 SHP1 的位点 Cys480 共价结合。SHP1‑IN‑2 可诱导强效抗肿瘤免疫并抑制同基因肿瘤生长。SHP1-IN-2 通过激活自然杀伤细胞和细胞毒性 CD8＋ T 细胞，以及减少 T 细胞，在 svngeneic 癌症模型中阻止肿瘤进展。SHP1‑IN‑2 可用于癌症相关研究。

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SHP1-IN-2

SHP1-IN-2 Chemical Structure

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Customer Review

SHP1-IN-2 相关抗体

Top Publications Citing Use of Products

查看 Phospholipase 亚型特异性产品:

查看所有亚型
Phospholipase A PLD Phospholipase C

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by activating natural killer cells and cytotoxic CD8＋ T cells, along with reduced T cel l. SHP1‑IN‑2 can be used for cancer‑related research[1].

IC50 & Target

ERK1

 

ERK2

 

PLC

 

IL-2

 

体外研究
(In Vitro)

SHP1-IN-2 (M029) (up to 50 μM; 24-72 h) 在 Jurkat T、HEK293、MC38、EO771、B16-F10 和 Raw264.7 细胞中无明显细胞毒性[1]。
SHP1-IN-2 (0-20 μM; Anti-CD3 Antibody (OKT-3) (HY-P990864) 刺激10 min) 可增强 TCR 刺激的 Jurkat T 细胞中 LCK、PLCγ 和 ERK1/2 的磷酸化水平，并促进 IL-2 的产生[1]。

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

SHP1-IN-2 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC F
Mice[1] 25 mg/kg p.o. 38.5 min 29.8 μM 1411 μM·h 18 %
Mice[1] 25 mg/kg i.p. 36.3 min 122.1 μM 5094 μM·h /
体内研究
(In Vivo)

SHP1‑IN‑2 (M029) (25 mg/kg、100 mg/kg；每日 1 次) 可显著抑制 MC38 结肠癌同源小鼠模型中的肿瘤生长[1]。
SHP1‑IN‑2 (25 mg/kg；每日 1 次) 可增加 MC38 肿瘤组织中 NK 细胞和 CD8+ T 细胞的浸润与活化，降低 PD-1+ TIM3+ 耗竭型 T 细胞的比例，对荷瘤小鼠无明显毒性或体重下降作用，且在 CD8+ T 细胞耗竭小鼠和裸鼠中丧失抗肿瘤活性[1]。

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

Animal Model: Female immunocompetent C57BL/6 mice (6-8 weeks old) are subcutaneously inoculated with MC38 colon cancer cells[1]
Dosage: 25 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; for 10 days
Result: Markedly suppresses tumor growth and reduces tumor weight without affecting body weight in mice.
Animal Model: Female immunocompetent C57BL/6 mice (6-8 weeks old) are subcutaneously inoculated with MC38 colon cancer cells[1]
Dosage: 25 mg/kg
Administration: Oral administration; once daily; for 10 days
Result: Significantly increases infiltration and activation of NK cells and CD8+ T cells in tumor tissues.
Reduces the proportion of PD-1+ TIM3+ exhausted T cells in the tumor microenvironment.
Loses antitumor efficacy in CD8+ T cell-depleted mice and nude mice.
分子量

355.82

Formula

C13H10ClN3O3S2
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

SHP1-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

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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:

SHP1-IN-2SHP1PhospholipaseERKInterleukin RelatedShp1PTPN6Src homology region 2 (SH-2) domain-containing phosphatase 1Extracellular signal regulated kinasesILsyngeneic tumorPTPsantitumor immunitycancerCys480phenyl chloroacetamideallosteric inhibitorInhibitorinhibitorinhibit

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