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

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.

For research use only. We do not sell to patients.

SHP1-IN-2

SHP1-IN-2 Chemical Structure

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Description

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

 

In Vitro

SHP1-IN-2 (M029) (up to 50 μM; 24-72 h) shows no obvious cytotoxicity in Jurkat T, HEK293, MC38, EO771, B16-F10, and Raw264.7 cells[1].
SHP1-IN-2 (0-20 μM; Anti-CD3 Antibody (OKT-3) (HY-P990864) stimulation for 10 min) enhances the phosphorylation of LCK, PLCγ, and ERK1/2 and promotes IL-2 production in TCR-stimulated Jurkat T cells[1].

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

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 /
In Vivo

SHP1‑IN‑2 (M029) (25 mg/kg, 100 mg/kg; once daily) significantly suppresses tumor growth in MC38 colon cancer syngeneic mouse models[1].
SHP1‑IN‑2 (25 mg/kg; once daily) increases infiltration and activation of NK cells and CD8+ T cells, reduces the proportion of PD-1+ TIM3+ exhausted T cells in MC38 tumor tissues, shows no obvious toxicity or body weight loss in tumor‑bearing mice, and loses antitumor efficacy in CD8+ T cell‑depleted mice and nude mice[1].

MedChemExpress (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.
Molecular Weight

355.82

Formula

C13H10ClN3O3S2

SMILES

O=S(C1=CC=C(NC(CCl)=O)C=C1)(NC2=C(C#N)C=CS2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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.

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SHP1-IN-2
Cat. No.:
HY-186140
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