TREM2-IN-1 

TREM2-IN-1 (OPA) is a TREM2 inhibitor derived from oxaliplatin and artesunate. TREM2-IN-1 can relieves immunosuppressive tumor microenvironment and enhancing chemical anticancer efficiency. TREM2-IN-1 deters the tumor growth in mice models bearing MC38 colorectal tumor by reducing the number of CD206⁺ and CX₃CR1⁺ immunosuppressive macrophages. TREM2-IN-1 also promotes the expansion and infiltration of immunostimulatory dendritic, cytotoxic T and natural killer cells^[1].

TREM2^[1]

TREM2-IN-1 (0.8 μM, 72 h) inhibits the prophase of DNA synthesis (G1 phase) and has potent proapoptotic ability in HCT-116 cells^[1].
TREM2-IN-1 (1 μM, 24 h) remarkably inhibits the expression of TREM2 in the THP-1-derived macrophages^[1].

IC₅₀ (μM) of TREM2-IN-1 at 72 h against different cell lines^[1]

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

TREM2-IN-1 (1.5 mg Pt per kg, treat, a single dose for 15 days) effectively inhibits the growth of tumor with low general toxicity in C57BL/6 mice models bearing MC38 murine colorectal cancer^[1].

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

1164.12

C₄₆H₆₈N₂O₂₀Pt

2000236-36-0

Solid

White to off-white

O=C(O[C@@H]1[C@H](C)[C@@](CC[C@@H](C)[C@]2([H])CC[C@](OO3)(C)O4)([H])[C@@]23[C@]4([H])O1)CCC(O[Pt]5(OC6=O)(OC6=O)(OC(CCC(O[C@@H]7[C@H](C)[C@@](CC[C@@H](C)[C@]8([H])CC[C@]9(C)O%10)([H])[C@@]8(OO9)[C@]%10([H])O7)=O)=O)[NH2][C@H](CCCC%11)[C@@H]%11[NH2]5)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Yang T, et al. Platinum-Based TREM2 Inhibitor Suppresses Tumors by Remodeling the Immunosuppressive Microenvironment. Angew Chem Int Ed Engl. 2023 Jan 9;62(2):e202213337.  [Content Brief]