SHP2 Inhibitor

SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC₅₀ of 23 nM.

3-Azetidinemethanol hydrochloride, an intermediate, can be used in the synthesis of SHP2 inhibitor.

JAB-3068 (SHP2-IN-6) hydrochloride is a potent SHP2 inhibitor with an IC₅₀ of 25.8 nM. JAB-3068 hydrochloride is extracted from patent WO2017211303A1, compound 7.

SHP2-IN-9 is a specific SHP2 inhibitor (IC₅₀ =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo.

NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC₅₀ values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).

LYP-IN-1 is a potent, selective and specific LYP inhibitor with a K_i and an IC₅₀ of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC₅₀=5 μM) and SHP2 (IC₅₀=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders. LYP-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

SHP2-IN-13 is a highly selective and orally active SHP2 “tunnel site” allosteric inhibitor with an IC50 of 83.0 nM. SHP2-IN-13 has the potential for cancers bearing RTK oncogenic drivers and SHP2-related diseases research.

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.

Ellagic acid (Standard) is the analytical standard of Ellagic acid. This product is intended for research and analytical applications. Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC50 of 40 nM and a Ki of 20 nM.

SHP2-IN-37 (compound C5) is a potent and selective SHP2 allosteric inhibitor with an IC₅₀ of 0.023 μM. SHP2-IN-37 exhibits antiproliferative effect on KYSE-520 and MV-411 cells with IC₅₀s of 6.97 and 0.67 μM, respectively

SHP2-IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC₅₀ of 3 nM.

IACS-15414 is a potent and orally bioavailable SHP2 inhibitor with an IC₅₀ value of 122 nM.

SHP389 is an allosteric SHP2 inhibitor, with an IC₅₀ of 36 nM for both SHP2 and p-ERK.

PHPS1 sodium is a potent and selective Shp2 inhibitor with K_is of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.

BPDA2 is a highly selective and competitive active site SHP2 inhibitor with IC₅₀s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes.

II-B08 is a reversible and noncompetitive SHP2 inhibitor (IC₅₀: 5.5 μM, 15.7, 14.3 μM for SHP2, SHP1, PTP1B). II-B08 can be used for cancer research.

SHP2/HDAC-IN-1 is a dual allosteric SHP2/HDAC inhibitor with IC₅₀ values of 20.4 nM (SHP2) and 25.3 nM (HDAC1) respectively. SHP2/HDAC-IN-1 triggers efficient antitumor immunity by activating T cells, enhancing the antigen presentation function and promoting cytokine secretion. SHP2/HDAC-IN-1 can be used in the research of cancer immunoresearch.

GS-493 is a selective protein tyrosine phosphatase SHP2 (PTPN11) inhibitor with an IC₅₀ of 71 nM. GS-493 is 29- and 45-fold more active toward SHP2 than related SHP1 and PTP1B. GS-493 blocks cellular motility and growth of cancer cells. Antitumor activity.

SHP2-IN-39 (Example 63) is an inhibitor of SHP2 with an IC₅₀ of 0.007 μM. SHP2-IN-39 can be used in the research of cancer.

YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC₅₀=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells.