shp2 in-1

SHP2 IN-1 is an allergic SHP2 (PTPN11) inhibitor(IC50 : 3 nM).

SHP2 CDK4-IN-1 (compound 10) is a dual inhibitor targeting SHP2 and CDK4, with oral activity and high potency, showing IC50 values of 4.3 nM for SHP2 and 18.2 nM for CDK4. It induces G0 G1 arrest, inhibits proliferation of TNBC cell lines, and demonstrates significant antitumor efficacy in the EMT6 syngeneic mouse model. This compound is valuable for research into triple-negative breast cancer (TNBC) [1].

SHP2 HDAC-IN-1, a dual allosteric inhibitor targeting SHP2 and HDAC, exhibits potent inhibitory effects with IC 50 values of 20.4 nM (SHP2) and 25.3 nM (HDAC1), respectively. This compound activates T cells, enhances antigen presentation, and promotes cytokine secretion, facilitating efficient antitumor immunity. It holds potential for cancer immunotherapy research.

BPDA2 is a highly selective and competitive SHP2 inhibitor, exhibiting IC50 values of 92.0 nM for SHP2, and 33.39 μM and 40.71 μM for SHP1 and SHP1B, respectively. This compound effectively downregulates mitogenic and cell survival signaling, including reducing expression of receptor tyrosine kinases (RTKs). Furthermore, BPDA2 suppresses SHP2-mediated signaling, leading to the inhibition of breast cancer cell phenotypes [1].

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive, and orally active pan-PTP (protein tyrosine phosphatases) inhibitor with insulin-mimicking effects and anti-diabetic properties. BMOV is a potent insulin sensitizer and has been shown to improve cardiac dysfunctions in diabetic models. BMOV inhibits HCPTPA, PTP1B, HPTPβ, and SHP2 with IC50s of 126 nM, 109 nM, 26 nM, and 201 nM, respectively [1][2].

LYP-IN-1 is a powerful LYP inhibitor that demonstrates high potency, selectivity, and specificity, with a Ki of 110 nM and an IC 50 of 0.259 μM. Beyond its primary target, LYP-IN-1 also exhibits selectivity towards a wide range of PTPs, including SHP1 (IC 50 = 5 μM) and SHP2 (IC 50 = 2.5 μM). Additionally, LYP-IN-1 demonstrates remarkable efficacy in T- and mast cells, making it a valuable tool for investigating autoimmune disorders.

SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2, inducing its degradation and resulting in cell apoptosis; it shows promising potential for studying diseases associated with SHP2.

SHP2-IN-9 is a potent inhibitor (IC50 = 1.174 μM) specifically targeting the SHP2 protein, displaying improved penetration across the blood-brain barrier. It exhibits a remarkable 85-fold selectivity for SHP2 over SHP1. By inhibiting SHP2-mediated cell signal transduction and impairing cancer cell proliferation, SHP2-IN-9 effectively suppresses the growth of both cervix cancer tumors and glioblastoma in vivo [1].

NSC-87877 disodium (NSC87877) is a cell-permeable inhibitor of both SHP-1 and SHP-2 with IC50 values of 355 and 318 nM respectively. It also inhibits EGF-induced Erk1 2 activation in HEK293 cells and significantly reduces MDA-MB-468 cell viability proliferation.

Trichomide A, a natural cyclodepsipeptide, serves as a potent activator of SHP2. This compound exhibits immunosuppressive activity against activated T lymphocyte-mediated immune responses in Con A-activated T cells, highlighting its potential utility in researching immune-related skin diseases [1].

CD31 TFA, also known as platelet endothelial cell adhesion molecule-1 (PECAM-1), functions as the specific receptor for Clostridium perfringens beta-Toxin (CPB) in endothelial cells. It is recognized as an ER-MP12 antigen and plays a pivotal role in connecting mechanical stress, metabolism, and inflammation. Additionally, the CD31 TFA peptide facilitates the phosphorylation of CD31 ITIM 686 and SHP2, further inhibiting TCR-induced T-cell activation [1]-[5].

SHP2-IN-5 (compound 1) is a non-receptor protein tyrosine phosphatase inhibitor targeting SHP2, with an IC50 value of 97 nM, and is associated with regulating cell growth and proliferation. This compound exhibits potential therapeutic properties in inhibiting cancer and other SHP2-related human diseases [1].

SHP2-IN-22, a potent SHP2 allosteric inhibitor, exhibits an IC50 value of 17.7 nM and effectively suppresses proliferation, migration, and invasion in MIA PaCa-2 pancreatic cancer cells. This compound is utilized in the study of Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research [1].

SHP2-IN-14 (compound 27) is a potent, orally active allosteric inhibitor of SHP2 with an IC50 of 7 nM, exhibiting strong anti-tumor activity, inhibiting tumor progression in NCI-H358 tumor-bearing mice, and demonstrating favorable pharmacokinetic properties and safety [1].

CNBCA, a selective and potent competitive inhibitor of the SHP2 enzyme, exhibits an IC50 value of 0.87 μM. It binds to the full-length SHP2, effectively inhibiting its enzyme activity, as well as impeding pAkt and pERK1 2. Furthermore, CNBCA suppresses the proliferation of BT474 and MDA-MB468 cells, indicating potential utility in breast cancer research [1].

SHP2-IN-16 (compound 222) is a potent SHP2 inhibitor with an IC50 of 1 nM, applicable in glioblastoma research [1].

YF704 (compound 4w), a selective allosteric inhibitor of SHP2, exhibits antiproliferative effects and induces apoptosis in cancer cells with an IC50 of 0.25 μM. Furthermore, it downregulates Erk1 2 and Akt phosphorylation levels in cancer cells [1].

SHP2-IN-21 (compound 208) is an SHP2 inhibitor with an IC50 of 3 nM, used in glioblastoma research [1].

SHP2-IN-20 (compound 193), a potent SHP2 inhibitor, exhibits an IC50 of 3 nM, making it suitable for glioblastoma research [1].

SHP2-IN-19 (compound 183) is a SHP2 inhibitor with potent activity, demonstrated by an IC50 of 3 nM, and is used in glioblastoma research [1].

SHP2-IN-18 (compound 183) is a potent SHP2 inhibitor with an IC50 of 3 nM, suitable for glioblastoma research [1].

SHP2-IN-17 (compound 192) is a potent SHP2 inhibitor with an IC50 of 2 nM, showing potential for glioblastoma research [1].

LXQ-217 is an orally active SHP2 inhibitor with an IC50 of 2.01 μM, inducing apoptosis and inhibiting cell growth both in vivo and in vitro [1].

SHP2-IN-23 (compound 30) is an orally active inhibitor of SHP2, exhibiting potent activity with an IC50 value of 38 nM and demonstrating favorable pharmacokinetic profiles and in vivo efficacy. Additionally, it robustly inhibits ERK phosphorylation, achieving an IC50 of 5 nM [1].