2. Signalwege
  3. Protein Tyrosine Kinase/RTK
  4. SHP2

SHP2

Src homology phosphatase 2; PTPN11

Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a 593 amino acid classical non-receptor protein tyrosine phosphatase (PTP). SHP2 is involved in diverse signalling pathways such as RAS-MAPK, PI3K-AKT, JAK-STAT and PD-1/PD-L1. Besides, SHP2 negatively regulates the activation of recombinant NLRP3 (NLR family, pyrin domain containing protein 3) inflammasome via mitochondrial homeostasis. SHP2 has been regarded as an extremely attractive target for human diseases therapies, particular in cancer.

Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-169111
    SHP2-IN-32
    		Inhibitor
    SHP2-IN-32 (compound C6) is an orally active, allosteric SHP2 inhibitor with an IC50 value of 0.13 nM. SHP2-IN-32 exhibits antitumor activity.
    SHP2-IN-32
  • HY-150609
    SHP2/CDK4-IN-1
    		Inhibitor
    SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research.
    SHP2/CDK4-IN-1
  • HY-115527
    SHP244
    		Inhibitor
    SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC50 value for SHP2WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers.
    SHP244
  • HY-162355
    SHP2-IN-27
    		Inhibitor
    SHP2-IN-27 (compound 28) is an allosteric inhibitor of tyrosine phosphatase SH2.
    SHP2-IN-27
  • HY-170877
    SHP2-IN-35
    		Inhibitor
    SHP2-IN-35 (Compound 3f) is the inhibitor for SHP2. SHP2-IN-35 exhibits antiproliferative activity in cancer cells RKO, SW480 and CT26 with IC50 of 5.72 μM, 3.71 μM and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the cell cycle associated gene expressions, and induces mitochondrial-related autophagy. SHP2-IN-35 inhibits the expression of certain cytokines and chemokines in the tumor microenvironment (TME), thereby regulating the tumor progression.
    SHP2-IN-35
  • HY-125257
    SHP2 inhibitor LY6
    		Inhibitor
    SHP2 inhibitor LY6 (LY6) is a selective SHP2 inhibitor with an IC50 of 9.8 μM, showing 7-fold selectivity over SHP1. SHP2 inhibitor LY6 inhibits SHP2-mediated cell signaling pathways and suppresses cell proliferation. SHP2 inhibitor LY6 elicits induces apoptosis and G2/M cell cycle arrest in lung cancer cells. SHP2 inhibitor LY6 can be used for the research of B cell acute lymphoblastic leukemia, acute myeloid leukemia, and lung cancer.
    SHP2 inhibitor LY6
  • HY-130631
    SHP2-IN-5
    		Inhibitor
    SHP2-IN-5 (compound 1) is an inhibitor of SHP2 (IC50: 97 nM). SHP2 is a non-receptor protein tyrosine phosphatase associated with cell growth and proliferation. SHP2-IN-5 has the potential to inhibit cancer and SHP2-related human diseases.
    SHP2-IN-5
  • HY-139467
    PF-04577806
    		Inhibitor
    PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.
    PF-04577806
  • HY-161360
    LXQ-217
    		Inhibitor
    LXQ-217 is an oral active SHP2 inhibitor with the IC50 of 2.01 μM. LXQ-217 induces apoptosis and inhibits cell growth in vivo and in vitro.
    LXQ-217
  • HY-155098
    CNBCA
    		Inhibitor
    CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study.
    CNBCA
  • HY-175803
    SHP2-IN-44
    		Inhibitor
    SHP2-IN-44 (Compound 26) is an allosteric and orally active SHP2 inhibitor with an IC50 of 27 ?nM. SHP2-IN-44 also inhibits ERK phosphorylation (IC50 of 299 ?nM) without off-target hERG activity. SHP2-IN-44 has a broad-spectrum anticancer activity, such as juvenile myelomonocytic leukemia, neuroblastoma and breast cancer. SHP2-IN-44 can be used for Noonan syndrome, LEOPARD syndrome and cancers research.
    SHP2-IN-44
  • HY-157888
    SHP2-IN-26
    		Inhibitor
    SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC50 value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity.
    SHP2-IN-26
  • HY-139466
    PF-03622905
    		Inhibitor
    PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases.
    PF-03622905
  • HY-155273
    SHP2-IN-17
    SHP2-IN-17 (compound 192) is a SHP2 inhibitor with an IC50 value of 2 nM. SHP2-IN-17 can be used for glioblastoma research.
    SHP2-IN-17
  • HY-162233
    SHP2-IN-25
    		Inhibitor
    SHP2-IN-25 (Compound 6) is a SHP2 allosteric inhibitor, with an IC50 of 225 nM. SHP2-IN-25 can be used for the research of cancer.
    SHP2-IN-25
  • HY-172916
    LC-SF-14
    		Inhibitor
    LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR (IC50 values are 71.6 and 8.9 nM, respectively). LC-SF-14 inhibits FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation. LC-SF-14 inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). LC-SF-14 has antitumor activity in the SNU-16 xenograft mouse model. LC-SF-14 can be used in FGFR2-driven gastric cancer research.
    LC-SF-14
  • HY-173573
    TK-684
    		Inhibitor
    TK-684 is a potent and selective allosteric SHP2 inhibitor with IC50 values of 2.1, ＞1000 nM for SHP2WT, SHP22PTP, respectively. TK-684 inhibits cell proliferation and induces apoptosis. TK-684 decreases the protein expression of p-AKT, p-ERK.
    TK-684
  • HY-172454
    SHP2-IN-36
    		Inhibitor
    SHP2-IN-36 (Compound B8) is an allosteric inhibitor of SHP2, with an IC50 value of 9.0 nM. In addition, its IC50 for p-ERK is 40 nM. SHP2-IN-36 also exhibited significant antitumor activity in the KYSE520 xenograft mouse model. SHP2-IN-36 can be used for research in the field of anti-tumor .
    SHP2-IN-36
  • HY-183936
    SDUY127
    		Inhibitor
    SDUY127 is a bivalent SHP2 inhibitor with an IC50 value of 16 nM. SDUY127 binds simultaneously to the tunnel allosteric site and latch allosteric site of SHP2 at a 1:1 stoichiometric ratio, stabilizes the protein in an inactive conformation, and induces sustained inhibition of the MAPK signaling pathway. SDUY127 can be used in research related to leukemia and hepatocellular carcinoma.
    SDUY127
  • HY-155275
    SHP2-IN-19
    SHP2-IN-19 (compound 183) is a SHP2 inhibitor with an IC50 value of 3 nM. SHP2-IN-19 can be used for glioblastoma research.
    SHP2-IN-19
Art. -Nr. Produktname / Synonyms Application Reactivity