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SHP2 protein degrader-2 (SHP2-D26) is a SHP2 protein PROTAC degrader. SHP2 protein degrader-2 reduces expression level of SHP2 in various cancer cells .
SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases .
SHP2 inhibitor LY6 (LY6) is potent and selective inhibitor of SHP2, with an IC50 of 9.8 µM. SHP2 inhibitor LY6 can inhibits SHP2-mediated cell signaling and proliferation .
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-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.
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 .
SHP2-D26 is a first, potent and effective SHP2 degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent .
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-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells .
SHP2-IN-22 is SHP2 allosteric inhibitor with an IC50 value of 17.7 nM. SHP2-IN-22 inhibits the proliferation, migration, and invasion of MIA PaCa-2 pancreatic cancer cells. SHP2-IN-22 can be used for Kirsten rat sarcoma viral oncogene (KRAS) mutant 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 .
SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC50=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC50=5 nM .
SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .
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 .
Vociprotafib (RMC-4630) is a SHP2 inhibitor, a phosphatase whose inhibition blocks activation of the RAS-RAF-MEK-ERK signaling pathway. Vociprotafib has antitumor activity [2].
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 .
PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively .
PHPS1 is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively .
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively [2].
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 .
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers .
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 .
SHP099 hydrochloride is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 hydrochloride inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 hydrochloride inhibits RAS-ERK signaling and inhibit tumor growth [2].
PB17-026-01 is a potent SHP2 allosteric inhibitor and shows the highest inhibitory activity with an IC50 value of 38.9?nM. PB17-026-01 can be used for the research of tumor .
SHP844 is a SHP2 inhibitor with the IC50 of 18.9 µM. SHP2 is a protein tyrosine phosphatase (PTP) that regulates tyrosine phosphorylation levels and is involved in cell proliferation, differentiation and survival .
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML) .
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases .
Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors .
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 .
NSC-87877 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)[2].
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)[2].
Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase. Sodium stibogluconate inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer [2].
Ellagic acid- 13C12 is 13 C-labeled Ellagic acid (HY-B0183). 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 [2].
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 .
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively .
LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki 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.
PTP Inhibitor IV is a protein tyrosine phosphatase (PTP) inhibitor that competitively inhibits DUSP14 phosphatase activity with an 50 of 5.21 μM . PTP Inhibitor IV inhibits SHP-2, PTP1B, PTP-ε, PTP Meg-2, PTP-σ, PTP-β, and PTP-μ with 50s of 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively [2].
Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN proteins. Thalidomide-NH-(CH2)2-NH2 TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules designed to synthesize small PROTAC molecules targeting SHP2 protein.
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
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 .
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases .
CD31 (PECAM-1) is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
CD31 (PECAM-1) TFA is platelet endothelial cell adhesion molecule-1, serves as the endothelial cell-specific receptor of clostridium perfringens b-Toxin (CPB). CD31 TFA is also an ER-MP12 antigen, acts as a linker between mechanical stress, metabolism and inflammation. CD31 TFA peptide is able to sustain phosphorylation of the CD31 ITIM686 and of SHP2 and to inhibit TCR-induced T-cell activation - .
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML) .
Cryptosporioptide A (Compound 3) is a pigment protein tyrosine phosphatase inhibitor derived from the insect-parasitic fungus Cordyceps gracilioides. Cryptosporioptide A inhibits PTP1B, SHP2, CDC25B, LAR and SHP1 enzymes with IC50 of 7.3, 5.7, 7.6, >50, 4.9 μg/mL, respectively .
SHP-2 Protein functions downstream of diverse receptor and cytoplasmic tyrosine kinases, participating in signal transduction from the cell surface to the nucleus. It positively regulates the MAPK pathway and dephosphorylates key proteins like GAB1, ARHGAP35, EGFR, ROCK2, CDC73, and SOX9. Additionally, SHP-2 dephosphorylates NEDD9/CAS-L to modulate cellular processes. SHP-2 Protein, Mouse (HEK293, His) is the recombinant mouse-derived SHP-2 protein, expressed by HEK293 , with C-His labeled tag. The total length of SHP-2 Protein, Mouse (HEK293, His) is 593 a.a., with molecular weight of ~65 kDa.
The SHP-2 protein is a key player downstream of the receptor and cytoplasmic protein tyrosine kinases, facilitating signal transduction from the cell surface to the nucleus. It actively regulates the MAPK pathway and dephosphorylates key substrates, including GAB1, ARHGAP35, EGFR, ROCK2 ("Tyr-722"), and CDC73. SHP-2 Protein, Human (T253M, Q257L, His) is the recombinant human-derived SHP-2 protein, expressed by E. coli , with N-6*His labeled tag and T253M, Q257L, , , mutation. The total length of SHP-2 Protein, Human (T253M, Q257L, His) is 592 a.a., with molecular weight of 70-75 kDa.
Ellagic acid- 13C12 is 13 C-labeled Ellagic acid (HY-B0183). 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 [2].
Phospho-SHP2 (Tyr542) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 68 kDa, targeting to Phospho-SHP2(Y542). It can be used for WB,ICC,IP assays with tag free, in the background of Mouse.
