SHP1 Inhibitor

TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC₅₀ of 40 nM.

SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.

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).

BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8⁺ T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields.

PHPS1 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.

IB15C is an ILT3 (LILRB4) inhibitor with a human K_d of 0.92 μM. IB15C binds to a specific ILT3 pocket, disrupts ApoE interaction, and interferes with downstream inhibitory signaling pathways. IB15C reduces SHP1 and SHP2 phosphorylation, suppresses pro-inflammatory cytokine secretion, enhances amyloid uptake, and attenuates NF-κB activation. IB15C can be used for the research of alzheimer's disease.

Diorcinol is a potent SHP1 inhibitor with an IC₅₀ value of 0.96 μM. Diorcinol can be isolated from Aspergillus sydowii. Diorcinol has good blood-brain barrier penetration and can be used for diabetes research.

SHP1 activator 1 (Compound 3n) is an activator for src homology-2 domain-containing protein tyrosine phosphatase 1(SHP1) with an EC₅₀ of 17.66 μM. SHP1 activator 1 inhibits the proliferation of ABC-DLBCL cells, induces apoptosis by inhibiting STAT3 signaling pathway. SHP1 activator 1 emitts blue and green fluorescence signalis in MDA-MB-231 cell, and can be used as a cell imaging agent.

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.

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.

Sydowimide A is a potent inhibitor of Src homology region 2 domain-containing phosphatase-1 (SHP1), T-cell protein tyrosine phosphatase (TCPTP) and leukocyte common antigen (CD45), with IC₅₀ values of 1.5, 2.4 and 18.83 μM, 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.

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.

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.

SHP1-IN-1 (compound 5p) is a fluorescent probe for the protein tyrosine phosphatase SHP1 containing the Src homology 2 domain. SHP1-IN-1 has SHP1 inhibitory activity, selectivity for Fe³⁺ ions and good fluorescence properties. SHP1-IN-1 exhibits aggregation post-quenching (ACQ) effect, good interference immunity and low detection limit (5.55 μM).

SHP1‑IN‑2 is a selective and orally active SHP1 inhibitor. SHP1‑IN‑2 covalently binds to Cys480 of SHP1. SHP1‑IN‑2 elicits potent antitumor immunity and suppresses syngeneic tumor growth. SHP1‑IN‑2 blocks tumor progression in a svngeneic cancer model by activating natural killer cells and cytotoxic CD8^＋ T cells, along with reduced T cel l. SHP1‑IN‑2 can be used for cancer‑related research.

OSE-279 is a high-affinity humanized monoclonal bivalent antibody targeting PD-1, the recommended isotype control is HY-P99003. OSE-279 blocks PD-1 ligand binding, inhibits PDL1-induced SHP1 phosphorylation, restores T cell activation, and promotes reactivation of primary T cell effector functions. OSE-279 binds hFcRn receptor, predicts long half-life, induces CD4 and CD8 T cell proliferation, and promotes interleukin 2 and interferon gamma secretion. OSE-279 can be used for the research of advanced malignancies, colon cancer, hepatocarcinoma, mesothelioma.