STAT3 Inhibitor

Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5.

SD-36 is a potent STAT3 PROTAC degrader with a K_d of 44.4 nM and a K_i of 11 nM. SD-36 recruits the cereblon/culin 4A E3 ligase complex to mediate ubiquitination and proteasomal degradation of STAT3, inducing G1 phase cell cycle arrest and apoptosis. SD-36 is useful for research on acute myeloid leukemia, anaplastic large cell lymphoma, and hematopoietic and lymphoid malignancies.

Diosgenin, a steroidal saponin, can inhibit STAT3 signaling pathway. Diosgenin is an exogenous activator of Pdia3/ERp57. Diosgenin inhibits aortic atherosclerosis progression by suppressing macrophage miR-19b expression.

Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.

1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells.

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.

Sorafenib-d₃ (Donafenib) is the deuterated-labeled Sorafenib (HY-10201). Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.

Morusin is a prenylated flavonoid isolated from Morus alba Linn. with various biological activities, such as antitumor, antioxidant, and anti-bacteria property. Morusin could inhibit NF-κB and STAT3 activity.

SI-109 is a potent STAT3 SH2 domain inhibitor (K_i=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC₅₀=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.

SH-4-54 is a CNS-penetrant STAT inhibitor that binds to STAT3 and STAT5 with K_Ds of 300, 464 nM, respectively.

Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.

BP-1-102 is an orally available, small-molecule inhibitor of transcription factor Stat3, with an IC₅₀ of 6.8 μM.

Anti-IL11 Antibody (X203) (EnX203) is a human-derived IgG1, κ type antibody inhibitor, targeting to human IL-11. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

Anti-Mouse NK1.1 Antibody (PK136) is an anti-mouse NK1.1 IgG2a monoclonal antibody. Anti-Mouse NK1.1 Antibody (PK136) can deplete natural killer (NK) cells. Anti-Mouse NK1.1 Antibody (PK136) inhibits the JAK-STAT and NF-κB signaling pathways. Anti-Mouse NK1.1 Antibody (PK136) can be used for research on inflammation conditions such as non-alcoholic steatohepatitis (NASH).

STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC₅₀ values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis.

Guanosine 5'-diphosphate (GDP) sodium, 96% (HPLC) is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K⁺ channel. Guanosine 5'-diphosphate sodium, 96% (HPLC) is an iron mobilizer, which forms a complex with hepcidin to inhibit the hepcidin-ferroportin (FPN) interaction and modulates the IL-6/stat-3 pathway. Guanosine 5'-diphosphate sodium, 96% (HPLC) ameliorates the Turpentine-induced anemia of inflammation (AI) in mice when combined with FeSO₄. Guanosine 5'-diphosphate sodium, 96% (HPLC) can be used in the research of AI.

Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC₅₀s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis.

Alantolactone is a selective STAT3 inhibitor, with potent anticancer activity. Alantolactone induces apoptosis in cancer.

Anti-Mouse IL-6 Antibody (MP5-20F3) is an anti-mouse IL-6 IgG1 monoclonal antibody. Anti-Mouse IL-6 Antibody (MP5-20F3) reshapes the tumor microenvironment by blocking IL-6. Anti-Mouse IL-6 Antibody (MP5-20F3) can inhibit the STAT3 pathway and enhance T cell infiltration. Anti-Mouse IL-6 Antibody (MP5-20F3) can be used for researches on inflammation and infection conditions such as malignant pleural effusion (MPE).