STAT Inhibitor

MMP-2/9-IN-2 (Compound 6k) is a MMP-2 and MMP-9 inhibitor, with IC₅₀ values of 29.27 and 24.87 μM respectively. MMP-2/9-IN-2 exhibits good selective toxicity against multiple human hepatoma cell lines. MMP-2/9-IN-2 induces cell cycle arrest and apoptosis, significantly inhibits cell migration and invasion. MMP-2/9-IN-2 inhibits the phosphorylation of the STAT3 signaling pathway. MMP-2/9-IN-2 shows strong anti-tumor activity in a nude mouse xenograft model of HepG2 liver cancer cells.

STAT3-IN-28 (compound 18) is a STAT3 inhibitor. STAT3-IN-28 can inhibit the activation of microglia and has anti-neuroinflammatory effects. STAT3-IN-28 can cross the blood-brain barrier.

JAK2-IN-9 is an orally active selective JAK2 inhibitor with a human IC₅₀ of 5 nM. JAK2-IN-9 inhibits JAK2 kinase activity, blocks JAK2 phosphorylation, and suppresses the activation of the downstream JAK2-STAT signaling pathway. JAK2-IN-9 inhibits the phosphorylation of STAT3, STAT5 and AKT in cancer cells. JAK2-IN-9 induces cancer cell apoptosis (apoptosis) and cell cycle arrest. JAK2-IN-9 can be used for the research of myeloproliferative neoplasms.

Cirsilineol (Standard) is the analytical standard of Cirsilineol. This product is intended for research and analytical applications. Cirsilineol, a natural flavone compound, selectively inhibits IFN-γ/STAT1/T-bet signaling in intestinal CD4+ T cells. Cirsilineol has potent immunosuppressive and anti-tumor properties. Cirsilineol significantly ameliorates trinitro-benzene sulfonic acid (TNBS)-induced T-cell-mediated experimental colitis in mice.

MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer.

Cappariloside A is a larvicide that exhibits larvicidal activity against Aedes aegypti larvae and reduces larval glutathione-S-transferase activity. Cappariloside A also possesses antiviral activity, decreases the level of phosphorylated STAT1 in cells, inhibits the replication of influenza viruses H1N1, H3N2, PIV3 and ADV, and downregulates the expression of IL-6, IP-10, MIG, RANTES/CCL-5, IFN-β and IL-29. Cappariloside A suppresses the inflammatory response induced by mouse lung-adapted influenza virus strains. Cappariloside A can be used in studies related to larvicidal applications and influenza virus infection.

KW-2478 hydrochloride is an HSP90 inhibitor (IC₅₀ = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer.

PROTAC ALK degrader-3 is an orally active ALK PROTAC degrader with a DC₅₀ of 119.33 nM in Karpas 299 cells. PROTAC ALK degrader-3 induces the degradation of ALK fusion proteins via the ubiquitin-proteasome system. PROTAC ALK degrader-3 induces NPM-ALK degradation and inhibits the expression of p-ALK and p-STAT3. PROTAC ALK degrader-3 inhibits cancer cell proliferation and suppresses the growth of xenografts in vivo. PROTAC ALK degrader-3 can be used for the research of ALK-positive cancers (e.g., anaplastic large cell lymphoma).

EGFR/STAT3-IN-1 (Compound 5k) is a dual inhibitor of EGFR/STAT3 with IC₅₀ values for EGFR and STAT3 are 41 and 3.34 nM, respectively. EGFR/STAT3-IN-1 has antitumor activity.

STAT3-IN-34 (Compound 15E) is an inhibitor for STAT3, and inhibits the nuclear translocation and transcriptional regulator activity of STAT3. STAT3-IN-34 inhibits the proliferation of cell HaCaT with IC₅₀ of 0.008 μM. STAT3-IN-34 inhibits IL-17A expression and ameliorates Imiquimod (HY-B0180)-induced psoriasis in mice.

FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC₅₀s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML).

Z169667518 is a ligand of IL-6. Z169667518 can inhibit IL-6-induced STAT3 reporter activity with an IC₅₀ of 2.7 µM. Z169667518 can be used in the research of IL-6-related diseases.

PROTAC RET Degrader 2 is a RET degrader with a target IC₅₀ of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.

Saikosaponin D (Standard) is the analytical standard of Saikosaponin D. This product is intended for research and analytical applications. 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.

JAK1-IN-21, biotin-conjugated isoxazole derivative, is a JAK1 inhibitor. JAK1-IN-21 directly engages and stabilizes JAK1, reduces the phosphorylation of JAK1, STAT1 and AKT, induces apoptotic marker cleavage (PARP, Caspase-3, Caspase-7) and exhibits broad-spectrum antiproliferative activity against cancer cells. JAK1-IN-21 can be used for the study of liver cancer, prostate cancer, and breast cancer.

STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (K_d: 60.03 μM) and CAIX (IC₅₀: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC).

SHN7 is a selective HDAC1/HDAC6 inhibitor, NQO1 substrate and ROS inducer, with an IC₅₀ of 30 nM against HDAC1 and an IC₅₀ of 10 nM against HDAC6. SHN7 inhibits STAT3 with a K_d of 8.9 μM. SHN7 arrests the cell cycle at the G2/M phase and induces Apoptosis. SHN7 exhibits anti-tumor effects in triple-negative breast cancer (TNBC) xenograft models. SHN7 can be used for the research of triple-negative breast cancer.

STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase.

NTZ-24 is a selective STAT3 pathway inhibitor. NTZ-24 suppresses STAT3 phosphorylation at Tyr705, blocks STAT3-DNA interaction, and downregulates the levels of STAT3 downstream target proteins. NTZ-24 induces cell-cycle arrest and promotes apoptosis in cancer cells. NTZ-24 exerts significant antiproliferative activity against HeLa cells (IC₅₀ = 3.3 μM). NTZ-24 can be used for the research of cervical cancer.

DG-8 is a potent inhibitor of STAT3-dependent transcription (IC₅₀ 0.98 μM). DG-8 is a fluorescent probe that contains a fluorescent dansyl moiety.