STAT Inhibitor

Fludarabine (Standard) is the analytical standard of Fludarabine. This product is intended for research and analytical applications. Fludarabine (NSC 118218) is a DNA synthesis inhibitor and a fluorinated purine analogue with antineoplastic activity in lymphoproliferative malignancies. Fludarabine inhibits the cytokine-induced activation of STAT1 and STAT1-dependent gene transcription in normal resting or activated lymphocytes.

STX-0119 (Standard) is the analytical standard of STX-0119 (HY-103692). This product is intended for research and analytical applications. STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC₅₀ of 74 μM.

Ritlecitinib (Standard) is the analytical standard of Ritlecitinib (HY-100754). This product is intended for research and analytical applications. Ritlecitinib (PF-06651600) is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC50=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC50 >10 μ M). Ritlecitinib rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

Tofacitinib-¹³C (Tasocitinib-¹³C; CP-690550-¹³C) is the ¹³C-labeled Tofacitinib (HY-40354). Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1/JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury.

GYY4137 (GMP) is the GMP-grade version of GYY4137 (HY-107632). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. GYY4137 (GMP) is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GYY4137 (GMP) can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.

Pimozide-d₅ N-Oxide is the deuterium labeled Pimozide. 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 Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.

CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC₅₀ values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML).

inS3-54-A26 is a STAT3 inhibitor. inS3-54-A26 has a toxic IC₅₀ of 4.0 μM for non-cancerous lung fibroblasts.

L002 (Standard) is the analytical standard of L002 (HY-100671). This product is intended for research and analytical applications. L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.

Graveoline (Standard) is the analytical standard of Graveoline (HY-12538). This product is intended for research and analytical applications. Graveoline (Rutamine) is an orally active alkaloid with various activities such as antifungal, antiparasitic, anti-inflammatory, and antitumor effects. Graveoline can induce tumor cell apoptosis and autophagy through a reactive oxygen species-mediated pathway. Graveoline has an MIC of 500 μg/mL for Candida albicans. Graveoline can be used in the research of various diseases such as tumors and liver injury.

Pexmetinib hydrochloride (ARRY-614 hydrochloride) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib hydrochloride binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib hydrochloride inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib hydrochloride can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

TPCA-1 (Standard) is the analytical standard of TPCA-1 (HY-10074). This product is intended for research and analytical applications. TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

Homoharringtonine (Standard) is the analytical standard of Homoharringtonine. This product is intended for research and analytical applications. Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

RSVA405 (Standard) is the analytical standard of RSVA405 (HY-103238). This product is intended for research and analytical applications. RSVA405 is a potent, orally active activator of AMPK, with an EC₅₀ of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.

TT-301 hydrochloride is a small-molecule immunomodulator capable of penetrating the blood-brain barrier. TT-301 hydrochloride exerts neuroprotective effects by binding to IL-1β, downregulating STAT3 expression, and modulating the JAK-STAT signaling pathway, thereby inhibiting microglial activation and the release of proinflammatory mediators, and alleviating neuroinflammation and brain edema. TT-301 hydrochloride is used in research on traumatic brain injury, intracerebral hemorrhage, subarachnoid hemorrhage, muscle wasting and atrophy, and periodontal disease.

DETD-35 is an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways, which promotes cancer cell apoptosis (Apoptosis) and reduces cancer cell resistance to Vemurafenib (HY-12057). The IC₅₀ values of DETD-35 against wild-type and mutant melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c are 2.7, 6.0, 3.9, 3.1, and 2.5 μM, respectively. DETD-35 holds promise for research in the field of anti-melanoma therapy.

Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

NT157 (Standard) is the analytical standard of NT157 (HY-100037). This product is intended for research and analytical applications. NT157 (Tyrphostin NT157) is a selective IRS-1/2 inhibitor that induces Ser-phosphorylation and consequently the degradation of IRS-1/2. NT157 (Tyrphostin NT157) is a first-in-class anti-cancer agent that also targets Stat3 signaling pathway.

(E/Z)-AG490 (Standard) is the analytical standard of (E/Z)-AG490 (HY-107459). This product is intended for research and analytical applications. (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine K_inase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

MK256 is an orally active, selective CDK8 inhibitor and CDK19/cyclin C inhibitor with IC₅₀ values of 2.5 nM and 3.3 nM, respectively. MK256 downregulates phosphorylated STAT1 ^(S727), STAT5 ^(S726), MCL-1 mRNA and CCL2 mRNA. MK256 exhibits anti-tumor activity in acute myeloid leukemia. MK256 can be used for the research of acute myeloid leukemia.