signal transducer and activator of transcription

The signal transducer and activator of transcription 6 fragments is a peptide with the sequence H2N-Ser-Tyr-Trp-Ser-Asp-Arg-Leu-Ile-Ile-OH, MW= 1152.3.

STAT3-IN-3 is a potent and selective signal transducer inhibitor and transcription 3 (STAT3) activator.

7-Bromohept-1-yne是一种PROTAC Linker，可用于合成AK-1690,一种STAT6（Signal transducer and activator of transcription 6） PROTAC降解物。

DB-381831是一种有机磷化合物，具有复杂的分子结构，包含苯并噻吩环、羧基、二乙氧基磷酰基和二氟甲基基团，具有作为重要的中间体或试剂的潜力。DB-381831参与合成了AK-2292，一种STAT5（Signal transducer and activator of transcription 5）小分子降解物。

STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) 是一种用于降解信号转导及转录活化因子 3 (STAT3) 的PROTAC分子。它在HeLa细胞和MCF-7细胞中的IC50值分别为1335 nM和1973 nM，具有抗肿瘤活性。该化合物通过与STAT3的DNA结合域结合，并招募E3连接酶VHL形成复合物，促进STAT3的泛素化和蛋白酶体降解。此外，STAT3-D11-PROTAC-VHL 能抑制肿瘤细胞的生长，诱导细胞周期停滞和凋亡 (apoptosis)，并抑制肿瘤的免疫逃逸。

STAT3/AKT-IN-1 是一种同时抑制信号转导子和转录激活子 3 (STAT3) 以及蛋白激酶 B (AKT) 信号通路的双重抑制剂，具备抗肿瘤活性，并可以诱导 SGC-7901 细胞凋亡 (apoptosis)。

HJC0149 is a potent orally bioavailable signal transducer and activator of transcription 3 inhibitor.

HJC0416 is a potent orally bioavailable signal transducer and activator of transcription 3 inhibitor.

CAY10763 is a dual inhibitor of indolamine 2,3-dioxygenase 1 (IDO1; IC50= 46 nM) and STAT3 activation.1It binds to STAT3 (Kd= 530 nM) and selectively reduces the levels of STAT3 phosphorylated at the tyrosine in position 705 (STAT3Y705) over phosphorylated STAT3S727, STAT1, and STAT5 in SKOV3 cells when used at a concentration of 500 nM. It also inhibits STAT3 nuclear translocation in SKOV3 cells. CAY10763 is cytotoxic to HCT116, SKOV3, A549, and HepG2 cancer cells (IC50s = 37, 28, 33, and 12 nM, respectively). It reduces tumor growth in B16/F10 mouse melanoma and HepG2 mouse xenograft models when administered at doses of 100 and 10 mg/kg, respectively. 1.Huang, R., Jing, X., Huang, X., et al.Bifunctional naphthoquinone aromatic amide-oxime derivatives exert combined immunotherapeutic and antitumor effects through simultaneous targeting of indoleamine-2,3-dioxygenase and signal transducer and activator of transcription 3J. Med. Chem.63(4)1544-1563(2020)

HJC0152 hydrochloride (HJC0152) 是一种信号转导和转录激活因子 3的抑制剂。

Brivudine monophosphate is a phosphate ester of Brivudine. Brivudine, also known as bromovinyl-deoxyuridine, is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator of transcription 3), which may result in the downregulation of vascular endothelial growth factor (VEGF). BVDU has also been found to inhibit the upregulation of chemoresistance genes (Mdr1 and DHFR) during chemotherapy.

Ganoderic acid A 能够抑制 JAK-STAT3信号通路，也能抑制细胞增殖，存活率和 ROS。 它对人骨肉瘤 HOS 和MG-63细胞具有增殖抑制、凋亡和侵袭抑制作用。

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Falbikitug 是一种靶向白血病抑制因子（LIF）的人源化IgG1单克隆抗体。它通过特异性阻断糖蛋白130（gp130）辅助受体与LIF受体（LIFR）亚基（gp190）的结合来抑制下游信号传导，从而阻止信号转导和转录激活因子3（STAT3）的磷酸化，可以用于研究晚期实体瘤。

Manassantin B is a potent inhibitor of NF-κB activation by the suppression of transciptional activity of RelA/p65 subunit of NF-κB. It also possesses anti-EBV lytic replication activity. Manassantin B inhibits interleukin-6-induced signal transducer and activator of transcription 3 activation in Hep3B cells, it has potential as a potent anti-inflammatory drug for use in pathological processes such as sepsis or acute lung injury. Manassantin B exerts antifibrotic activity in HSC-T6 cells, in part, via inhibition of cell proliferation and decrease of collagen production.

Boscialin can inhibit signal transducer and activator of transcription 1 translocation at a concentration of 10 uM.