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22

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13009	STAT3-IN-1	Apoptosis; STAT	Apoptosis; JAK/STAT signaling; Stem Cells
	STAT3-IN-1 是一种选择性的、口服有效的 STAT3的强效抑制剂，可诱导肿瘤细胞凋亡，其在 HT29 和MDA-MB 231 细胞中的IC50值分别为1.82 μM 和2.14 μM。
T4216	STAT5-IN-1 STAT5 Inhibitor	STAT	JAK/STAT signaling; Stem Cells
	STAT5-IN-1 (STAT5 Inhibitor) 是STAT5的抑制剂，对 STAT5β 亚型的IC50值为 47 μM。
T3708	BP-1-102	STAT	JAK/STAT signaling; Stem Cells
	BP-1-102 是可口服的转录因子Stat3小分子抑制剂，IC50值为 6.8 μM。
T78607	JAK-STAT-IN-1	JAK; STAT	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JAK-STAT-IN-1 是一种特异性 JAK-STAT 抑制剂，适用于研究自身免疫性疾病。
T9339	Stafia-1	STAT	JAK/STAT signaling; Stem Cells
	Stafia-1 是STAT5a 抑制剂，Ki 为 10.9 μM，IC50 为 22.2 μM。它与 STAT5b 和其他 STAT 家族成员相比，显示出高选择性。
T3049	TPCA-1 GW683965,IKK2 Inhibitor IV,TPCA1	Apoptosis; IκB/IKK; STAT	Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells
	TPCA-1 (TPCA1) 是一种选择性IKK-2抑制剂，IC50值为 17.9 nM。它也是反式激活、DNA 结合以及STAT3磷酸化的一种抑制剂。
T8478	SC-43	Apoptosis; Phosphatase; STAT	Apoptosis; JAK/STAT signaling; Metabolism; Stem Cells
	SC-43 是一种具有口服活性的SHP-1 (PTPN6)激动剂。它是Sorafenib 的衍生物，可抑制STAT3的磷酸化并诱导细胞凋亡，具有抗纤维化和抗癌作用。
T22424	1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea	Apoptosis; STAT	Apoptosis; JAK/STAT signaling; Stem Cells
	SC-1 是一种 Sorafenib 的衍生物，可抑制 STAT3磷酸化，通过依赖 SHP-1 的 STAT3失活诱导细胞凋亡，具有抗癌作用。
T9945	MNK8 3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione	STAT	JAK/STAT signaling; Stem Cells
	MNK8 (3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione) 是一种有效的STAT3抑制剂，降低STAT3与DNA 结合的能力，对肝癌细胞也有良好的生长抑制作用。
T1127	Beclometasone dipropionate Beclovent,Beclomethasone dipropionate,二丙酸倍氯米松,丙酸倍氯米松,Beconase,Vancenase	Glucocorticoid Receptor	Endocrinology/Hormones
	Beclometasone dipropionate (Vancenase) 是具有口服活性的糖皮质激素，具有抗炎和免疫抑制作用。它是Betamethasone 的前体药物，Betamethasone 是 LPS 诱导的炎症及 MMP 释放的抑制剂。
T24838	Stafib-1 Stafib 1,Stafib1	STAT	JAK/STAT signaling; Stem Cells
	Stafib-1 是一种特异性的 STAT5β 抑制剂，靶向 SH2 结构域，IC50 为 154 nM，Ki 为 44 nM。
T2600	AG490 Zinc02557947,Tyrphostin AG 490,AG 490,AG-490,Tyrphostin B42	EGFR; JAK; STAT; Autophagy	Angiogenesis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	AG490 (Tyrphostin B42) 是一种 EGFR 抑制剂，IC50为 0.1 μM。它对 EGFR 的选择性比 ErbB2 高 135 倍，还抑制 JAK2。
T35407	Ζ-Stat	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	ζ-Stat 是非典型的、特异性的PKC-ζ抑制剂，IC50为 5 μM。ζ-Stat 能够减少黑色素瘤细胞系的增殖并诱导细胞凋亡，在体外显示除抗肿瘤活性。
T1849	Momelotinib CYT11387,CYT387,LM-1149	Apoptosis; JAK; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	Momelotinib (LM-1149) 是一种 ATP 竞争性的 JAK1/JAK2抑制剂，IC50值分别为 11 nM/18 nM。
T18680	SD-36	Others	Others
	SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their transcriptional activity (IC50=10 nM). The compound, consisting of the STAT3 inhibitor SI-109, a linker, and a CRBN ligand Lenalidomide analog for E3 ubiquitin ligase[1], demonstrates significant anti-tumor effects and achieves complete, long-lasting tumor regression in mouse mod...
T26596	Allylpyrocatechol
	Allylpyrocatechol is an antioxidant. Allylpyrocatechol attenuates collagen-induced arthritis via attenuation of oxidative stress secondary to modulation of the MAPK, JAK/STAT, and Nrf2/HO-1 pathways.
T74800	HAT-SIL-TG-1&AT
	HAT-SIL-TG-1&AT 是一种 Janus 酪氨酸激酶 (JAK) 抑制剂，具有抗肿瘤作用。HAT-SIL-TG-1&AT 是缺氧激活的前药，可抑制肿瘤组织中的JAK-STAT 信号传导。HAT-SIL-TG-1&AT 在低氧条件下抑制 HEL 细胞增殖并下调磷酸化的STAT3/5。
T26895	BRD0476 BRD-0476,ML 187,ML187,ML-187,BRD 0476
	BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT
T75535	5-epi-Arvestonate A
	5-epi-Arvestonate A是一种从(Seriphidium transiliense)绢毛菊中提取的倍半萜化合物，能够通过激活(MITF)小眼相关转录因子和酪氨酸酶家族基因来促进黑色素的产生。此外，5-epi-Arvestonate A还能通过JAK/STAT信号通路，抑制永生化人角化细胞(HaCaT)中IFN-γ趋化因子的表达。
T77038	Interferon alfa
	Interferon alfa 是 I 型干扰素，可激活新基因，对靶细胞产生有效抗病毒和抗增殖活性。Interferon alfa 的信号传导需要 Stat1和 Stat2 的受体依赖性激活，形成异源二聚化 STAT。STAT 复合物与 DNA 结合蛋白 IRF-9 (p48) 结合并形成 ISGF-3 (IFN 刺激基因因子 3)。随后由 ISGF-3 进一步激活驱动基因，实现抗病毒功能。
T37265	15(R)-Lipoxin A4 15(R)-Lipoxin A4,AT-Lipoxin A4
	Lipid-derived lipoxins are produced at the site of vascular and mucosal inflammation where they down-regulate polymorphonuclear leukocyte recruitment and function. 15(R)-Lipoxin A4 (15(R)-LXA4) is derived from the aspirin-triggered formation of 15(R)-HETE from arachidonic acid. [1] [2] 15(R)-LXA4 inhibits LTB4-induced chemotaxis, adherence, and transmigration of neutrophils with twice the potency of LXA4 demonstrating activity in the nM range.[2] [3] The anti-inflammatory effects of aspirin may...
T68306	INCB16562
	INCB16562 is a novel, selective, and orally bioavailable small-molecule inhibitor of JAK1 and JAK2 markedly selective over JAK3. Treatment of myeloma cells with INCB16562 potently inhibited interleukin-6 (IL-6)-induced phosphorylation of STAT3. INCB16562 abrogated the protective effects of recombinant cytokines or bone marrow stromal cells and sensitized myeloma cells to cell death by exposure to dexamethasone, melphalan, or bortezomib. Oral administration of INCB16562 antagonized the growth of ...

化合物

Cat.No: T13009

Target: Apoptosis, STAT

Cat.No: T4216

Synonym: STAT5 Inhibitor

Target: STAT

Cat.No: T3708

Target: STAT

JAK-STAT-IN-1

Cat.No: T78607

Target: JAK, STAT

Cat.No: T9339

Target: STAT

Cat.No: T3049

Synonym: GW683965,IKK2 Inhibitor IV,TPCA1

Target: Apoptosis, IκB/IKK, STAT

Cat.No: T8478

Target: Apoptosis, Phosphatase, STAT

1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea

Cat.No: T22424

Target: Apoptosis, STAT

Cat.No: T9945

Synonym: 3-methyl-6-(naphthalen-1-yl)pyrimidine-2,4(1H,3H)-dione

Target: STAT

Beclometasone dipropionate

Cat.No: T1127

Synonym: Beclovent,Beclomethasone dipropionate,二丙酸倍氯米松,丙酸倍氯米松,Beconase,Vancenase

Target: Glucocorticoid Receptor

Cat.No: T24838

Synonym: Stafib 1,Stafib1

Target: STAT

Cat.No: T2600

Synonym: Zinc02557947,Tyrphostin AG 490,AG 490,AG-490,Tyrphostin B42

Target: EGFR, JAK, STAT, Autophagy

Cat.No: T35407

Target: PKC

Cat.No: T1849

Synonym: CYT11387,CYT387,LM-1149

Target: Apoptosis, JAK, Autophagy

Cat.No: T18680

Target: Others

Allylpyrocatechol

Cat.No: T26596

HAT-SIL-TG-1&AT

Cat.No: T74800

Cat.No: T26895

Synonym: BRD-0476,ML 187,ML187,ML-187,BRD 0476

5-epi-Arvestonate A

Cat.No: T75535

Interferon alfa

Cat.No: T77038

15(R)-Lipoxin A4

Cat.No: T37265

Synonym: 15(R)-Lipoxin A4,AT-Lipoxin A4

Cat.No: T68306

Cat. No.	Product Name	Target	Signaling Pathways
TN1413	Atranorin 荔枝素，巴美灵,荔枝素	Endogenous Metabolite; NO Synthase; Ras	GPCR/G Protein; Immunology/Inflammation; MAPK; Metabolism
	Atranorin 是地衣的次生代谢产物，具有显着的抗伤害、抗炎和氧化还原活性，对 H(2)O(2) 诱导的氧化应激下的细胞具有细胞保护作用。
T5668	Triacetylresveratrol 乙酰化白藜芦醇,三乙酰基白藜芦醇,Acetyl-trans-resveratrol	BCL; NF-κB; STAT	Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells
	Triacetylresveratrol (Acetyl-trans-resveratrol) 是 Resveratrol 的乙酰化类似物，可降低 STAT3和 NF-κB 磷酸化，具有抗癌作用。
TN1237	3-O-Methylgallic acid 3,4-Dihydroxy-5-methoxybenzoic acid,3-O-甲基没食子酸	Apoptosis; NF-κB; OCT; DNA/RNA Synthesis; STAT	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; JAK/STAT signaling; Membrane transporter/Ion channel; NF-κB; Stem Cells
	3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) 是一种花青素代谢产物，具有强大的抗氧化能力。它还诱导细胞凋亡并具有抗癌作用，可抑制 Caco-2 细胞增殖，IC50值为 24.1 μM。
T3673	Mollugin 大叶茜草素,Rubimaillin	HER; JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	Mollugin (Rubimaillin) 是Rubia cordifolia L.中主要的生物活性成分。它能通过 p38-Smad 信号通路增强 BMP-2 的成骨作用。它通过抑制 TNF-α 诱导的 NF-κB 激活起抗癌疗效。
T5S1897	Linderalactone	Apoptosis; Others; JAK	Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Others; Stem Cells
	Linderalactone 是从乌药中分离出来的一种倍半萜烯内酯，通过调节凋亡相关蛋白的表达和抑制 JAK/STAT 信号通路来抑制癌细胞生长。它以 IC50值为 15 µM 来抑制肺癌 A-549 细胞的增殖。
T6S1966	Curculigoside Curculigoside A,仙茅苷	Antioxidant; NF-κB; JAK; STAT	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; NF-κB; oxidation-reduction; Stem Cells
	Curculigoside (Curculigoside A) 是仙茅中的主要皂苷，具有显著的抗氧化、抗骨质疏松、抗抑郁和神经保护作用。它通过调节JAK/STAT/NF-κB 信号传导途径，具有抗关节炎作用。

天然产物

Cat.No: TN1413

Synonym: 荔枝素，巴美灵,荔枝素

Target: Endogenous Metabolite, NO Synthase, Ras

Triacetylresveratrol

Cat.No: T5668

Synonym: 乙酰化白藜芦醇,三乙酰基白藜芦醇,Acetyl-trans-resveratrol

Target: BCL, NF-κB, STAT

3-O-Methylgallic acid

Cat.No: TN1237

Synonym: 3,4-Dihydroxy-5-methoxybenzoic acid,3-O-甲基没食子酸

Target: Apoptosis, NF-κB, OCT, DNA/RNA Synthesis, STAT

Cat.No: T3673

Synonym: 大叶茜草素,Rubimaillin

Target: HER, JAK

Cat.No: T5S1897

Target: Apoptosis, Others, JAK

Cat.No: T6S1966

Synonym: Curculigoside A,仙茅苷

Target: Antioxidant, NF-κB, JAK, STAT

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