STAT3 选择性抑制剂 | 激活剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S7923 SH5-07 (SH-5-07)

SH5-07是一种强效的异羟肟酸类STAT3抑制剂,在体内外具有抗肿瘤活性。

Selective
S8197 APTSTAT3-9R

APTSTAT3-9R是特异的STAT3结合肽段,加上一段可穿透细胞的模体。对多种类型的癌细胞处理以APTSTAT3-9R可阻断STAT3的磷酸化以及减少STAT靶标的表达。

Selective
S8561 HJC0152

HJC0152是signal transducer and activator of transcription 3 (STAT3)抑制剂,其溶解度相较于niclosamide有显著的改善。

Selective
S8605 C188-9

C188-9 (TTI 101) is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

Selective STAT3, Kd: 4.7 nM
S7769 BP-1-102

BP-1-102是有效的、具有口服生物活性的、选择性STAT3抑制剂,与STAT3结合亲和力Kd为504 nM.在4-6.8 μM时,抑制Stat3与pTyr肽段的相互作用和STAT3的激活。

Selective STAT3, Kd: 504 nM
S3030 Niclosamide (BAY2353)

Niclosamide能够抑制DNA复制,并抑制STAT3,无细胞试验中IC50为0.7 μM。 Niclosamide 选择性地抑制STAT3的磷酸化,对其他同系物如STAT1和STAT5的激活没有明显抑制作用。

Selective STAT3, IC50: 0.7 μM
S0818 STAT3-IN-1

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

Selective STAT3, IC50: 2.14 μM; STAT3, IC50: 1.82 μM
S2796 WP1066

WP1066是一种新型JAK2STAT3抑制剂,在HEL细胞中IC50分别为2.30 μM和2.43 μM;对JAK2,STAT3,STAT5和ERK1/2具有抑制活性,而对JAK1和JAK3没有作用。Phase 1。

Selective STAT3, IC50: 2.43 μM
S2285 Cryptotanshinone

Cryptotanshinone是一种STAT3抑制剂,无细胞试验中IC50为4.6 μM,强烈抑制STAT3 Tyr705磷酸化,对STAT3 Ser727作用效果弱,对STAT1和STAT5没有作用效果。

Selective STAT3, IC50: 4.6 μM
S7024 Stattic

Stattic是第一个非肽类STAT3小分子抑制剂,有效抑制STAT3激活和核易位,IC50为5.1 μM,其作用于STAT3的选择性远高于STAT1。

Selective STAT3, IC50: 5.1 μM
S1396 Resveratrol (SRT501)

Resveratrol具有广泛靶点,包括环氧酶(如COX, IC50=1.1 μM)、脂肪氧合酶(LOC, IC50=2.7 μM)、sirtuins和其他蛋白质。它是一种天然的植物抗毒素,具有抗癌,抗炎,降血糖和其他有益心血管的作用。

Selective STAT3, IC50: 20 μM
S1155 S3I-201

S3I-201有效抑制STAT3的DNA结合活性,IC50为86 μM,而对STAT1和STAT5的抑制活性低。

Selective STAT3, IC50: 86 μM
S9920 GYY4137

GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity.

Selective
S8152 Cucurbitacin I

Cucurbitacin-I (Elatericin B, JSI 124, NSC 521777), a natural cell-permeable triterpenoid isolated from Cucurbitaceae, is a novel selective inhibitor of JAK2/STAT3.

Selective
S7501 HO-3867

HO-3867, 姜黄素的一种类似物, 是选择性的STAT3抑制剂。抑制STAT3的磷酸化、转录和DNA结合活性,而不影响其他活性STATs的表达。

Selective
S2265 Artesunate (WR-256283)

Artesunate 是一种抗疟类药,作用于小细胞肺癌细胞系H69,IC50为< 5 μM。它是一种潜在的STAT3抑制剂,在体外对癌细胞有选择性细胞毒性作用;是有效的EXP1抑制剂。

Selective
S7977 Napabucasin (BBI608)

Napabucasin是一种口服具有活性的Stat3和癌细胞多能性抑制剂。

Selective
S1014 Bosutinib (SKI-606)

Bosutinib (SKI-606)是一种新型的双重Src/Abl抑制剂,在无细胞试验中IC50分别为1.2 nM 和 1 nM。

Selective
S3810 Scutellarin

Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide), the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities. Scutellarin can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclast

Selective
S0445 SC-43

SC-43 is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1) that inactivates STAT3 and reduces liver fibrosis. SC-43 is found to have anti-tumor activity.

Selective
S2824 TPCA-1

TPCA-1是一种IKK-2抑制剂,无细胞试验中IC50为17.9 nM,抑制NF-κB通路,比作用于IKK-1选择性高22倍。

Selective
S7951 Ochromycinone (STA-21)

STA-21是一个选择性的STAT3抑制剂。

Selective
S0918 Ginkgolic acid C17:1

Ginkgolic acid (C17:1) suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid (C17:1) is extracted from Ginkgo biloba Leaves, Ginkgolic acid (C17:1) exhibits anticancer effects.

Selective
S9664 Colivelin

Colivelin (CLN) is a brain-penetrant neuroprotective peptide with potent long-term capacity against deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin is an activator of STAT3.

Selective
S0949 Cucurbitacin IIb

Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α. Cucurbitacin IIb is isolated from Hemsleya amabilis that induces apoptosis with anti-inflammatory activity.

Selective
S6919 Brevilin A

Brevilin A (6-O-Angeloylplenolina), a sesquiterpene lactone isolated from Centipeda minima, is a selective inhibitor of STAT3 and attenuates the JAKs activity by blocking the JAKs tyrosine kinase domain JH1. Brevilin A induces apoptosis and autophagy of colon adenocarcinoma cell CT26 via mitochondrial pathway and PI3K/AKT/mTOR inactivation.

Selective
S3267 Kaempferol-3-O-rutinoside

Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.

Selective
S7337 SH-4-54

SH-4-54是一种高效的STAT抑制剂,其作用STAT3和STAT5的KD分别为300 nM和464 nM。

Pan STAT3, Kd: 300 nM
S4182 Nifuroxazide

Nifuroxazide是可渗透细胞的,口服有效的硝基呋喃类止泻药,有效地抑制细胞内STAT1/3/5转录活性的激活,IC50为3 µM。

Pan
S4358 Pimozide

Pimozide is an antipsychotic drug of the diphenylbutylpiperidine class, which is a strong inhibitor of CYP2D6.

Pan