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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T16940 |
STAT5-IN-2
|
Apoptosis; STAT | Apoptosis; JAK/STAT signaling; Stem Cells |
STAT5-IN-2 是一种具有抗白血病作用的 STAT5 抑制剂(EC50:在 K562 和 KU812 细胞中分别为 9 μM 和 5 μM)。 | |||
T9209 |
PF-05221304
STAT5 Inhibitor III,NSC 170984,R 6238,,Clesacostat |
Acetyl-CoA Carboxylase | Metabolism |
PF-05221304 (NSC-170984) 是一种具有口服活性的肝脏靶向乙酰辅酶A 羧化酶 (ACC) 抑制剂,ACC 是脂肪酸合成的限速酶。 | |||
T8494 |
NS-3-008 hydrochloride
NS-3-008 HCl |
Others | Others |
NS-3-008 hydrochloride (NS-3-008 HCl) 是一种口服具有活性的G0s2转录抑制剂(IC50:2.25 μM)。它可用于慢性肾脏疾病的研究。 | |||
T1995 |
Fedratinib
TG-101348,SAR 302503 |
Apoptosis; FLT; c-RET; JAK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Fedratinib (TG-101348) 是选择性,ATP 竞争性和具有口服活性的 JAK2抑制剂,对于 JAK2和JAK2V617F 激酶的IC50均为 3 nM。它是对JAK2的选择性分别比 JAK1 和 JAK3 高 35 倍和 334 倍。它可诱导癌细胞凋亡,并可用于骨髓增生性疾病的研究。 | |||
T9251 |
Fedratinib hydrochloride hydrate
TG-101348 hydrochloride hydrate,SAR 302503 hydrochloride hydrate |
Apoptosis; JAK | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Fedratinib hydrochloride hydrate (SAR 302503 hydrochloride hydrate) 是一种选择性的,ATP 竞争性和具有口服活性的JAK2抑制剂,对于JAK2和JAK2V617F 激酶的IC50均为 3 nM。它可诱导癌细胞凋亡,可研究骨髓增生性疾病。 | |||
T21267 |
HODHBt
|
STAT | JAK/STAT signaling; Stem Cells |
HODHBt 是一种 STAT5-SUMO 蛋白-蛋白相互作用抑制剂。 | |||
T8546 |
BD750
|
JAK; STAT | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
BD750 是免疫抑制剂和JAK3/STAT5的抑制剂,可抑制 IL-2 诱导的、JAK3/STAT5 依赖的 T 细胞增殖,对小鼠和人 T 细胞增殖的IC50值分别为 1.5 和 1.1 μM。 | |||
TP1433 |
CMD178 TFA
|
STAT | JAK/STAT signaling; Stem Cells |
CMD178 TFA 是一种先导肽,可始终降低由 IL-2/s IL-2Rα 信号传导诱导的 Foxp3 和 STAT5 的表达。 | |||
T6669 |
SH-4-54
|
STAT | JAK/STAT signaling; Stem Cells |
SH-4-54 是有效小分子非磷酸化 STAT3 抑制剂,与 STAT3 和 STAT5 结合的 KD 值分别为 300 和 464 nM。 | |||
T27650 |
JAK3i
JAK-3i,JAK 3i |
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK3i 是JAK3激酶的选择性共价抑制剂。JAK3i 揭示了STAT5磷酸化的两个不同的时间波,并且更有效地靶向第二波,这是细胞周期进程和T 细胞增殖所必需的。 | |||
T72029 |
CDK8-IN-13
|
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
CDK8-IN-13是一种 CDK8抑制剂(IC50:51.9 nM),具有强效性、选择性和口服活性。CDK8-IN-13能诱导细胞凋亡,降低了 p-STAT1 S727和p-STAT5 S726的表达。CDK8-IN-13表现出抗肿瘤活性。 | |||
T67894 |
Butyzamide
|
Thrombopoietin Receptor; JAK | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells |
Butyzamide 是一种有效的 可口服的Mpl 激活剂,是一种对血小板生成素(TPO)受体具有拮抗作用的新型非肽基分子,促进表达人Mpl (hMpl)的和小鼠pro B 细胞株Ba/F3的增殖,诱导JAK2、STAT3、STAT5和MAPK 的磷酸化。Butyzamide 在小鼠异种移植试验中有助于提升血小板水平。 | |||
T9428 |
HM43239
|
FLT | Angiogenesis; Tyrosine Kinase/Adaptors |
HM43239 是一种具有口服活性和选择性 FLT3抑制剂,IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性,并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖并诱导其凋亡 (apoptosis)。 | |||
T7101 |
Tyrphostin AG30
Tyrphostin AG30(AG30),酪氨酸磷酸化抑制剂 AG 30 |
EGFR; Tyrosine Kinases | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Tyrphostin AG30 (AG30) 是一种有效的蛋白质酪氨酸激酶 (PTK) 抑制剂,选择性地抑制 c-ErbB 的自我更新诱导,并能抑制原发性红细胞 c-ErbB 激活 STAT5。 | |||
T3072 |
XL019
|
Apoptosis; FLT; JAK; PDGFR | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors |
XL019 是一种具有口服活性的选择性JAK2抑制剂。它对JAK2的选择性是 100 多种丝氨酸/苏氨酸和酪氨酸激酶的 50 倍以上。它对 JAK2 V617F 和野生型 JAK2 细胞中 STAT3 和 STAT5 磷酸化有抑制作用。 | |||
TQ0037 |
Abrocitinib
PF-04965842 |
JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Abrocitinib (PF-04965842) 是可口服、选择性的JAK1抑制剂,可用于自身免疫症的研究,对 JAK1 和 JAK2 的IC50值分别为 29 和 803 nM。它可抑制 TYK2 的活性,IC50为1.253 μM, 也可抑制刺激后 STAT1、STAT3 和 STAT5 的磷酸化水平。 | |||
T8378 |
AS2863619
|
CDK; STAT | Cell Cycle/Checkpoint; JAK/STAT signaling; Stem Cells |
AS2863619 是一种口服的细胞周期蛋白依赖性激酶 8 和CDK19抑制剂,抑制CDK8/19可增强STAT5的激活,从而激活 Foxp3 基因。它可将抗原特异性效应子/记忆 T 细胞转换为 Foxp3+调节性 T 细胞,以研究各种免疫疾病。 | |||
T2546 |
Pimozide
R6238,匹莫奇特,匹莫齐特 |
Potassium Channel; Dopamine Receptor; Adrenergic Receptor; STAT | GPCR/G Protein; JAK/STAT signaling; Membrane transporter/Ion channel; Neuroscience; Stem Cells |
Pimozide (R6238) 是多巴胺受体拮抗剂,对多巴胺 D1、D2 和 D3 受体的 Ki 值分别为 588、1.4 和 2.5 nM。它也是STAT3和STAT5的抑制剂,对 α1 肾上腺素受体也有较高亲和性,Ki 值为 39 nM。 | |||
T2156 |
WP1066
|
Apoptosis; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
WP1066 是一种新型JAK2和STAT3抑制剂,对 STAT5 和 ERK1/2 也起作用。它用于研究黑色素瘤、脑癌、实体瘤和中枢神经系统肿瘤治疗。 | |||
T35429 |
AC-4-130
|
||
AC-4-130, a powerful inhibitor of the SH2 domain of STAT5, effectively hinders STAT5 activation, dimerization, nuclear translocation, and transcription of genes reliant on STAT5. This compound directly binds to STAT5, ultimately leading to cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 exhibits notable anti-cancer properties and effectively suppresses abnormal STAT5 activity in acute myeloid leukemia (AML), making it a promising therapeutic option [1]. | |||
T69292 | IQDMA | ||
IQDMA is an inhibitor of the transcription factor STAT5. | |||
T70950 | BP-1-108 | ||
BP-1-108 is a potent and selective STAT5 inhibitor. | |||
T28113 |
MS-1020
MS 1020 |
||
MS-1020 is a JAK3 and STAT3 inhibitor. MS-1020 selectively blocks constitutively-active JAK3 and consistently suppressed interleukin-2-induced JAK3/STAT5 signalling. MS-1020 potently inhibits persistently-active STAT3 in a cell type-specific manner. | |||
T35894 |
Atiprimod dihydrochloride
|
||
JAK2 inhibitor (IC50 = 397 nM). Also inhibits STAT3 and STAT5 phosphorylation. Inhibits cell growth and induces apoptosis in cells expressing the JAK2V617F mutation. Manshouri et al (2011) Bone marrow stroma-secreted cytokines protect JAK2(V617F)-mutated cells from the effects of a JAK2 inhibitor. Cancer Res. 71 3831 PMID:21512135 |Quintás-Cardama et al (2011) Preclinical characterization of atiprimod, a novel JAK2 AND JAK3 inhibitor. Invest.New Drugs 29 818 PMID:20372971 | |||
T10382 |
AS2863619 free base
|
CDK | Cell Cycle/Checkpoint |
AS2863619 free base enables the conversion of antigen-specific effector/memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8/19, which consequently activates the Foxp3 gene. | |||
T70333 |
PM-43I
|
||
PM-43I is a potent inhibitor of both STAT5- and STAT6-dependent allergic airway disease in mice. | |||
T79581 | JAK2-IN-9 | JAK | Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
JAK2-IN-9(Compound A8)是一款选择性JAK2抑制剂(IC50:5 nM),能够抑制JAK2、STAT3和STAT5的磷酸化,并显示出代谢稳定性。此外,JAK2-IN-9能够诱导细胞凋亡(apoptosis),适用于骨髓增生性肿瘤(MPN)的研究。 | |||
T73142 | FLT3-IN-18 | ||
FLT3-IN-18是一种高效且选择性的FLT3抑制剂,具有0.003 μM的IC50值。该化合物能够诱导(apoptosis)并使细胞周期在G1期停滞,同时抑制FLT3和STAT5的磷酸化,显示出对急性髓系白血病(AML)研究的潜力。 | |||
T64110 |
Debio 0617B
|
||
Debio 0617B 是一种多激酶抑制剂,能够降低原代人 AML CD34+干/祖细胞的维持和自我更新。Debio 0617B 靶向 STAT3/STAT5 信号上游关键激酶,如 JAK、ABL、SRC 和 III/V 类受体酪氨酸激酶。Debio 0617B 能够用于研究 STAT3 驱动的实体瘤。 | |||
T77932 |
PF15 TFA
|
PROTACs | PROTAC |
PF15 TFA是一种连接FLT3 kinase配体和CRBN配体的PROTAC,作为FLT3-ITD的高选择性降解剂,DC50值为76.7 nM。该化合物可显著抑制FLT3-ITD阳性细胞增殖,并降低FLT3和STAT5磷酸化水平。PF15 TFA亦能抑制小鼠模型的肿瘤生长,并可用于白血病研究。 | |||
TP1770 |
CMD178
|
||
CMD178 is an important polypeptide that consistently reduces the expression of Foxp3 and STAT5 by inhibiting the IL-2/s IL-2Rα signaling pathway. | |||
T73330 |
JAK-IN-24
|
||
JAK-IN-24 是一种 JAK 抑制剂,在 4 μM 或 1 mM ATP 存在时,IC50分别为 0.534 和 24 nM。JAK-IN-24 还抑制 PBMCIL-15诱导的 STAT5磷酸化,IC50为 86.171 nM。 | |||
T71654 |
APcK110
|
||
APcK110 is a novel Kit inhibitor . APcK110 inhibits proliferation of the mastocytosis cell line HMC1.2 and the SCF-responsive cell line OCI/AML3 in a dose-dependent manner . APcK110 is a more potent inhibitor of OCI/AML3 proliferation than the clinically used Kit inhibitors imatinib and dasatinib and at least as potent as cytarabine. APcK110 inhibits the phosphorylation of Kit, Stat3, Stat5, and Akt in a dose-dependent fashion, showing activity of APcK110 on Kit and its downstream signaling path... | |||
T14925 |
Cenisertib
AS-703569,R-763 |
Akt; Bcr-Abl; STAT | Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors |
Cenisertib 是一种有效的 ATP 竞争性的多激酶抑制剂,对 Aurora-kinase-A/B,ABL1,AKT,STAT5, FLT3 的活性具有抑制作用,对FER 及其同源物的激酶也显示出抑制作用。Cenisertib 通过抑制肿瘤肥大细胞 (MC) 中几种不同分子靶标的活性抑制其生长,也抑制异种移植模型中胰腺癌,乳腺癌,结肠癌,卵巢癌和肺癌以及白血病的肿瘤生长。 | |||
T74259 | PF15 | PROTACs | PROTAC |
PF15是一种将FLT3 kinase配体与CRBN配体结合的PROTAC,它是FLT3-ITD的高选择性降解剂,显示出76.7 nM的DC50。该化合物能有效抑制FLT3-ITD阳性细胞增殖,并降低FLT3和STAT5的磷酸化水平。在小鼠模型中,PF15也能够抑制肿瘤生长,对白血病研究具有潜在应用价值。 | |||
T83756 |
S1H TFA
Site 1-binding Helix |
||
S1H是一种人造肽类模拟物,模仿人类生长激素的第36至51个氨基酸,且为生长激素受体的拮抗剂。在溶液中呈现α-螺旋结构,并在100和200纳摩尔(nM)的浓度下,能降低SK-MEL-28和MALME-3M黑色素瘤细胞系以及IM-9 B细胞淋巴细胞中,由人类生长激素及泌乳素诱导的STAT5磷酸化。 | |||
T74749 | AK-2292 | ||
AK-2292 是一种有效和选择性STAT5PROTAC 降解剂,DC50值为 0.10 μM。AK-2292 在体外和体内诱导 STAT5A/B 蛋白的降解。AK-2292 可在急性髓性白血病和慢性髓性白血病异种移植小鼠模型中诱导肿瘤消退。 | |||
T36645 |
CAY10763
CAY10763 |
||
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... | |||
T70779 | BPR1J-340 | ||
BPR1J-340 is a potent and selective FLT3 inhibitor with potential anticancer activity. BPR1J-340 was identified as a novel potent FLT3 inhibitor by biochemical kinase activity (IC50 approximately 25 nM) and cellular proliferation (GC50 approximately 5 nM) assays. BPR1J-340 inhibited the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD(+) AML cells. The pharmacokinetic parameters of BPR1J-340 in rats were determined. BPR1J-340 also demonstrated pronounced tumor growth inhibit... | |||
T12476 |
Pimozide-d4
Pimozide D4,R6238 D4 |
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Pimozide D4 is a deuterium labeled Pimozide. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2814 |
Cryptotanshinone
隐丹参酮,Cryptotanshinon,Tanshinone c,隐丹参醌 |
STAT; Autophagy | Autophagy; JAK/STAT signaling; Stem Cells |
Cryptotanshinone (Cryptotanshinon) 是从丹参的根中提取的一种天然产物,抑制STAT3的IC50为4.6 μM,具有抗肿瘤活性。 |