TGF-β Receptor(TGF-β受体)
TGF-β receptors (Transforming growth factor-β receptors) are single pass serine/threonine kinase receptors. Transforming growth factor beta (TGF-beta) is a member of a large family of pleiotropic cytokines that are involved in many biological processes, including growth control, differentiation, migration, cell survival, adhesion, and specification of developmental fate, in both normal and diseased states. TGF-beta superfamily members signal through a receptor complex comprising a type II and type I receptor, both serine/threonine kinases.
The type I receptors, referred to as activin receptor-like kinases (ALK), lie at the epicenter of the signaling cascade as they transduce TGF-beta signals to intracellular regulators of transcription known as Smad proteins. ALKs possess an extracellular binding domain, a transmembrane domain, a GS domain that serves as the site of activation by type II receptors, and a kinase domain that activates downstream signaling molecules. ALKs mediate the effect of TGF-beta superfamily on a variety of cellular processes such as proliferation, differentiation, apoptosis, adhesion and migration, and therefore play important roles in many biological processes. Some ALKs have been implicated in several disorders, including tumorigenesis and immune diseases, suggesting that these receptors can be used as drug targets.
Products for TGF-β Receptor
- Cat.No. 产品名称 Information
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GC65539
Fresolimumab
非苏木单抗,GC1008
Fresolimumab (GC1008) 是一种高亲和力的全人单克隆抗体,可中和人 TGFβ1、TGFβ2 和 TGFβ3 的活性形式。Fresolimumab 可用于癌症和纤维性疾病的研究。
- GC65329 EW-7195 EW-7195 是一种有效的、选择性 ALK5 (TGFβR1) 抑制剂,IC50 为 4.83 nM。EW-7195 对 ALK5 的选择性是 p38α 的 300 多倍。EW-7195 能有效抑制 TGF-β1 诱导的 Smad 信号转导、上皮间质转化 (EMT) 和乳腺癌向肺转移。
- GC65294 ALK2-IN-2 ALK2-IN-2 是一种有效的、选择性的活化素受体样激酶 2 (ALK2) 抑制剂,IC50 值为 9 nM,对 ALK2 的抑制作用是 ALK3 的 700 倍。
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GC62868
BIO-013077-01
6-(3-(6-甲基吡啶-2-基)-1H-吡唑-4-基)喹噁啉
BIO-013077-01 是一种吡唑类的 TGF-β 抑制剂。 - GC62146 XST-14 XST-14 是一种有效的,竞争性强且高度选择性的 ULK1 抑制剂,IC50 为 26.6 nM。XST-14 通过减少 ULK1 下游底物的磷酸化来诱导自噬抑制。XST-14 诱导肝细胞癌 (HCC) 细胞凋亡,并具有抗肿瘤作用。
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GC60210
Isosaponarin
异肥皂草苷
Isosaponarin是一种从芥末叶中分离出的黄酮苷,可以增加胶原蛋白(collagen)的合成,这是由上调的TGF-βII型受体(TβR-II)和脯氨酰4-羟化酶(P4H)蛋白产生引起的。 -
GC39398
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
LSKL, 血小板反应蛋白抑制剂 (TSP-1) 三氟醋酸盐
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 是一种衍生自 LAP-TGFβ 的四肽,是一种竞争性的 TGF-β1 拮抗剂。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 抑制 TSP-1 与 LAP 的结合并减轻肾间质纤维化和肝纤维化。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 通过抑制 TSP-1 介导的 TGF-β1 活性来抑制蛛网膜下纤维化,防止慢性脑积水的发生并改善蛛网膜下腔出血后的长期神经认知缺陷。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 可以轻松穿越血脑屏障。
- GC50593 BMP signaling agonist sb4 BMP signaling agonist sb4 是一种有效的苯并恶唑骨形态发生蛋白 4 (BMP4) 信号激动剂,EC50 值为 74 nM,通过稳定细胞内 p-SMAD-1/5/9 来激活 BMP 信号传导。 BMP 信号激动剂 sb4 激活 BMP4 靶基因(DNA 结合抑制剂,Id1 和 Id3)经典 BMP 信号。
- GC50589 AZ 12799734 AZ 12799734 是一种选择性的、口服活性的 TGFBR1 激酶抑制剂,IC50 为 47 nM。
- GC50317 IN 1130 IN 1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂,对 ALK5 介导的 Smad3 磷酸化的 IC50 为 5.3 nM。
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GC37880
Vactosertib Hydrochloride
EW-7197 Hydrochloride; TEW-7197 Hydrochloride
Vactosertib Hydrochloride (EW-7197 Hydrochloride) 是 TGFβRI (ALK5) 的小分子 ATP 竞争性抑制剂,其 IC50 值为 12.9 nM。 - GC36433 LDN193189 Tetrahydrochloride An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6
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GC35210
A 83-01 sodium salt
3-(6-Methylpyridin-2-yl)-N-phenyl-4-(quinolin-4-yl)-1H-pyrazole-1-carbothioamide, sodium salt
A TGF-β type I receptor inhibitor
- GC44303 N-Acetylpuromycin A non-ribotoxic form of puromycin
- GC34493 BIBF0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
- GC32840 R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
- GC32788 SJ000291942 A BMP signaling activator
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GC32728
LSKL, Inhibitor of Thrombospondin TSP-1
LSKL, 血小板反应蛋白抑制剂 (TSP-1)
LSKL,InhibitorofThrombospondin(TSP-1)是一种四肽,源于潜在联系多肽,能够抑制TSP-1的活性,来降低TGF-β的活性,能够阻止肝损伤和肝纤维化。
- GC19447 SM 16 An inhibitor of ALK5
- GC19234 LY3200882 An inhibitor of TGF-βRI
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GC13354
EW-7197
Vactosertib,TEW-7197
A potent inhibitor of ALK5 - GC12108 ITD 1 An inhibitor of TGF-β
- GC13225 LDN-214117 A selective ALK1 and ALK2 inhibitor
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GC17582
ML347
LDN 193719
A selective ALK1 and ALK2 inhibitor -
GC17035
LDN-212854
5-(6-(4-(哌嗪-1-基)苯基)吡唑并[1,5-a]嘧啶-3-基)喹啉
An ALK2 inhibitor -
GC14298
DMH-1
BMP Inhibitor II, DorsoMorphin Homolog 1, VU036482
A potent ALK2 inhibitor -
GC11604
LY364947
HTS466284
Inhibitor of TGF-β type-1 receptors - GC13769 SB505124 Inhibitor of receptors ALK4, ALK5, and ALK7
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GC17243
Dorsomorphin (Compound C)
6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶,Compound C
Dorsomorphin(Compound C)是一种细胞渗透的AMPK抑制剂。 - GC15567 K02288 A BMP signaling inhibitor
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GC12560
Dorsomorphin (Compound C) 2HCl
BML-275 2HCl,Compound C 2HCl
IC50:Dorsomorphin 以剂量依赖性方式抑制 BMP4 诱导的 BMP 反应性 SMAD 磷酸化(半数最大抑制浓度 (IC50) =0.47 mM)。 - GC12363 LY2109761 A dual inhibitor of TGF-β type 1/type II receptor kinases
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GC18015
LY2157299
LY-2157299;LY 2157299
A TGF-β type 1 receptor kinase inhibitor -
GC16580
LDN-193189
LDN 193189;LDN193189
An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6
- GC11878 GW788388 An inhibitor of ALK5 (TGFBR1)
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GC14349
SB525334
6-[2-(1,1-二甲基乙基)-5-(6-甲基-2-吡啶基)-1H-咪唑-4-基]喹喔啉
A potent inhibitor of TGF-β R1/ALK5 kinase - GC11545 SB 431542 SB-431542是一种小分子抑制剂,可以阻止TGF-β受体类型I的内部介导物,从而降低TGF-β1介导的增殖、细胞因子和胶原蛋白表达。
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GC13904
SD-208
SD 208; SD208
A potent, selective inhibitor of TGF-βRI -
GC10421
SB-505124 hydrochloride
SB 505124 hydrochloride;SB505124 hydrochloride
Inhibitor of receptors ALK4, ALK5, and ALK7 -
GC16793
RepSox
2-[3-(6-甲基-2-吡啶基)-1H-吡唑-4-基]-1,5-萘啶,E-616452;SJN 2511;E616452;SJN2511;E 616452;SJN-2511,ALK5 Inhibitor II
RepSox是一种有效的选择性转化生长因子-β受体I/激活素样激酶5(TGF-β-RI/ALK5)抑制剂,IC50为23nM。RepSox抑制ALK5自身磷酸化,IC50 值为4nM。 -
GC10166
A 83-01
3-(6-甲基-2-吡啶基)-N-苯基-4-(4-喹啉基)-1H-吡唑-1-硫代甲酰胺,A83-01;A-83-01
A 83-01 是 TGF-β I 型受体 ALK5 激酶、I 型淋巴结受体 ALK4 和 I 型淋巴结受体 ALK7 的有效抑制剂,IC50 s 分别为 12 nM、45 nM和 7.5 nM 分别抑制 ALK5、ALK4 和 ALK7 诱导的转录。 -
GC13927
A 77-01
A77-01;A-77-01
A potent ALK5 inhibitor