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.
Cat. No. | Product Name | CAS No. | Purity | Chemical Structure |
---|---|---|---|---|
KM18978 |
A 77-01
A 77-01 是一种有效的 TGF-β I 型受体家族 ALK5 抑制剂,IC50 值为 25 nM。 |
607737-87-1 | 98% |
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KM2595 |
A 83-01
A 83-01 是一种有效的 TGF-β I 型受体 ALK5,ALK4 和 ALK7 的抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。 |
909910-43-6 | ≥98% |
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KM2596 |
A 83-01 sodium salt
A 83-01 sodium salt 是一种有效的 TGF-β I 型受体 ALK5,ALK4 和 ALK7 的抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。 |
≥95% |
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KM6700 |
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。 |
2254409-25-9 | 98% |
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KM7296 |
ALK2-IN-4
ALK2-IN-4 是一种有效的 ALK2 抑制剂,详细信息请参见专利 WO2020086963A1,compound Formula I free base。 |
2248154-85-8 | 98% |
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KM5181 |
ALK2-IN-4 succinate
ALK2-IN-4 succinate 是一种有效的 ALK2 抑制剂,详细信息请参见专利 WO2020086963A1,compound Formula I free base。 |
2416307-25-8 | 98% |
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KM2901 |
AZ12601011
AZ12601011 是一种具有口服活性的,选择性 TGFBR1 激酶抑制剂,IC50 为 18 nM,Kd 为 2.9 nM。AZ12601011 通过选择性的抑制 ALK4,TGFBR1 和 ALK7 来抑制 SMAD2 的磷酸化。AZ12601011 抑制乳腺肿瘤的生长。 |
98% |
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|
KM7940 |
BIBF0775
BIBF0775是有效,选择性的TGFβI型受体 (Alk5)的抑制剂,IC50为34 nM。 |
334951-90-5 | 98% |
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KM10194 |
BIO-013077-01
BIO-013077-01 是一种吡唑类的 TGF-β 抑制剂。 |
746667-48-1 | 98% |
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KM10848 |
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 激活 BMP 信号。BMP signaling agonist sb4 还能激活典型 BMP 信号通路中的 BMP4 靶基因 (DNA 结合抑制剂,Id1 和 Id3)。 |
100874-08-6 | 98% |
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KM31821 | BMPR2-IN-1 |
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KM2892 |
DMH-1
DMH-1 是一种有效的,具有选择性的 BMP 抑制剂,对 ALK1/ALK2/ALK3/ALK6的IC50 值分别为 27/107.9/<5/47.6 nM。 |
1206711-16-1 | 98% |
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KM10457 |
Dorsomorphin
Dorsomorphin (Compound C) 是一种选择性,ATP 竞争性的 AMPK 抑制剂 (在没有 AMP 的情况下,Ki 为 109 nM)。Dorsomorphin 选择性抑制 BMP I 型受体 ALK2,ALK3 和 ALK6。Dorsomorphin 诱导自噬 (autophagy) 作用。 |
866405-64-3 | 98% |
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KM7350 |
Dorsomorphin Dihydrochloride
Dorsomorphin dihydrochloride (Compound C dihydrochloride) 是一种有效,选择性和 ATP 竞争性的 AMPK 抑制剂,Ki 为 109 nM。Dorsomorphin dihydrochloride 通过靶向抑制 I 型受体 ALK2,ALK3 和 ALK6 来抑制 BMP 途径。Dorsomorphin dihydrochloride 诱导自噬 (autophagy) 作用。 |
1219168-18-9 | 98% |
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KM8371 |
Galunisertib
Galunisertib (LY2157299) 是一种选择性的 TGF-β 受体 I 型 (TGF-βRI) 激酶抑制剂,IC50 为 56 nM。 |
700874-72-2 | 98% |
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KM4917 |
GW788388
GW788388 是一种有效的 ALK5 抑制剂,IC50 值 18 nM;同时抑制 TGF-β II 型受体 和激活素 II 型受体的活性,但对 BMP II 型受体无作用。 |
452342-67-5 | 98% |
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KM19982 | IN-1130 | 868612-83-3 | 98% |
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KM13999 |
Isosaponarin
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。 |
19416-87-6 | 98% |
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KM10948 |
ITD-1
ITD-1 是第一个选择性的 TGFβ 受体抑制剂,IC50 为 460 nM。 |
1099644-42-4 | 98% |
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KM10267 |
K02288
K02288是一种有效的骨形态发生蛋白 (BMP) I 型受体抑制剂,抑制 ALK1,ALK2,ALK6 的 IC50 为1.8,1.1,6.4 nM。对 ALK3 和 ALK6 的抑制稍弱,IC50在 5-34 nM 之间。 |
1431985-92-0 | 98% |
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