TGF-β / Smad Signaling(TGF-β / Smad 信号转导)

Transforming growth factor-beta (TGF-beta) is a multifunctional cytokine that regulates proliferation, migration, differentiation, and survival of many different cell types. Deletion or mutation of different members of the TGF-β family have been shown to cause vascular remodeling defect and absence of mural cell formation, leading to embryonic lethality or severe vascular disorders. TGF-β induces smooth muscle differentiation via Notch or SMAD2 and SMAD3 signaling in ES cells or in a neural crest stem cell line. TGF-β binds to TGF-βRI and to induce phosphorylation of SMAD2/3, thereby inhibiting proliferation, tube formation, and migration of endothelial cells (ECs).

TGF-β is a pluripotent cytokine with dual tumour-suppressive and tumour-promoting effects. TGF-β induces the epithelial-to-mesenchymal transition (EMT) leading to increased cell plasticity at the onset of cancer cell invasion and metastasis.

Products for TGF-β / Smad Signaling

Cat.No. 产品名称 Information
GC36433 LDN193189 Tetrahydrochloride An inhibitor of BMP receptors ALK1, ALK2, ALK3, and ALK6
GC36282 Hypocrellin A
竹红菌甲素
A perylenequinoid with diverse biological activities
GC36208 H-1152 dihydrochloride H-1152 dihydrochloride (2HCl) is a membrane-permeable and selective inhibitor of Rho-associated protein kinase (ROCK). H-1152 inhibits ROCK2, PKA, PKC, PKG, AuroraA and CaMK2 with IC50 of 0.0120 μM, 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.
GC36207 H-1152 A ROCK inhibitor
GC36167 GMB-475 GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
GC35897 DPH
5-(3-(4-氟苯基)-1-苯基-1H-吡唑-4-基)咪唑烷-2,4-二酮
DPH 是一种有效的细胞渗透性 c-Abl 激活剂，在刺激 c-Abl 活化方面表现出有效的酶和细胞活性。
GC35812 Dasatinib hydrochloride
达沙替尼盐酸盐; BMS-354825 hydrochloride
An inhibitor of Abl and Src
GC35753 CT-721 CT-721 是一种有效的，时间依赖性的 Bcr-Abl 激酶抑制剂，抑制野生型 Bcr-Abl 激酶的 IC50 值为 21.3 nM，具有抗慢性骨髓白血病 (CML) 活性。
GC35682 CHMFL-ABL/KIT-155
CHMFL-ABL-KIT-155
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的，具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC50 分别为 46 nM 和 75 nM)，对 BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM), PDGFRβ (IC50=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。
GC35651 Cenisertib
AS-703569; R-763
Cenisertib (AS-703569) 是一种多激酶抑制剂，可抑制 Aurora-kinase-A/B，ABL1，AKT，STAT5, FLT3 的活性。 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。 Cenisertib 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。
GC35530 BJE6-106
B106
BJE6-106 (B106) 是一种有效的选择性 PKCδ 抑制剂，IC50 值为 0.05 μM，BJE6-106 (B106) 靶向 PKCδ 的选择性是 PKC 同工酶 PKCα 的 1000倍 (IC50=50 μM)。BJE6-106 (B106) 可以诱导 caspase 依耐性细胞凋亡 (apoptosis)。BJE6-106 (B106) 具有肿瘤特异性作用。
GC35462 Bafetinib
巴氟替尼; INNO-406; NS-187
A Bcr-Abl inhibitor
GC35442 Azaindole 1
6-氯-N4-[3,5-二氟-4-[(3-甲基-1H-吡咯并[2,3-B]吡啶-4-基)氧]苯基]-2,4-嘧啶二胺,ROCK-IN-2?，TC-S 7001
A ROCK1 and ROCK2 inhibitor
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
GC44903 SMAD3 Inhibitor, SIS3 An inhibitor of TGF-β signaling
GC44729 Prostratin
13-O-乙酰基-12-脱氧佛波醇,13-O-Acetylphorbol
An HIV re-activator
GC44655 PKCε Inhibitor Peptide
Protein Kinase Cɛ Inhibitor Peptide，ɛV1-2
PKCε Inhibitor Peptide，也称为 εV1-2，是一种蛋白激酶 C ε (PKCε) 衍生肽，作为选择性 PKCε 抑制剂，抑制 PKCε 的易位。
GC44303 N-Acetylpuromycin A non-ribotoxic form of puromycin
GC44094 LX7101 (hydrochloride) A LIMK and ROCK inhibitor
GC43993 K252b A cell-impermeable kinase inhibitor
GC43286 CMPD101 A GRK2 and GRK3 inhibitor
GC43184 CAY10622 A ROCK1 and ROCK2 inhibitor
GC43105 C8 Ceramide (d18:1.8:0)
N-辛酰基-D-神经鞘氨醇; N-Octanoyl-D-erythro-sphingosine
A cell-permeable ceramide analog
GC42747 Afuresertib (hydrochloride)
GSK2110183 hydrochloride
A pan-Akt inhibitor
GC41863 10,11-dehydro Curvularin
α,β-dehydro Curvularin
A natural mycotoxin
GC41737 (S)-Glycyl-H-1152 (hydrochloride)
Rho Kinase Inhibitor IV
A ROCK inhibitor
GC40928 Trimethylamine N-oxide
三甲胺N-氧化物

A metabolite of choline, phosphatidylcholine, and L-carnitine
GC40770 L-erythro Sphingosine (d18:1)
双琥珀酰亚胺辛二酸酯
A bioactive sphingolipid
GC34493 BIBF0775 BIBF-0775 is a selective inhibitor of transforming growth factor β Receptor I (TGFβRI,Alk5) with an IC50 of 34nM.
GC40197 Pirfenidone-d5
5-甲基-1-(苯基-2,3,4,5,6-D5)-2(1H)-吡啶酮,AMR69-d5
An internal standard for the quantification of pirfenidone
GC40080 Bosutinib-d8
SKI-606 D8
An internal standard for the quantification of bosutinib
GC34300 AR-13324 analog mesylate AR-13324类似物甲磺酸盐是AR-13324的类似物。
GC34060 Disitertide (P144)
地司特泰,P144
Disitertide (P144) (P144) 是一种肽类转化生长因子-β 1 (TGF-β1) 抑制剂，专门设计用于阻断与其受体的相互作用。 Disitertide (P144) (P144) 也是一种 PI3K 抑制剂和凋亡诱导剂。
GC33901 Pentanoic acid Pentanoicacid是一种短链脂肪酸，是细菌代谢产物，与过敏性皮肤病有关系。Pentanoicacid能够激活ROCK信号通路。
GC33368 BCR-ABL-IN-2 BCR-ABL-IN-2是BCR-ABL1激酶的抑制剂，其对ABL1native和ABL1T315I的IC50值分别为57nM，773nM。
GC33351 CZC-8004 (CZC-00008004)
N2-(4-(氨甲基)苯)-5-氟-N4-苯基嘧啶-2,4-二胺,CZC-00008004
A tyrosine kinase inhibitor
GC33343 BCR-ABL-IN-1 BCR-ABL-IN-1是一种BCR-ABL酪氨酸激酶抑制剂，pIC50值为6.46，可能用于慢性髓细胞白血病的研究。
GC33310 Rho-Kinase-IN-1 Rho-Kinase-IN-1是一个rho激酶抑制剂，来自专利US20090325960A1，化合物1.008。
GC33201 GZD856 GZD856是一种新型，有口服活性的PDGFRα/β抑制剂，IC50分别为68.6和136.6nM。具有抗肺癌活性。也是Bcr-AblT315I的抑制剂，对Bcr-Abl和T315I突变型的IC50分别为19.9和15.4 nM。
GC33120 ZINC00881524 A ROCK inhibitor
GC32914 EMT inhibitor-1 EMTinhibitor-1是Hippo，TGF-β和Wnt信号通路的抑制剂，并拥有抗肿瘤活性。
GC32870 Ingenol ((-)-Ingenol)
巨大戟醇; (-)-Ingenol
A PKC activator
GC32868 BDP5290 BDP5290对MRCKβ、ROCK1、ROCK2的IC50值分别为17nM、230nM、123nM和100nM，是ROCK和MRCK的有效抑制剂。
GC32867 Flumatinib (HHGV678)
4-[(4-甲基-1-哌嗪基)甲基]-N-[6-甲基-5-[[4-(3-吡啶基)-2-嘧啶基]氨基]-3-吡啶基]-3-(三氟甲基)苯甲酰胺,HHGV678
A Bcr-Abl inhibitor
GC32840 R-268712 R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
GC32811 LXS196
LXS196; IDE196
A PKC inhibitor
GC32788 SJ000291942 A BMP signaling activator
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。
GC32714 Mitoxantrone (mitozantrone)
米托蒽醌; Mitozantrone; NSC 301739
米托蒽醌Mitoxantrone是一种抗肿瘤的蒽醌衍生物。
GC32703 Asciminib (ABL001)
ABL001
An allosteric inhibitor of Abl1