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Cat. No. | Product Name | ||
---|---|---|---|
L4100 | TGF-β/Smad靶点化合物库 | 184 compounds | |
184 个 TGF-β/Smad 靶点相关的小分子化合物的特有集合,用于高通量、高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1748 |
Kartogenin
KGN |
TGF-beta/Smad | Stem Cells |
Kartogenin (KGN) 是一种人间充质干细胞分化为软骨细胞的诱导剂(EC50:100 nM)。它能够结合纤维蛋白 A,破坏其与转录因子核心结合因子 β 亚基 (CBFβ) 的相互作用,并通过调节 CBFβ-RUNX1 转录程序,诱导软骨形成,可用于研究骨关节炎。 | |||
T4283 |
SRI-011381
|
TGF-beta/Smad | Stem Cells |
SRI011381 是口服具有活力的 TGF-β信号通路的激活剂,具有神经保护活性。 | |||
T16708 |
R-268712
|
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
R-268712 是选择性的 ALK5 抑制剂(IC50:2.5 nM)。 | |||
T1449 |
Hydrochlorothiazide
HCTZ,双氢氯噻嗪,氢氯噻嗪 |
Potassium Channel; Carbonic Anhydrase; TGF-beta/Smad | Membrane transporter/Ion channel; Metabolism; Stem Cells |
Hydrochlorothiazide (HCTZ) 是一种口服有效的噻嗪类的利尿药,可抑制转化 TGF-β/Smad 信号通路。它通过打开钙激活钾 (KCA) 通道发挥直接的血管松弛作用。它改善心脏功能,减少纤维化并具有降压作用。 | |||
T3636 |
(E)-SIS3
SIS3,SIS3 盐酸盐,SIS3 HCl |
TGF-beta/Smad | Stem Cells |
(E)-SIS3 (SIS3) 是 Smad3 的选择性抑制剂,能够抑制 Smad3 磷酸化(IC50:3 μM)。它利用 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。 | |||
T5129 |
SRI-011381 hydrochloride
SRI-011381 hydrochloride [1629138-41-5(free base)] |
TGF-beta/Smad | Stem Cells |
SRI-011381 hydrochloride 是口服具有活力的TGF-β信号通路的激活剂,具有神经保护活性。 | |||
T5125 |
LY3200882
|
TGF-beta/Smad | Stem Cells |
LY3200882 是一种高度选择性的、口服活性的、具有 ATP 竞争性的 TGF-β 受体 1 型 (ALK5) 抑制剂(IC50:38.2 nM)。它能够抑制多种促肿瘤活性,可用作免疫调节剂。 | |||
T2386 |
Pirfenidone
S-7701,AMR-69,S-7701,AMR69,吡非尼酮 |
CCR; TGF-beta/Smad | Immunology/Inflammation; Microbiology/Virology; Stem Cells |
Pirfenidone (AMR69) 是一种抗纤维化剂,可减弱纤维细胞中CCL2和CCL12的产生。它可抑制细胞生长,并能降低人胶质瘤细胞系中的TGF-β2蛋白水平,具有抗炎活性。 | |||
T7799 |
BMP signaling agonist sb4
SB 4 |
TGF-beta/Smad | Stem Cells |
BMP signaling agonist sb4 (SB 4) 是苯并恶唑骨形态发生蛋白 4 (BMP4) 信号激动剂(EC50:74 nM),能够稳定细胞内 p-SMAD-1/5/9 ,激活 BMP 信号。它还能激活典型 BMP 信号通路中的 BMP4 靶基因 (DNA 结合抑制剂,Id1和Id3)。 | |||
T6496 |
Vactosertib
TEW-7197,EW-7197 |
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
Vactosertib (EW-7197) 是有效的、具有 ATP 竞争性的、具有口服活性的激活素受体样激酶 5 (ALK5) 抑制剂(IC50:12.9 nM)。它还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50为 17.3 nM),表现出强大的抗转移活性和抗癌作用。 | |||
T74204 |
Trabedersen
|
Others | Others |
Trabedersen (AP 12009) 是一种反义寡脱氧核苷酸,可特异性抑制 TGF-β2(TGF-beta/Smad)。Trabedersen 可用于研究恶性脑肿瘤和其他过度表达 TGF-β2的实体瘤,例如皮肤、胰腺和结肠肿瘤。 | |||
T3689L |
Ruboxistaurin mesylate
LY-333531,LY333531,LY 333531,LY-333531 Mesylate |
Others | Others |
Ruboxistaurin is a PKC beta inhibitor. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/ | |||
T69990 |
Ruboxistaurin mesylate monohydrate
|
Others | Others |
Ruboxistaurin mesylate monohydrate is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0184 |
Chebulinic acid
|
ATPase; Proton pump; DNA/RNA Synthesis; Antibacterial; TGF-beta/Smad | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Stem Cells |
Chebulinic acid 是从诃子果中提取的一种天然产物,结核分枝杆菌 DNA 促旋酶的有效抑制剂。它也能抑制 SMAD-3 phosphorylation 和 H+ K+-ATPase 的活性。 | |||
T13741 |
Isoviolanthin
异佛莱心苷,异佛来心苷 |
Others | Others |
Isoviolanthin 是一种黄酮类苷类化合物,提取自铁皮石斛叶中。它能减少 TGF-β1 处理的 HCC 细胞的迁移和入侵能力,对正常细胞没有毒性影响,对转移性肝癌晚期具有潜在的研究价值。 | |||
T2754 |
Oxymatrine
Oxysophoridine,氧化苦参碱,Matrine N-oxide |
Influenza Virus; Autophagy; TGF-beta/Smad | Autophagy; Microbiology/Virology; Stem Cells |
Oxymatrine (Oxysophoridine) 是来自槐属物种根部的一种生物碱,具有抗炎,抗纤维化和抗肿瘤的作用。它是一种用于治疗乙型肝炎病毒的中药。它可抑制博卡病毒 MVC 复制,降低病毒基因表达并减少病毒感染诱导的细胞凋亡。它还可以抑制 iNOS 的表达和 TGF-β/Smad 通路。 | |||
T5247 |
Trimethylamine N-oxide dihydrate
二水氧化三甲胺,TMANO Dihydrate |
Others; Endogenous Metabolite | Metabolism; Others |
Trimethylamine N-oxide dihydrate (TMANO Dihydrate) 是内源性代谢产物的一种。 | |||
T6856 |
Halofuginone
卤夫酮,常山酮,Tempostatin,empostatin,RU-19110 |
Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Stem Cells |
Halofuginone (RU-19110) 是Febrifugine 的衍生物,是一种竞争性脯氨酰-tRNA 合成酶抑制剂。它也是肺血管扩张剂,可激活Kv 通道并阻断电压门控、受体操作和存储操作的钙离子通道。它具有抗炎、抗癌、抗疟疾和抗纤维化作用。 | |||
T2896 |
Alantolactone
土木香内酯,helenin,Eupatal,Helenine,(+)-Alantolactone,Alant camphor,土木香脑,Inula camphor |
Apoptosis; STAT; TGF-beta/Smad | Apoptosis; JAK/STAT signaling; Stem Cells |
Alantolactone (Inula camphor) 是一种STAT3的选择性抑制剂,可诱导癌症相关的凋亡,具有抗肿瘤活性。 | |||
T3524 |
Halofuginone hydrobromide
卤夫酮溴氢酸盐,Tempostatin,RU-19110 (hydrobromide),Stenorol,常山酮溴酸盐 |
Others; Calcium Channel; DNA/RNA Synthesis; Sodium Channel; Parasite; TGF-beta/Smad | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Others; Stem Cells |
Halofuginone hydrobromid 是Febrifugine 的衍生物,是竞争性脯氨酰-tRNA 合成酶抑制剂。它是 I 型胶原合成的特异性抑制剂,并通过抑制TGF-β活性可减轻骨关节炎。它具有抗疟疾、抗炎、抗癌、抗纤维化作用。 | |||
T3025 |
Asiaticoside
BRN0078195,CCRIS8995,Emdecassol,Ba 2742,Madecassol,积雪草皂苷,NSC166062,积雪草苷 |
Apoptosis; p38 MAPK; Reactive Oxygen Species; Endogenous Metabolite; TGF-beta/Smad | Apoptosis; Immunology/Inflammation; MAPK; Metabolism; NF-κB; Stem Cells |
Asiaticoside (Emdecassol) 是一种从积雪草中分离得到的三萜皂苷化合物,具有抗氧化、抗炎、抗溃疡等作用。在瘢痕疙瘩成纤维细胞中,它通过活化 Smad7,抑制 TGF-βRI 和 TGF-βRII,抑制 TGF-β/Smad 信号通路。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-03291 |
SMAD2 Protein, Mouse, Recombinant (His & GST)
mMad2,Smad-2,7120426M23Rik,Madr2,Madh2,SMAD |
Mouse | Baculovirus Insect Cells |
SMAD2 is a member of the SMAD family. Members of this family mediate signal transduction by the TGF-beta/activin/BMP-2/4 cytokine superfamily from receptor Ser/Thr protein kinases at the cell surface to the nucleus. SMAD2 mediates the signal of the TGF-beta, and therefore regulates multiple cellular processes, such as cell proliferation, apoptosis, and differentiation. SMAD2 is recruited to the TGF-beta receptors through its interaction with the SMAD anchor for receptor activation (SARA) protein... | |||
TMPJ-00271 |
SMAD3 Protein, Human, Recombinant (His & Flag)
SMAD 3,Mothers against DPP homolog 3,hMAD-3,MADH3,J... |
Human | E. coli |
Mothers against decapentaplegic homolog 3(SMAD3) is a cytoplasm protein which belongs to the dwarfin/SMAD family. Smad proteins undergo rapid nuclear translocation upon stimulation by transforming growth factor and in so doing transduce the signal into the nucleus. Receptor-regulated SMAD is an intracellular signal transducer and transcriptional modulator activated by TGF-beta and activin type 1 receptor kinases. SMAD3 binds the TRE element in the promoter region of many genes that are regulated... | |||
TMPH-01699 |
SMAD2 Protein, Human, Recombinant (His & SUMO)
JV18-1,SMAD2,SMAD family member 2,Mothers ... |
Human | E. coli |
Receptor-regulated SMAD (R-SMAD) that is an intracellular signal transducer and transcriptional modulator activated by TGF-beta (transforming growth factor) and activin type 1 receptor kinases. Binds the TRE element in the promoter region of many genes that are regulated by TGF-beta and, on formation of the SMAD2/SMAD4 complex, activates transcription. May act as a tumor suppressor in colorectal carcinoma. Positively regulates PDPK1 kinase activity by stimulating its dissociation from the 14-3-3... | |||
TMPY-00499 |
TMP21 Protein, Human, Recombinant (mFc)
Tmp-21-I,p23,S31III125,TMP21,P24(DELTA),transmembrane emp24-... |
Human | HEK293 Cells |
TMED10 disrupts the complex formation between TGF-beta type I (also termed ALK5) and type II receptors (TbetaRII). Misexpression studies revealed that TMED10 attenuated TGF-beta-mediated signaling. A 20-amino acid-long region from Thr(91) to Glu(110) within the extracellular region of TMED10 was found to be crucial for TMED10 interaction with both ALK5 and TbetaRII. Synthetic peptides corresponding to this region inhibit both TGF-beta-induced Smad2 phosphorylation and Smad-dependent transcriptio... | |||
TMPJ-01178 |
TGFBR1 Protein, Mouse, Recombinant (hFc)
ALK-5,ALK-5ALK5,TGFβRI,tβR-I,LDS1A,TGF... |
Mouse | HEK293 Cells |
TGF-beta RI, also called ALK-5, is an approximately 55 kDa type I transmembrane serine/threonine receptor kinase. In the presence of TGF-beta, TGF-beta RI forms a complex with, and is phosphorylated by, TGF-beta RII. Phosphorylated TGF-beta RI can then transiently bind and phosphorylate Smad2 and Smad3. TGF-beta functions as a tumor suppressor by inhibiting the cell cycle in the G1 phase. Administration of TGF-beta is able to protect against mammary tumor development in transgenic mouse models i... | |||
TMPH-01702 |
SMAD6 Protein, Human, Recombinant (E. coli, His & Myc)
SMAD6,Mothers against decapentaplegic homolog 6, |
Human | E. coli |
Transforming growth factor-beta superfamily receptors signaling occurs through the Smad family of intracellular mediators. SMAD6 is an inhibitory Smad (i-Smad) that negatively regulates signaling downstream of type I transforming growth factor-beta. Acts as a mediator of TGF-beta and BMP anti-inflammatory activities. Suppresses IL1R-TLR signaling through its direct interaction with PEL1, preventing NF-kappa-B activation, nuclear transport and NF-kappa-B-mediated expression of proinflammatory gen... | |||
TMPY-04203 |
RAB1B Protein, Human, Recombinant (hFc)
RAB1B, member RAS oncogene family |
Human | HEK293 Cells |
RAB1B, a member of the RAS oncogene family, was significantly down-regulated in highly metastatic breast cancer cells. Moreover, down-regulation of RAB1B was also found to promote the proliferation and migration of TNBC cells in vitro and in vivo. Mechanistically, loss of RAB1B resulted in elevated expression of TGF-beta receptor 1 (TbetaR1) through decreased degradation of ubiquitin, increased levels of phosphorylated SMAD3 and TGF-beta-induced epithelial-mesenchymal transition (EMT). Furthermo... | |||
TMPY-03419 |
SMAD3 Protein, Human, Mouse, Rat, Recombinant (His & GST)
SMAD family member 3 |
Human,Mouse,Rat | Baculovirus Insect Cells |
SMAD3 belongs to the SMAD family. Members of this family mediate signal transduction by the TGF-beta/activin/BMP-2/4 cytokine superfamily from receptor Ser/Thr protein kinases at the cell surface to the nucleus. SMAD3 is involved in cell signalling. It modulates signals of activin and TGFβ's. Binding of SMAD3 with SMAD4 enables its transmigration into the nucleus where it forms complexes with other proteins and acts as a transcription factor. SMAD3 is a receptor-regulated SMAD (R-SMAD). In mice,... | |||
TMPY-04468 |
STK16 Protein, Human, Recombinant (His & NusA)
MPSK,serine/threonine kinase 16,TSF1,KRCT,PKL12 |
Human | E. coli |
Serine/threonine-protein kinase 16, also known as myristoylated and palmitoylated serine/threonine-protein kinase, Protein kinase PKL12, TGF-beta-stimulated factor 1, TSF-1, MPSK1 and STK16, is a membrane protein that is ubiquitously expressed at very low levels. STK16 / MPSK1 belongs to the protein kinase superfamily and Ser/Thr protein kinase family. It contains one protein kinase domain. Transforming growth factor-beta (TGF-beta) shows a variety of biological activities in various organs or c... | |||
TMPH-01015 |
BMP-3 Protein, Human, Recombinant (His)
BMP3A,Bone morphogenetic protein 3A,BMP3,Osteogenin,Bone mor... |
Human | E. coli |
Growth factor of the TGF-beta superfamily that plays an essential role in developmental process by inducing and patterning early skeletal formation and by negatively regulating bone density. Antagonizes the ability of certain osteogenic BMPs to induce osteoprogenitor differentitation and ossification. Initiates signaling cascades by associating with type II receptor ACVR2B to activate SMAD2-dependent and SMAD-independent signaling cascades including TAK1 and JNK pathways. BMP-3 Protein, Human, R... | |||
TMPJ-01158 |
ALK-2/ACVR1 Protein, Human, Recombinant (hFc)
ACVRLK2,FOP,Activin RIA,ACTRI,ALK-2,activin A receptor, type... |
Human | HEK293 Cells |
Activin RIA, also known as ALK-2, TSK-7L, SKR1, TSR-I, and ACTR-I, is a glycosylated 65 kDa type I receptor in the TGF-beta serine/threonine kinase receptor family. Binding of TGF-beta superfamily ligands induces formation of a heterotetrameric complex that contains two chains each of a type I and a type II receptor in multiple combinations. The type II receptors phosphorylate the type I receptors which then phosphorylate and activate Smad signal transduction proteins. Activin RIA functions in a... |