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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 |
---|---|---|---|
T9205 |
NCGC00378430
|
Phosphatase; Others | Metabolism; Others |
NCGC00378430 是一种 SIX1/EYA2 相互作用抑制剂。它部分逆转 SIX1 过表达介导的转录和代谢谱,并逆转 SIX1 诱导的 TGF-β 信号传导和上皮-间质转化。在小鼠模型中,它能够抑制 SIX1 介导的乳腺癌转移。 | |||
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。 | |||
T9953 |
BT173
|
Others | Others |
BT173 是一种新型的同源域相互作用蛋白激酶 2 (HIPK2) 抑制剂,通过抑制 TGF-β1/Smad3 通路减轻肾纤维化。 | |||
T15572 |
IN-1130
|
ALK | Angiogenesis; Tyrosine Kinase/Adaptors |
IN-1130 是一种选择性的 ALK5 抑制剂,对 ALK5 介导的 Smad3 磷酸化、酪蛋白和 p38α 丝裂原活化蛋白激酶的 ALK5 磷酸化,IC50 值为 5.3 nM、36 nM 和 4.3 μM。 | |||
T2247 |
KenPaullone
9-Bromopaullone,NSC-664704,9-溴-7,12-二氢吲哚并[3,2-D][1]苯并氮杂卓-6(5H)-酮 |
GSK-3; CDK | Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells |
KenPaullone (9-Bromopaullone) 是一种CDK1/cyclin B 和GSK-3β抑制剂,IC50值分别为 0.4 μM 和 23 nM。它也抑制 CDK2/cyclin A、CDK2/cyclin E 和 CDK5/p25 的活性,IC50值分别为 0.68 μM、7.5 μM 和 0.85 μM。。它通过增强 TGFβ-Smad3 信号通路增加和延长 foxp3 基因的转录来促进 iTreg 细胞分化。 | |||
T24470 |
Mitochonic Acid 35
MA35,MA-35,MA 35,Mitochonic Acid-35 |
Others | Others |
Mitochonic Acid 35 is a dual TNF-α and TGF-β1 inhibitor that acts by inhibiting IκB kinase phosphorylation and Smad3 phosphorylation. | |||
T12923 |
(Rac)-SIS3 free base
|
TGF-beta/Smad | Stem Cells |
SIS3 free base is a potent and selective Smad3 phosphorylation inhibitor. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. | |||
T80628 |
Myristoyl tetrapeptide-12
|
TGF-beta/Smad | Stem Cells |
Myristoyl tetrapeptide-12 直接激活SMAD2,并促使SMAD3与DNA结合。该化合物能有效促进毛发,特别是睫毛的生长。 | |||
T72383 |
3,3-Dimethyl-1-butanol
Neohexanol,DMB,DMB ; Neohexanol |
Others | Others |
3,3-Dimethyl-1-butanol (DMB)是一种口服有效的三甲胺(TMA)和三甲基胺-N-氧化物(TMAO)抑制剂,能够抑制p65NF-κB和TGF-β1/Smad3信号通路,展示了在心血管疾病(CVD)中的潜在应用。 | |||
T74544 |
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
|
PROTACs | PROTAC |
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine 是一种能同时靶向Smad3的泛素化和降解并提高HIF-α蛋白水平的双靶点PROTAC,展现出对肾性贫血的多途径抗纤维化和肾脏保护作用。 | |||
T61203 |
ALK5-IN-8
|
Others | Others |
ALK5-IN-8 is a highly effective inhibitor of TGFβRI (ALK5). It hinders the phosphorylation of ALK5 on downstream signaling proteins (Smad2 or Smad3) by obstructing the interaction between TGFβRI and ligands. Consequently, it disrupts or prevents TGF-β signaling. ALK5-IN-8 shows promise in the study of diverse diseases associated with ALK5-mediated pathways[1]. | |||
T61586 |
TGFβ-IN-2
|
Others | Others |
TGFβ-IN-2 (Compound 9d) effectively inhibits the accumulation of total collagen induced by TGF-β in NRK-49F cells, with an IC 50 value of 4.31 μM. It also suppresses the in vitro protein expression of COL1A1, α-SMA, and p-Smad3, which are induced by TGF-β. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1]. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T14854 |
Caerulomycin A
浅蓝霉素,Cerulomycin,Caerulomycin |
Antifungal | Microbiology/Virology |
Caerulomycin A (Caerulomycin) 是抗真菌和抗细菌化合物,能够诱导 T 细胞的产生。它能够抑制 IFN-γ 诱导的 STAT1 通路,从而增强 TGF-β-Smad3 信号通路。它可用于自身免疫病的研究。 | |||
T4938 |
Potassium 1H-indol-3-yl sulfate
硫酸吲哚钾盐,Indoxyl sulfate potassium salt,Potassium 3-indoxyl sulfate |
AhR; Endogenous Metabolite | Immunology/Inflammation; Metabolism |
Potassium 1H-indol-3-yl sulfate (Potassium 3-indoxyl sulfate) 是人芳烃受体(AhR)的激动剂。芳烃受体(AhR)最近被发现是免疫炎症条件的病理生理调节剂,Potassium 1H-indol-3-yl sulfate 已被证明是AhR的配体。Potassium 1H-indol-3-yl sulfate 也是膳食蛋白质中色氨酸的代谢物。色氨酸被肠道细菌代谢为吲哚,吲哚被吸收到血液中,然后在肝脏中进一步代谢为硫酸吲哚,通常通过尿液排出体外。在肾功能受损的慢性肾病患者中,Potassium 1H-indol-3-yl sulfate 可作为尿毒症毒素在血清中积累,诱导氧化应激并加速疾病进展。250 μM Potassium 1H-indol-3-yl sulfate 可诱导NF-Κb活化,促进大鼠近端小管细胞TGF-β1和Smad3的表达,与促纤维化活性相关。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01700 |
SMAD3 Protein, Human, Recombinant (His)
JV15-2,SMAD family member 3,SMAD<... |
Human | Baculovirus Insect Cells |
SMAD3 Protein, Human, Recombinant (His) is expressed in Baculovirus insect cells with N-10xHis tag. The predicted molecular weight is 50.6 kDa and the accession number is P84022. | |||
TMPJ-00271 |
SMAD3 Protein, Human, Recombinant (His & Flag)
SMAD 3,Mothers against DPP homolog 3 |
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... | |||
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,... | |||
TMPH-03764 |
YAP1 Protein, Human, Recombinant (His)
YAP1-2gamma,YAP2L,YAP65 |
Human | P. pastoris (Yeast) |
Transcriptional regulator which can act both as a coactivator and a corepressor and is the critical downstream regulatory target in the Hippo signaling pathway that plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1,... | |||
TMPH-02055 |
RBPMS Protein, Human, Recombinant (His & Myc)
RBPMS,Heart and RRM expressed sequence,RNA-binding protein w... |
Human | E. coli |
Acts as a coactivator of transcriptional activity. Required to increase TGFB1/Smad-mediated transactivation. Acts through SMAD2, SMAD3 and SMAD4 to increase transcriptional activity. Increases phosphorylation of SMAD2 and SMAD3 on their C-terminal SSXS motif, possibly through recruitment of TGFBR1. Promotes the nuclear accumulation of SMAD2, SMAD3 and SMAD4 proteins. Binds to poly(A) RNA. RBPMS Protein, Human, Recombinant (His & Myc) is expressed in E. coli expression system with N-10xHis and C-... | |||
TMPH-02866 |
RBBP9 Protein, Mouse, Recombinant (His)
Retinoblastoma-binding protein 9,Putative hydrolase RBBP9,B5... |
Mouse | P. pastoris (Yeast) |
Serine hydrolase whose substrates have not been identified yet. May negatively regulate basal or autocrine TGF-beta signaling by suppressing SMAD2-SMAD3 phosphorylation. May play a role in the transformation process due to its capacity to confer resistance to the growth-inhibitory effects of TGF-beta through interaction with RB1 and the subsequent displacement of E2F1. RBBP9 Protein, Mouse, Recombinant (His) is expressed in yeast with C-6xHis tag. The predicted molecular weight is 22.4 kDa and t... | |||
TMPJ-00936 |
CCND2 Protein, Human, Recombinant (His)
G1/S-specific cyclin-D2,CCND2 |
Human | E. coli |
CCND2,also known as G1/S-specific cyclin-D2,is a member of the highly conserved cyclin family. Different cyclins exhibit distinct expression and degradation patterns which contribute to the temporal coordination of each mitotic event. Cyclins function as regulators of CDK kinases. This cyclin forms a complex with and functions as a regulatory subunit of CDK4 or CDK6, whose activity is required for cell cycle G1/S transition. CCND2 is involved in a number of fundamental biological processes such ... | |||
TMPH-01413 |
GDF11 Protein, Human, Recombinant (His & SUMO)
Bone morphogenetic protein 11,GDF11,Growth/differentiation f... |
Human | E. coli |
Secreted signal that acts globally to regulate anterior/posterior axial patterning during development. May play critical roles in patterning both mesodermal and neural tissues. It is required for proper vertebral patterning and orofacial development. Signals through activin receptors type-2, ACVR2A and ACVR2B, and activin receptors type-1, ACVR1B, ACVR1C and TGFBR1 leading to the phosphorylation of SMAD2 and SMAD3. GDF11 Protein, Human, Recombinant (His & SUMO) is expressed in E. coli expression... | |||
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-02444 |
ATF2 Protein, Human, Recombinant (His & GST)
CREB2,CRE-BP1,CREB-2,TREB7,activating transcription factor 2... |
Human | Baculovirus Insect Cells |
Activating transcription factor 2, also known as ATF2, is a member of the leucine zipper family of DNA-binding proteins that binds to the cAMP response element. Its activity is enhanced after phosphorylation by stress-activated protein kinases such as c-Jun N-terminal kinase and p38. ATF2 has been found to be a target of the JNK signal transduction pathway and mediate adenovirus E1A-inducible transcriptional activation. ATF2 is also been reported playing roles in TGF-β signaling pathway. It has ... | |||
TMPJ-01108 |
SMAD4 Protein, Human, Recombinant (His)
DPC4,SMAD 4,Deletion Target in Pancreatic Carcinoma... |
Human | E. coli |
SMAD Family Member 4 (SMAD4) is a cytoplasmic protein that belongs to the Dwarfin/SMAD family. SMAD4 contains one MH1 (MAD homology 1) domain and one MH2 (MAD homology 2) domain. It is the component of the heterotrimeric SMAD2/SMAD3-SMAD4 complex that forms in the nucleus and is required for the TGF-mediated signaling. SMAD4 promotes binding of the SMAD2/SMAD4/FAST-1 complex to DNA and provides an activation function required for SMAD1 or SMAD2 to stimulate transcription. SMAD4 may act as a tumo... | |||
TMPY-03861 |
Amelotin Protein, Human, Recombinant (mFc)
amelotin,UNQ689 |
Human | HEK293 Cells |
Amelotin (AMTN) is a tooth enamel protein which is expressed in maturation-stage ameloblasts and also in the internal basal lamina of junctional epithelium, a unique epithelial structure attached to the tooth surface which protects against the constant microbiological challenge to the periodontium. TNF-α stimulates AMTN gene transcription in human gingival epithelial cells via C/EBP1, C/EBP2, and YY1 elements in the human AMTN gene promoter.AMTN mRNA levels increased at 6 h and reached maximum a... | |||
TMPH-01269 |
SMURF2 Protein, Human, Recombinant (His)
SMAD ubiquitination regulatory factor 2,E3... |
Human | E. coli |
E3 ubiquitin-protein ligase which accepts ubiquitin from an E2 ubiquitin-conjugating enzyme in the form of a thioester and then directly transfers the ubiquitin to targeted substrates. Interacts with SMAD7 to trigger SMAD7-mediated transforming growth factor beta/TGF-beta receptor ubiquitin-dependent degradation, thereby downregulating TGF-beta signaling. In addition, interaction with SMAD7 activates autocatalytic degradation, which is prevented by interaction with AIMP1. Also forms a stable com... | |||
TMPY-04422 |
Casein Kinase 1 gamma 2 Protein, Human, Recombinant (His)
CK1g2,casein kinase 1, γ2,casein kinase 1, gamma 2,Casein Ki... |
Human | Baculovirus Insect Cells |
Casein kinase I gamma 2 isoform (CSNK1G2), a member of the large casein kinase I (CKI) subfamily, protein kinase superfamily. It may affect the development of brain, and associate with vesicular trafficking and neurotransmitter releasing from small synaptic vesicles. The CKI family includes several other isoforms (alpha, beta, gamma, and delta). Dishevelled (Dsh), another positive component of the Wnt pathway, becomes phosphorylated in response to Wnt signals. All the CKI isoforms, with the exce... | |||
TMPJ-01178 |
TGFBR1 Protein, Mouse, Recombinant (hFc)
ALK-5,ALK-5ALK5,TGFβRI,tβR-I,LDS1A,TGFbetaRI,TGFB1R1,activin... |
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... | |||
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... |