TGF-beta/Smad
信号通路图
研究领域
抑制剂选择性比较
TGF-beta/Smad产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1067 |
SB431542SB431542是一种有效的，选择性ALK5抑制剂，无细胞试验中IC50为94 nM，对ALK5的作用比对p38、MAPK和其他激酶强100倍。 |
Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01. |
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| S2618 |
LDN-193189LDN-193189是一种选择性的BMP信号通路抑制剂，抑制BMP I型受体ALK2和ALK3的转录活性，在C2C12细胞中IC50分别为5 nM和30 nM，作用于BMP比作用于TGF-β选择性高200倍。 |
LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment. |
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| S2230 |
Galunisertib (LY2157299)Galunisertib (LY2157299)是有效的TGFβ receptor I (TβRI)抑制剂，无细胞试验中IC50为56 nM。Phase 2/3。 |
Cells were treated in both formats with 10 uM of SB525334 (TGFβR1), SJN 2511 (TGFβR1), LY2157299 (TGFβR2, TGFβR1), Dorsomorphin (AMPK, ALK2, ALK3, ALK6), DMH-1 (ALK2), or GW5074 (c-raf), or 50 ng/ml of TGF-β. Microtissue or tissue-culture well fluorescence for each condition are shown after 3 days of culture for 393T5 cells, which proliferate slower in control conditions, so that the two cell lines undergo the same number of population doublings during each assay. |
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| S2704 |
LY2109761LY2109761是一种新型的，选择性TGF-β receptor type I/II (TβRI/II)双重抑制剂，无细胞试验中Ki分别为38 nM和300 nM，对Smad2的磷酸化产生负面影响。 |
The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.
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| S1476 |
SB525334SB525334是一种有效的，选择性TGFβ receptor I (ALK5)抑制剂，无细胞试验中IC50为14.3 nM，作用于ALK4比作用于ALK5效果低4倍，对ALK2，3，和 6没有活性。 |
LS 174T and SW480 cells were treated with SB525334 (1 umol/L) for 12 hours. HMGA2 expression was assessed by immunoblotting. Each experiment was repeated 3 times. Bars, SD; *, P < 0.05; **, P < 0.01.
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| S6713New |
ITD-1ITD-1是有效的TGF-β抑制剂。它不抑制TGFBR1或TGFBR的激酶活性，但能够有效地抑制TGFβ2诱导的效应因子SMAD2/3磷酸化，对Activin A的影响甚微。 |
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| S8868New |
NG25NG25是一种新型的TAK1抑制剂，对TAK1和MAP4K2的IC50分别为149 nM和21.7 nM。 |
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| S8772New |
LY 3200882LY 3200882是有效的、高选择性TGF-β receptor type 1 (TGFβRI)抑制剂，在体外肿瘤组织和免疫细胞以及体内皮下肿瘤中，有效地以浓度依赖方式抑制TGFβ介导的SMAD磷酸化。 |
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| S2186 |
SB505124SB505124是一种选择性TGFβR抑制剂，作用于ALK4和ALK5，无细胞试验中IC50分别为129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。 |
(D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.
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| S2907 |
PirfenidonePirfenidone抑制TGF-β产生和TGF-β刺激的胶原蛋白产生，且降低TNF-α和IL-1β产生，具有抗纤维化和抗炎特性。Phase 3。 |
Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.
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| S2750 |
GW788388GW788388是一种有效的，选择性ALK5抑制剂，无细胞试验中IC50为18 nM，也抑制TGF-βII型受体和activin II型受体活性，但不抑制BMP II型受体。 |
Combination treatment with GW788388 and IL-23 aiming to sustain Th17 cell levels increases spleen cell production of the inflammatory mediators IL-17 and TNF-a, the stimulatory mediators IL-2, IFN-g and RANTES, and the inhibitory mediator IL-10. Starting from Week 6 of 4NQO administration, when premalignant oral lesions were detectable on the tongue, mice were initiated on treatment with diluent, GW788388, IL-23 or both GW788388 and IL-23. After 2 months of these treatments, spleens were collected and cultured on anti-CD3 for 3 days. Supernatants were collected and used for measurement of the inflammatory mediators IL-17, TNF-a and IL-6 (a); stimulatory mediators IL-2, IFN-g and RANTES (b); and inhibitory mediators, TGF-b, IL-4 and IL-10 (c). *=p<0.05, **=p<0.01, ***=p<0.001.
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| S2805 |
LY364947LY364947是一种有效的ATP竞争性TGFβR-I抑制剂，无细胞试验中IC50为59 nM，比作用于TGFβR-II选择性高7倍。 |
The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively. |
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| S7223 |
RepSoxRepSox是一种有效的，选择性TGFβR-1/ALK5抑制剂，作用于ATP与ALK5结合以及ALK5自磷酸化，无细胞试验中IC50分别为23 nM和4 nM。 |
(C) Generation of pluripotent stem cell from Yamanaka factors-induced OG2-MEFs under treatment of diverse chemical compounds. Images of GFP+ colonies were taken on day 10 post-infection. VPA, 0.5 mmol/L. CHIR99021, 3 μmol/L. Repsox, 1 μmol/L. (D) Quantification of GFP+ colonies in (C). All figures are representative of three independent experiments (n = 3). All data are presented as mean ± SD. *P < 0.05, **P < 0.01 vs. DMSO
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| S7507 |
LDN-193189 2HClLDN193189 HCl是LDN193189的盐酸盐，是一种选择性BMP信号抑制剂，它能抑制BMP type I receptors ALK2和ALK3的转录活性，在C2C12细胞中IC50分别为5 nM 和 30 nM, 并且对于BMP的选择性是对TGF-β选择性的200倍。 |
LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
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| S7359 |
K02288K02288是一种高度选择性I型BMP受体抑制剂，针对 ALK2， ALK1和ALK6的IC50分别为1.1，1.8，6.4 nM，显示对其他ALKS（3，4，5）和的ActRIIa 有轻微抑制作用。 |
A549 cells were transfected with miR-205 inhibitor (IHT-205, 100 nM). Forty hours after transfection, the cells were seeded on transwell plates and treated with or without inhibitor K02288 (10 nM), AG1478 (1 µM), SB431542 (10 µM) for 10 hours. Migrated cells were quantified. All data are shown as mean± SD. N =3. All experiments have been repeated at least 3times independently. |
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| S7624 |
SD-208SD-208是一种选择性TGF-βRI (ALK5)抑制剂，with IC50为48 nM，选择性比TGF-βRII高100多倍。 |
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| S7627 |
LDN-214117LDN-214117是一种有效的选择性 BMP I型受体激酶 ALK2 抑制剂，IC50为 24 nM。 |
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| S7959 |
SIS3 HClSIS3是一种新型的特异性Smad3抑制剂，通过抑制Smad3的磷酸化抑制TGF-β和activin信号，而不影响MAPK/p38, ERK或PI3-kinase信号通路。 |
Cultured cardiac fibroblasts infected with vector lentiviruses or EphrinB2 overexpressing lentiviruses were stimulated with specific antagonist against Stat3 (Stattic, 2.5μM) and/or Smad3 (SIS3, 1μM), respectively. The expression level of α-SMA was quantified via western blotting. In vitro experiments repeat 3 times, *P<0.05, **P<0.01. |
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| S7530 |
Vactosertib (TEW-7197, EW-7197)Vactosertib (TEW-7197) 是一种高效的，选择性的，口服生物有效的TGF-β receptor ALK4/ALK5抑制剂，IC50分别为13 nM 和 11 nM。Phase 1。 |
Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.
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| S7146 |
DMH1DMH1是选择性BMP receptor抑制剂，抑制ALK2，IC50为107.9 nM,对AMPK, ALK5, KDR (VEGFR-2)和PDGFR没有抑制效果。 |
The combined treatment with miR-140-5p mimics and some common chemotherapeutics did not have any effect on the SK-MES1 cell line, whereas miR-140-5p and DMH1 and cisplatin decreased the proliferation of
the A549 cells. Data are presented as mean±SEM of three individual experiments undertaken in triplicate. t-Test was used to assess significance with *p<0.05.
|
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| S7147 |
LDN-212854LDN-212854 是一种强效的选择性BMP receptor抑制剂， 其作用于ALK2的IC50为1.3 nM , 分别超过作用于ALK1, ALK3, ALK4, 和 ALK5的选择性约 2-, 66-, 1641-, 和 7135倍。 |
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| S7148 |
ML347ML347 是一种选择性的BMP receptor抑制剂，其作用于ALK2的IC50为 32 nM ,选择性高于ALK3 300倍。 |
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| S7658 |
KartogeninKartogenin是一种smad4/smad5通路激活剂，促进多功能间充质干细胞选择性分化为软骨细胞。 |
||
| S2308 |
HesperetinHesperetin是一种生物类黄酮，更具体而言，是一种二氢黄酮。 |
||
| S8318 |
AlantolactoneAlantolactone，一种天然的桉烷类倍半萜内酯，能诱导activin/SMAD3信号、干扰Cripto-1/activin受体ⅡA型受体的相互作用。 |
Colon cancer cell lines (A) SW620, (B) HCT116, and (C) HT29 were treated with different concentrations (60, 12, 2.4, 0.48, and 0.098 μM) of nifuroxazide (nifu), niclosamide (nicl), cryptotanshinone (cry), and a lantolactone (ala), respectively, for 72 h. Cell proliferation in each group was detected by MTT assay. (D) HCT116, SW620, and HT29 cell lines were suppressed with niclosamide treatment at different concentrations (20, 10, 5, 2.5, and 1.25 μM) for 72 h. Subsequently, cell proliferation in each group was detected by MTT assay. The data were obtained from 3 independent experiments.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1067 |
SB431542SB431542是一种有效的，选择性ALK5抑制剂，无细胞试验中IC50为94 nM，对ALK5的作用比对p38、MAPK和其他激酶强100倍。 |
Long-term response of SB431542 and SB203580 release from scaffold implants. Histological results of H&E staining showing the capsule thickness of the various treatments at 14 days. The scale bar shows 100 uM and is applicable to all images in the panel. In each bar graph the tissue and cellular response to SB431542 were found to be significant from the control. For each treatment group six animals were tested. Statistics are performed by ANOVA with Bonferroni comparisons and taken to be significant at ∗∗P < 0.01. |
|
| S2618 |
LDN-193189LDN-193189是一种选择性的BMP信号通路抑制剂，抑制BMP I型受体ALK2和ALK3的转录活性，在C2C12细胞中IC50分别为5 nM和30 nM，作用于BMP比作用于TGF-β选择性高200倍。 |
LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment. |
|
| S2230 |
Galunisertib (LY2157299)Galunisertib (LY2157299)是有效的TGFβ receptor I (TβRI)抑制剂，无细胞试验中IC50为56 nM。Phase 2/3。 |
Cells were treated in both formats with 10 uM of SB525334 (TGFβR1), SJN 2511 (TGFβR1), LY2157299 (TGFβR2, TGFβR1), Dorsomorphin (AMPK, ALK2, ALK3, ALK6), DMH-1 (ALK2), or GW5074 (c-raf), or 50 ng/ml of TGF-β. Microtissue or tissue-culture well fluorescence for each condition are shown after 3 days of culture for 393T5 cells, which proliferate slower in control conditions, so that the two cell lines undergo the same number of population doublings during each assay. |
|
| S2704 |
LY2109761LY2109761是一种新型的，选择性TGF-β receptor type I/II (TβRI/II)双重抑制剂，无细胞试验中Ki分别为38 nM和300 nM，对Smad2的磷酸化产生负面影响。 |
The inhibition of TGF-β1 signaling pathways suppressed EBV-mediated EMT, and prevented the activation of Syk and Src signaling. The EBV-infected HCECs were treated with 100 nM of the dual TGF-β receptor I and II kinase inhibitor, LY2109761, for 48 hours. The EBV-infected HCECs were cultured with anti-TGF-β1 neutralizing antibody (5 ug/mL) or mouse IgG1 antibody (5 ug/mL) for 48 hours. Photographs were taken at x100 magnification by a digital camera.
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| S1476 |
SB525334SB525334是一种有效的，选择性TGFβ receptor I (ALK5)抑制剂，无细胞试验中IC50为14.3 nM，作用于ALK4比作用于ALK5效果低4倍，对ALK2，3，和 6没有活性。 |
LS 174T and SW480 cells were treated with SB525334 (1 umol/L) for 12 hours. HMGA2 expression was assessed by immunoblotting. Each experiment was repeated 3 times. Bars, SD; *, P < 0.05; **, P < 0.01.
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| S6713New |
ITD-1ITD-1是有效的TGF-β抑制剂。它不抑制TGFBR1或TGFBR的激酶活性，但能够有效地抑制TGFβ2诱导的效应因子SMAD2/3磷酸化，对Activin A的影响甚微。 |
||
| S8868New |
NG25NG25是一种新型的TAK1抑制剂，对TAK1和MAP4K2的IC50分别为149 nM和21.7 nM。 |
||
| S8772New |
LY 3200882LY 3200882是有效的、高选择性TGF-β receptor type 1 (TGFβRI)抑制剂，在体外肿瘤组织和免疫细胞以及体内皮下肿瘤中，有效地以浓度依赖方式抑制TGFβ介导的SMAD磷酸化。 |
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| S2186 |
SB505124SB505124是一种选择性TGFβR抑制剂，作用于ALK4和ALK5，无细胞试验中IC50分别为129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。 |
(D): Fluorescence micrographs of SOX2/FOXA2 double-staining of the conditions mentioned above. The TGF-b inhibitor SB-505124 (1 mM) was additionally used together with the complete medium. Nuclei were counterstained with DAPI. Original magnification 310 or 340. Abbreviations: DAPI, 40,6-diamidino-2-phenylindole; RA, retinoic acid.
|
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| S2907 |
PirfenidonePirfenidone抑制TGF-β产生和TGF-β刺激的胶原蛋白产生，且降低TNF-α和IL-1β产生，具有抗纤维化和抗炎特性。Phase 3。 |
Ex vivo tissue spotting experiment of pirfenidone dilutions and MalDI imagingn approach of in vivo administered pirfenidone measured with MalDI-TOF mass spectrometer. ex vivo dilution series of pirfenidone (m/z 186.2?.1 Da) covered with CHCa matrix. In vivo treated liver cryosections measured by MalDI-TOF imaging using CHCa. Size bar corresponds to 2 mm.
|
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| S2750 |
GW788388GW788388是一种有效的，选择性ALK5抑制剂，无细胞试验中IC50为18 nM，也抑制TGF-βII型受体和activin II型受体活性，但不抑制BMP II型受体。 |
Combination treatment with GW788388 and IL-23 aiming to sustain Th17 cell levels increases spleen cell production of the inflammatory mediators IL-17 and TNF-a, the stimulatory mediators IL-2, IFN-g and RANTES, and the inhibitory mediator IL-10. Starting from Week 6 of 4NQO administration, when premalignant oral lesions were detectable on the tongue, mice were initiated on treatment with diluent, GW788388, IL-23 or both GW788388 and IL-23. After 2 months of these treatments, spleens were collected and cultured on anti-CD3 for 3 days. Supernatants were collected and used for measurement of the inflammatory mediators IL-17, TNF-a and IL-6 (a); stimulatory mediators IL-2, IFN-g and RANTES (b); and inhibitory mediators, TGF-b, IL-4 and IL-10 (c). *=p<0.05, **=p<0.01, ***=p<0.001.
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| S2805 |
LY364947LY364947是一种有效的ATP竞争性TGFβR-I抑制剂，无细胞试验中IC50为59 nM，比作用于TGFβR-II选择性高7倍。 |
The cytoplasmic and nuclear proteins were separated and the protein expression levels were determined by performing western blotting. LY364947 (1 uM), which is a potent ATP-competitive inhibitor of TGF-βRI, was used as the positive control. GAPDH and PARP were used as cytosolic and nuclear markers, respectively. |
|
| S7223 |
RepSoxRepSox是一种有效的，选择性TGFβR-1/ALK5抑制剂，作用于ATP与ALK5结合以及ALK5自磷酸化，无细胞试验中IC50分别为23 nM和4 nM。 |
(C) Generation of pluripotent stem cell from Yamanaka factors-induced OG2-MEFs under treatment of diverse chemical compounds. Images of GFP+ colonies were taken on day 10 post-infection. VPA, 0.5 mmol/L. CHIR99021, 3 μmol/L. Repsox, 1 μmol/L. (D) Quantification of GFP+ colonies in (C). All figures are representative of three independent experiments (n = 3). All data are presented as mean ± SD. *P < 0.05, **P < 0.01 vs. DMSO
|
|
| S7507 |
LDN-193189 2HClLDN193189 HCl是LDN193189的盐酸盐，是一种选择性BMP信号抑制剂，它能抑制BMP type I receptors ALK2和ALK3的转录活性，在C2C12细胞中IC50分别为5 nM 和 30 nM, 并且对于BMP的选择性是对TGF-β选择性的200倍。 |
LDN induces signifiant cell death. OVCA429 cells were treated with vehicle (DMSO) or experimental drugs for 6 hr to capture different stages of cell death. OVCA429 cell viability was assessed in response to drug treatment for 6 hr by staining with AO (green) and EB (orange). For clarity the different fluorescent channels to detect AO, EB, and the over-lapping images are shown for 10 mM LDN treatment.
|
|
| S7359 |
K02288K02288是一种高度选择性I型BMP受体抑制剂，针对 ALK2， ALK1和ALK6的IC50分别为1.1，1.8，6.4 nM，显示对其他ALKS（3，4，5）和的ActRIIa 有轻微抑制作用。 |
A549 cells were transfected with miR-205 inhibitor (IHT-205, 100 nM). Forty hours after transfection, the cells were seeded on transwell plates and treated with or without inhibitor K02288 (10 nM), AG1478 (1 µM), SB431542 (10 µM) for 10 hours. Migrated cells were quantified. All data are shown as mean± SD. N =3. All experiments have been repeated at least 3times independently. |
|
| S7624 |
SD-208SD-208是一种选择性TGF-βRI (ALK5)抑制剂，with IC50为48 nM，选择性比TGF-βRII高100多倍。 |
||
| S7627 |
LDN-214117LDN-214117是一种有效的选择性 BMP I型受体激酶 ALK2 抑制剂，IC50为 24 nM。 |
||
| S7959 |
SIS3 HClSIS3是一种新型的特异性Smad3抑制剂，通过抑制Smad3的磷酸化抑制TGF-β和activin信号，而不影响MAPK/p38, ERK或PI3-kinase信号通路。 |
Cultured cardiac fibroblasts infected with vector lentiviruses or EphrinB2 overexpressing lentiviruses were stimulated with specific antagonist against Stat3 (Stattic, 2.5μM) and/or Smad3 (SIS3, 1μM), respectively. The expression level of α-SMA was quantified via western blotting. In vitro experiments repeat 3 times, *P<0.05, **P<0.01. |
|
| S7530 |
Vactosertib (TEW-7197, EW-7197)Vactosertib (TEW-7197) 是一种高效的，选择性的，口服生物有效的TGF-β receptor ALK4/ALK5抑制剂，IC50分别为13 nM 和 11 nM。Phase 1。 |
Representative immunofluorescent images of HuL6 cells treated with EW-7197, TGF-β1, both, or neither for 72 h. Scale bars, 20 μm.
|
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| S7146 |
DMH1DMH1是选择性BMP receptor抑制剂，抑制ALK2，IC50为107.9 nM,对AMPK, ALK5, KDR (VEGFR-2)和PDGFR没有抑制效果。 |
The combined treatment with miR-140-5p mimics and some common chemotherapeutics did not have any effect on the SK-MES1 cell line, whereas miR-140-5p and DMH1 and cisplatin decreased the proliferation of
the A549 cells. Data are presented as mean±SEM of three individual experiments undertaken in triplicate. t-Test was used to assess significance with *p<0.05.
|
|
| S7147 |
LDN-212854LDN-212854 是一种强效的选择性BMP receptor抑制剂， 其作用于ALK2的IC50为1.3 nM , 分别超过作用于ALK1, ALK3, ALK4, 和 ALK5的选择性约 2-, 66-, 1641-, 和 7135倍。 |
||
| S7148 |
ML347ML347 是一种选择性的BMP receptor抑制剂，其作用于ALK2的IC50为 32 nM ,选择性高于ALK3 300倍。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7658 |
KartogeninKartogenin是一种smad4/smad5通路激活剂，促进多功能间充质干细胞选择性分化为软骨细胞。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2308 |
HesperetinHesperetin是一种生物类黄酮，更具体而言，是一种二氢黄酮。 |
||
| S8318 |
AlantolactoneAlantolactone，一种天然的桉烷类倍半萜内酯，能诱导activin/SMAD3信号、干扰Cripto-1/activin受体ⅡA型受体的相互作用。 |
Colon cancer cell lines (A) SW620, (B) HCT116, and (C) HT29 were treated with different concentrations (60, 12, 2.4, 0.48, and 0.098 μM) of nifuroxazide (nifu), niclosamide (nicl), cryptotanshinone (cry), and a lantolactone (ala), respectively, for 72 h. Cell proliferation in each group was detected by MTT assay. (D) HCT116, SW620, and HT29 cell lines were suppressed with niclosamide treatment at different concentrations (20, 10, 5, 2.5, and 1.25 μM) for 72 h. Subsequently, cell proliferation in each group was detected by MTT assay. The data were obtained from 3 independent experiments.
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