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SB 431542 is a potent and selective inhibitor of the TGF-β1 receptor ALK5 with an IC50 of 94 nM, and its relatives ALK4 and ALK7. It does not affect the BMP receptors ALK2, ALK3, ALK6, or a panel of other kinases tested. SB 431542 specifically blocks Smad signaling, reducing gene expression relevant to fibrosis and cancer. Suppresses TGF-β-induced proliferation of human osteosarcoma cells.
Theriogenology. 2024 Mar 15;219:65-74.
Growth differentiation factor 9 regulates the expression of estrogen receptors via Smad2/3 signaling in goat cumulus cells
SB431542 purchased from AbMole
FEBS Open Bio. 2024 May 1.
Regulation of cardiac fibroblasts reprogramming into cardiomyocyte-like cells with a cocktail of small molecule compounds
SB431542 purchased from AbMole
Acta Histochem. 2022 Aug;124(6):151931.
Fibroblast-derived exosomal miRNA-133 promotes cardiomyocyte-like differentiation
SB431542 purchased from AbMole
Cell Experiment | |
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Cell lines | human DCs |
Preparation method | Effects of SB-431542 on murine BM-DCs and human DCs. DCs were incubated in 96-well plates (5x104 cells/200 μl/well) with SB-431542 or vehicle alone and LPS in the presence of LPS at different concentrations in triplicates, and then examined for expression of co-stimulatory molecules using FACSCalibur. After 24 h of incubation, the cells were examined for surface expression of CD86 or CD83 within the CD11c+ populations, and the supernatants were tested for cytokine production by enzyme-linked immunosorbent assay (ELISA). Following 24 h of incubation with a test drug, BM-DCs were incubated for 10 min with 5 mg/ml of fluorescein isothiocyanate (FITC)-conjugated dextran (DX) (70,000 Dalton molecular weight, Sigma) at 4˚C or 37˚C, washed extensively, and then examined for FITC signals by CD11c+ cells. After drug pretreatment, BM-DC preparations (derived from BALB/c mice) were washed 3 times and then co-cultured in 96 round-bottom well plates at 4 different cell densities (0.3-10x103 cells/well) with splenic T cells purified from C57BL/6 mice (5x104 cells/well). The magnitude of T cell proliferation was assessed by 3H-thymidine uptake on day 4. Human DC cultures derived from PBMCs were examined for surface phenotype within the CD11c+ population and cytokine production by ELISA as well as for allogeneic mixed lymphocyte reaction. |
Concentrations | 0~10 μM |
Incubation time | 24 hr |
Animal Experiment | |
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Animal models | BALB/c mice received intraperitoneal (i.p.) injections of colon-26 tumor cells |
Formulation | normal saline |
Dosages | 1 μM (100μL) |
Administration | directly injected into peritoneal cavity |
Molecular Weight | 384.39 |
Formula | C22H16N4O3 |
CAS Number | 301836-41-9 |
Solubility (25°C) | DMSO ≥ 50 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Related ALK Products |
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TL13-22
TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. |
TL13-110
TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. |
ALK inhibitor 2
ALK inhibitor 2 is a potent pyrimidin ALK inhibitor. |
NVL-655 TFA
NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
NVL-655
NVL-655 (ALK-IN-27) is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. NVL-655 (ALK-IN-27) can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
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