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.
Acta Histochem. 2022 Aug;124(6):151931.
Fibroblast-derived exosomal miRNA-133 promotes cardiomyocyte-like differentiation
SB431542 purchased from AbMole
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Source | Hum Reprod (2014). Figure 2. SB431542 |
| Method | HESC derivation | |
| Cell Lines | hESC lines | |
| Concentrations | 10 μM | |
| Incubation Time | 8 days | |
| Results | The number of GATA6-positive ICM cells did not differ between the SB, Activin A and control groups (8.8+4.3, 8.0+4.6 and 7.2+ 4.0, respectively) |
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Source | Hum Reprod (2014). Figure 1. SB431542 |
| Method | HESC colonies culture | |
| Cell Lines | hESC lines | |
| Concentrations | 10 μM | |
| Incubation Time | 8 days | |
| Results | HESC colonies cultured in the presence of SB did not proliferate well and showed early signs of differentiation at their periphery |
| Cell Experiment | |
|---|---|
| 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 | |
|---|---|
| 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 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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