SB431542

製品コードS1067 バッチS106708

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₁₆N₄O₃
	分子量	384.39	CAS No.	301836-41-9
Solubility (25°C)*	体外	DMSO	77 mg/mL (200.31 mM)
		Ethanol	5 mg/mL (13.0 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	SB431542 は強力かつ選択的 ALK5 阻害剤であり、cell-free assay における IC50 は 94 nM です。p38 MAPK などのキナーゼよりも ALK5 に対して 100 倍の選択性を有しています。
in vitro	SB 431542 inhibits the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are responsible for the phosphorylation of Smad2. SB 431542 has little effect on ALK1, ALK2, ALK3, and ALK6, which show phosphorylation of Smad1. SB 431542 is a selective inhibitor of endogenous activin but has no apparent effect on BMP signaling. SB 431542 could induce both Smad2/Smad4- and Smad3/Smad4-dependent transcription. ^[2] In A498 cells, SB 431542 inhibits both TGF-β1-induced collagen Iα1 and PAI-1 mRNA with IC50 of 60 nM and 50 nM, respectively. In addition, SB 431542 inhibits production of TGF-β1-induced fibronectin mRNA and protein with IC50 of 62 nM and 22 nM, respectively. ^[3] SB 431542 blocks the TGF-β-mediated growth factors, including PDGF-A, FGF-2 and HB-EGF, leading to an increase in proliferation of MG63 cells. SB 431542 also inhibits TGF-β-induced c-Myc and p21 ^WAF1/CIP1. ^[4] SB 431542 significantly suppresses TGF-β-induced G1 arrest, leading to accumulation of cells in the S phase of the cell cycle in FET, RIE, and Mv1Lu cells. SB 431542 also inhibits TGF-β-induced epithelial to mesenchymal transition (EMT) in NMuMG and PANC-1 cells. ^[5] SB 431542 significantly elevates the expression of CD86 in BM-DCs and that of CD83 within CD11c+ cells suppressed by TGF-β. SB 431542 is able to induce NK activity through functional maturation and IL-12 production of human DCs. ^[6]
in vivo	SB 431542 triggers cytotoxic T lymphocyte (CTL) activities in the colon-26 carcinoma models and is most likely to produce antitumor immunological outcomes through alteration of DC function suppressed by TGF-β. ^[6]

プロトコル(参考用のみ)

キナーゼアッセイ	Flashplate assay for ALK5
キナーゼアッセイ	SB 431542 is dissolved in DMSO at a concentration of 10 mM. The kinase domain of TGFβRI, from amino acid 200 to the C-terminus, and the full-length Smad3 protein are expressed as N-terminal glutathion S-transferase (GST) fusion proteins in the baculovirus expression system. Proteins are purified with glutathion Sepharose beads 4B. Basic FlashPlates are coated with 0.1 M sterile filtered sodium bicarbonate, pH 7.6, containing 700 ng of GST-Smad3 per 100 μL. Assay buffer contains 50 mM HEPES (pH 7.4), 5 mM MgCl₂, 1 mM CaCl₂, 1 mM DTT, 100 mM GTP, 3 μM ATP plus 0.5 μCi/well ɤ³³P-ATP, and 85 ng of GST-ALK5 with or without SB 431542. Plates are incubated at 30 °C for 3 hours. The assay buffer is removed by aspiration, and the plate is counted on a Packard TopCount 96-well scintillation plate reader.
細胞アッセイ	細胞株	MG63 and NIH3T3
	濃度	0.3 μM
	反応時間	30 minutes
	実験の流れ	To explore the effects of ligands, MG63 and NIH3T3 cells are seeded at a density of 8 × 10⁴ cells/well in 6-well plates and starved (0.1% FCS for MG63 cells and 0.5% FCS for NIH3T3 cells) for 24 hours before ligand stimulation. Media containing various ligands are exchanged at 48-hours intervals. Cells are trypsinized and counted by a Coulter counter on days 2, 4, and 6 after ligand stimulation. To explore the effects of constitutively active receptors, cells are seeded at a density of 2 × 10⁵ cells/well in 6-well plates. The next day, cells are infected with adenoviruses carrying various cDNAs at a multiplicity of infection of 100. Cells are trypsinized and counted on day 3. Cell proliferation assay is performed in the presence of 0.3 μM SB 431542.
動物実験	動物モデル	BALB/c mice receive intraperitoneal (i.p.) injections of colon-26 tumor cells.
	投薬量	1 μM solution, 100 μL/mouse
	投与方法	Directly injected into peritoneal cavity

参考

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カスタマーフィードバック

: Data from [Acta Biomater, 2014, 10(7):3108-16]

: Data from [Development, 2013, 140, 660-666]

: Data from [Stem Cells Dev, 2013]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

WNT signalling control by KDM5C during development affects cognition [ Nature, 2024, 10.1038/s41586-024-07067-y]	PubMed: 38383780
Generation of complex bone marrow organoids from human induced pluripotent stem cells [ Nat Methods, 2024, 10.1038/s41592-024-02172-2]	PubMed: 38374263
In vitro induction of patterned branchial arch-like aggregate from human pluripotent stem cells [ Nat Commun, 2024, 15(1):1351]	PubMed: 38355589
Self-renewing human naïve pluripotent stem cells dedifferentiate in 3D culture and form blastoids spontaneously [ Nat Commun, 2024, 15(1):668]	PubMed: 38253551
VGLL1 cooperates with TEAD4 to control human trophectoderm lineage specification [ Nat Commun, 2024, 15(1):583]	PubMed: 38233381
Cryptosporidium infection of human small intestinal epithelial cells induces type III interferon and impairs infectivity of Rotavirus [ Gut Microbes, 2024, 16(1):2297897]	PubMed: 38189373
Neural and metabolic dysregulation in PMM2-deficient human in vitro neural models [ Cell Rep, 2024, 43(3):113883]	PubMed: 38430517
FOXA2-initiated transcriptional activation of INHBA induced by methylmalonic acid promotes pancreatic neuroendocrine neoplasm progression [ Cell Mol Life Sci, 2024, 81(1):50]	PubMed: 38252148
iMSC-mediated delivery of ACVR2B-Fc fusion protein reduces heterotopic ossification in a mouse model of fibrodysplasia ossificans progressiva [ Stem Cell Res Ther, 2024, 15(1):83]	PubMed: 38500216
The MORC2 p.S87L mutation reduces proliferation of pluripotent stem cells derived from a patient with the spinal muscular atrophy-like phenotype by inhibiting proliferation-related signaling pathways [ Neural Regen Res, 2024, 19(1):205-211]	PubMed: 37488868

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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