Name: SB431542
Brand: Selleck Chemicals
SKU: S1067
Rating: 5 (811 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.99%

99.99

함께 자주 사용되는 제품 SB431542

LDN-193189

This compound and LDN-193189, along with other small molecules, reduce the expression of epithelial-mesenchymal cell transition (EMT) marker genes and effectively inhibit fibrosis of liver cells.

Y-27632 Dihydrochloride

This compound and Y-27632 2HCl combination reverse the mesenchymal actin cytoskeleton stress fibers induced by TGF-β1 in TGF-β1 knockout mice cells (mTEC-KO).

DMH1

This compound and DMH1 combined use regulates the two TGF-β signaling pathways independently in human-induced pluripotent stem cells (hiPSCs).

SU 5402

This compound and SU5402 block NODAL and FGF9 signalling that allows germ cells to differentiate in Emx2-knockdown testes in vitro.

CHIR-99021 (Laduviglusib)

It and Laduviglusib suppress the gene expressions of pluripotent-related transcription factors and epithelial‑mesenchymal transition (EMT)-related genes to various levels in HeLa cells.

관련 타겟	PKC ROCK Bcr-Abl
기타 TGF-beta/Smad 억제제	RepSox (E-616452) Vactosertib (TEW-7197) A-83-01 LDN-193189 Dihydrochloride Galunisertib (LY2157299) SRI-011381 (C381) LY2109761 SIS3 Hydrochloride SB-525334 LY364947

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
HEK293T	Function Assay	10 μM	22 h	DMSO	Inhibits TGBR2 signaling in human HEK293T cells assessed as Inhibition of SMAD activation with IC50 of 0.066μM	23130626
H1299	Migration Assay	1 μM	12-24 h	DMSO	Induces antimigratory activity against human H1299 cells assessed as Inhibition of cell migration with IC50 of 0.5μM	24417479
HaCaT	Function Assay	3.2-50 μM	15 min	DMSO	Inhibits TGFbeta receptor in human HaCaT cells assessed as Smad phosphorylation with IC50 of 0.172μM	20919678
HepG2	Function Assay		12 h	DMSO	Inhibits TGFR-1 in human HepG2 cells expressing PAI-luciferase with IC50 of 0.25μM	19914068
CHO-HIR	Function Assay	0.01-3 μM	2 h	DMSO	Inhibits TGFbeta-induced downstream transcriptional activation of ALK5 expressed in CHO-HIR cells assessed as intracellular translocation of EGFP-Smad2 with IC50 of 0.35μM	24055046
Sf9	Function Assay		2 h	DMSO	Inhibits human recombinant ALK5 phosphorylation expressed in Sf9 cells with IC50 of 1.542μM	17552507
C32	Function Assay	10 μM	20h		Inhibits Trypanosoma cruzi Y infection-induced TGFbeta signaling in mink C32 cells at 10 uM	17526757
Mouse embryo cardiomyocytes	Function Assay	10 μM	1 h		Inhibits invasion of Trypanosoma cruzi Y in mouse embryo cardiomyocytes assessed as pathogen infection at 10 uM	17526757
Mouse embryo cardiomyocytes	Function Assay	10 μM	1 h		Inhibits TGF-beta-1-induced Smad2 phosphorylation in mouse embryo cardiomyocytes at 10 uM	17526757
Mouse embryo cardiomyocytes	Function Assay	10 μM	1 h		Inhibits Trypanosoma cruzi Dm28C infection-induced Smad2 phosphorylation in mouse embryo cardiomyocytes at 10 uM	17526757
Trypanosoma cruzi trypomastigotes	Antimicrobial Assay	10 μM	4 h		Induces antitrypanosomal activity against Trypanosoma cruzi trypomastigotes assessed as effect on parasite morphology at 10 uM	17526757
Mouse cardiomyocytes	Antimicrobial Assay	10 μM	4 h		Induces antitrypanosomal activity against Trypanosoma cruzi Y in mouse cardiomyocytes assessed as reduction of intracellular amastigotes at 10 uM	17526757
Mouse cardiomyocytes	Antimicrobial Assay	10 μM	96 h		Induces antitrypanosomal activity against Trypanosoma cruzi Y in mouse cardiomyocytes assessed as Inhibition of trypomastigote release at 10 uM	17526757
HaCaT	Function Assay	0.05 μM	2 h	DMSO	Does not inhibit TGF-beta induced ALK5 activity in HaCaT cells assessed as p3TP-luciferase reporter activity at 0.05 uM	17552507
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	384.39	화학식	C₂₂H₁₆N₄O₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	301836-41-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	C1OC2=C(O1)C=C(C=C2)C3=C(NC(=N3)C4=CC=C(C=C4)C(=O)N)C5=CC=CC=N5

용해도 (Solubility)

In vitro
배치:

DMSO : 77 mg/mL (200.31 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 3 mg/mL

Water : Insoluble

DMSO : 13 mg/mL (33.81 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 3 mg/mL

Water : Insoluble

DMSO : 10 mg/mL (26.01 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (260.15 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 5 mg/mL

Water : Insoluble

DMSO : 77 mg/mL (200.31 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 9 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	0.1%DMSO 1 99.80% Saline Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.020mg/ml (0.05mM)	Taking the 1 mL working solution as an example, add 1 μL of 20 mg/ml clear DMSO stock solution to 998 μL of Saline and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.000mg/ml (10.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; then Continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 95% Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.000mg/ml (10.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC₅₀/Ki	ALK4 (Cell-free assay) ALK7 (Cell-free assay) ALK5 (Cell-free assay) 94 nM
시험관 내(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. 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. 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. 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. 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.
키나아제 분석	Flashplate assay for ALK5
키나아제 분석	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.
생체 내(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.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/11855979/ [2] https://pubmed.ncbi.nlm.nih.gov/12065756/ [3] https://pubmed.ncbi.nlm.nih.gov/12065755/ [4] https://pubmed.ncbi.nlm.nih.gov/14633705/ [5] https://pubmed.ncbi.nlm.nih.gov/15967103/ [6] https://pubmed.ncbi.nlm.nih.gov/21042762/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	phospho-SMAD3 / Phospho-p38 Y397 phospho-FAK pSmad2 / p-AKT / E-cadherin / vimentin / snail / slug CK18 / Fibronectin / Vimentin	17113264
Growth inhibition assay	Cell viability	28125630
Immunofluorescence	Smad2/3	19619490
Immunofluorescence	Na+/K+-ATPase	23451286
ELISA	collagen 1	23451286

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
I would appreciate it if you can help me in figuring out the formulation for it in vivo experiments.

답변:
S1067 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension for oral gavage. It can also be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5 mg/ml as a clear solution for IP injection.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

SB431542 TGF-beta/Smad inhibitor

화학 구조

분자량: 384.39

품질 관리 (Quality Control)

함께 자주 사용되는 제품 SB431542

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

자주 묻는 질문 (Frequently Asked Questions)

SB431542 TGF-beta/Smad inhibitor

화학 구조

분자량: 384.39

품질 관리 (Quality Control)

함께 자주 사용되는 제품 SB431542

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

자주 묻는 질문 (Frequently Asked Questions)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)