Name: NSC 74859 (S3I-201)
Brand: Selleck Chemicals
SKU: S1155
Rating: 5 (242 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.28%

99.28

관련 타겟	EGFR JAK Pim
기타 STAT 억제제	Napabucasin (BBI608) Stattic Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 HO-3867 Nifuroxazide Homoharringtonine (HHT)

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

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
U87	Growth Inhibition Assay		72 h		IC50=55.1 μM	20072652
U373	Growth Inhibition Assay		72 h		IC50=52.5 μM	20072652
HPAC	Growth Inhibition Assay		72 h		IC50＞100 μM	20072652
PANC-1	Growth Inhibition Assay		72 h		IC50＞100 μM	20072652
SK-BR-3	Growth Inhibition Assay		72 h		IC50＞100 μM	20072652
U-373 MG	Cytotoxicity Assay	3/10 μM	24 h		reduces FN-γ-induced cell neurotoxicity	20888416
MDA-MB-231	Growth Inhibition Assay		72 h		IC50＞100 μM	20072652
HUVEC	Function Assay	0.5-20 μM	24 h	DMSO	suppresses the hypoxia-induced accumulation of HIF-1α	21523559
Huh7	Growth Inhibition Assay	100 nM	48 h	DMSO	inhibits the IL-6 stimulation promoted cell proliferation	23364389
PLC/PRF/5	Growth Inhibition Assay	100 nM	48 h	DMSO	inhibits the IL-6 stimulation promoted cell proliferation	23364389
H460	Function Assay	50/100 μM	48 h		inhibits the Stat3C increased miR-92a expression	23820254
H1299	Function Assay	50/100 μM	48 h		suppresses miR-92a expression dose-dependently	23820254
T-cell	Growth Inhibition Assay				IC50=50 μM	24068731
U373	Growth Inhibition Assay	125 μM	24 h	DMSO	disrupts STAT3 signaling and proliferation	24070820
HUT-102	Apoptosis Assay	75-300 μM	24/48 h		suppresses cell proliferation in a dose-dependent manner and induces cell apoptosis	24090995
MT-2	Apoptosis Assay	75-300 μM	24/48 h		suppresses cell proliferation in a dose-dependent manner and induces cell apoptosis	24090995
H460	Apoptosis Assay	100 nM	24 h		enhances cell death co-treated with LY294002	24472538
A459	Apoptosis Assay	100 nM	24 h		induces cell apoptosis co-treated with BEZ235	24472538
H460	Apoptosis Assay	100 nM	24 h		induces cell apoptosis co-treated with BEZ235	24472538
GC	Growth Inhibition Assay	50-125 μM	72 h		attenuates the cell growth in a dose-dependent manner	25774503
GH3	Growth Inhibition Assay	50-125 μM	72 h		attenuates the cell growth in a dose-dependent manner	25774503
BT474R	Function Assay	50 μM	10-60 d		inhibits STAT3 activity	25327561
NCI-N87R	Function Assay	50 μM	10-60 d		inhibits STAT3 activity	25327561
MDA-MB-468	Function assay	100 uM	24 hrs		Inhibition of Stat3 activation in human MDA-MB-468 cells at 100 uM after 24 hrs	17463090
MDA-MB-435	Function assay	100 uM	24 hrs		Inhibition of Stat3 activation in human MDA-MB-435 cells at 100 uM after 24 hrs	17463090
MDA-MB-231	Function assay	100 uM	24 hrs		Inhibition of Stat3 activation in human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
NIH3T3	Function assay	100 uM	24 hrs		Reduction of pTyr-705 Stat3 level in v-Src expressing mouse NIH3T3 cells at 100 uM after 24 hrs	17463090
NIH3T3	Growth inhibition assay	100 uM	4 days		Growth inhibition of mouse NIH3T3 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-435	Growth inhibition assay	100 uM	4 days		Growth inhibition of human MDA-MB-435 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-231	Growth inhibition assay	100 uM	4 days		Growth inhibition of human MDA-MB-231 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
MDA-MB-468	Growth inhibition assay	100 uM	4 days		Growth inhibition of human MDA-MB-468 cells expressing v-Src at 100 uM after 4 days by trypan blue exclusion assay	17463090
NIH3T3	Growth inhibition assay	100 uM			Growth inhibition of mouse NIH3T3 cells expressing v-Ras at 100 uM for every 3 days by soft-agar colony-formation assay	17463090
MDA-MB-435	Apoptosis assay	30 to 100 uM	48 hrs		Induction of apoptosis in human MDA-MB-435 cells expressing active Stat3 at 30 to 100 uM after 48 hrs	17463090
MDA-MB-231	Apoptosis assay	100 uM	24 hrs		Reduction of apoptosis in Stat3 transfected human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
MDA-MB-231	Function assay	100 uM	48 hrs		Reduction of cyclin D1 gene expression in human MDA-MB-231 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Apoptosis assay	100 uM	24 hrs		Induction of apoptosis in Stat3 SH2 domain transfected human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
MDA-MB-231	Apoptosis assay	100 uM	24 hrs		Induction of apoptosis in Stat3C transfected human MDA-MB-231 cells at 100 uM after 24 hrs	17463090
NIH3T3	Function assay	100 uM	48 hrs		Reduction of cyclin D1 gene expression in v-Src transfected mouse NIH3T3 cells at 100 uM after 48 hrs	17463090
NIH3T3	Function assay	100 uM	48 hrs		Reduction of Bcl-xL gene expression in v-Src transfected mouse NIH3T3 cells at 100 uM after 48 hrs	17463090
NIH3T3	Function assay	100 uM	48 hrs		Reduction of survivin gene expression in v-Src transfected mouse NIH3T3 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Function assay	100 uM	48 hrs		Reduction of Bcl-xL gene expression in human MDA-MB-231 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Function assay	100 uM	48 hrs		Reduction of survivin gene expression in human MDA-MB-231 cells at 100 uM after 48 hrs	17463090
MDA-MB-231	Antitumor assay	5 mg/kg	2 weeks		Antitumor activity against human MDA-MB-231 cells expressing active Stat3 xenografted in mouse at 5 mg/kg, iv for every 3 days for 2 weeks	17463090
NIH3T3	Growth inhibition assay	100 uM			Growth inhibition of mouse NIH3T3 cells expressing v-Src at 100 uM for every 3 days by soft-agar colony-formation assay	17463090
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량	365.36	화학식	C₁₆H₁₅NO₇S	보관 (수령일로부터)	3년-20°C분말
CAS 번호	501919-59-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관

용해도 (Solubility)

In vitro
배치:

DMSO : 73 mg/mL (199.8 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 73 mg/mL (199.8 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 73 mg/mL (199.8 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 3 mg/mL

Water : Insoluble

DMSO : 73 mg/mL (199.8 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : 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.
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.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	3.000mg/ml (8.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	2% DMSO 1 40% PEG 300 2 5%Tween80 3 53%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.460mg/ml (4.00mM)	Taking the 1 mL working solution as an example, add 20 μL of 73 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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)

특징	A chemical probe inhibitor of Stat3 activity.
Targets/IC₅₀/Ki	STAT3 (Cell-free assay) 86 μM
시험관 내(In vitro)	NSC 74859 (S3I-201) inhibits growth and induces apoptosis preferentially in tumor cells that contain persistently activated Stat3 by inhibiting Stat3·Stat3 complex formation and Stat3 DNA-binding and transcriptional activities. Moreover, it also inhibits the expression of the Stat3-regulated genes encoding cyclin D1, Bcl-xL, and survivin.This compound inhibits breast carcinoma MDA-MB-435, MDA-MB-453 and MDA-MB-231 cell lines with IC50 of 100 μM. In addition, the cells with impaired TGF-β signaling are four times as sensitive to S3I-201.A recent study shows that it potentiates the antiproliferative effect in HepG2 and Huh-7 cells via the STAT3 signalling pathway.
키나아제 분석	시험관 내 STAT3 DNA 결합 분석 및 EMSA 분석
키나아제 분석	간략히, 100 µL의 biotinyl-e-Ac-EPQpYEEIEL-OH (50 mM Tris/150 mM NaCl, pH 7.5에 용해)를 스트렙타비딘 코팅된 96웰 마이크로타이터 플레이트의 각 웰에 추가하고 4 °C에서 밤새 흔들면서 배양합니다. 그런 다음 플레이트를 PBS/Tween 20으로 헹구고 이어서 200 µL의 BSA-T-PBS (0.2% BSA/0.1% Tween 20/PBS)로 두 번 헹굽니다. 이어서 50 µL의 Lck-SH2-GST 융합 단백질 (BSA-T-PBS에 6.4 ng/ml)을 96웰 플레이트의 각 웰에 50 µL의 NSC 74859 (S3I-201) (최종 농도 30 mM 및 100 mM) 존재 및 부재하에 추가하고, 플레이트를 실온에서 4시간 동안 흔들어줍니다. 용액을 제거한 후, 각 웰을 BSA-T-PBS (200 µL)로 4회 헹구고, 100 µL의 폴리클로날 토끼 항-GST 항체 (BSA-T-PBS에 100 ng/mL)를 각 웰에 추가하고 4 °C에서 밤새 배양합니다. BSA-T-PBS로 세척한 후, 100 µL의 200 ng/mL BSA-T-PBS 호스래디시 과산화효소-접합 마우스 항-토끼 항체를 각 웰에 추가하고 실온에서 45분 동안 배양합니다. BSA-T-PBS로 4회 세척 단계와 PBS-T로 3회 세척 단계를 거친 후, 100 µL의 과산화효소 기질을 각 웰에 추가하고 5-15분 동안 배양합니다. 과산화효소 반응은 100 µL의 1 M 황산 용액을 추가하여 중지하고, ELISA 플레이트 리더로 450 nm에서 흡광도를 측정합니다.
생체 내(In vivo)	NSC 74859 (S3I-201) (5 mg/kg, i.v. every 2 or every 3 days) shows the antitumor efficacy in mouse models with human breast tumor xenografts that harbor constitutively active Stat3.This compound treatment reduces Varicella-zoster virus (VZV) replication on the basis of the bioluminescence signal and the number of positive skin xenografts compared with DMSO-treated mice by inhibiting STAT3 phosphorylation.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/17463090/ [2] https://pubmed.ncbi.nlm.nih.gov/19137011/ [3] https://pubmed.ncbi.nlm.nih.gov/22098470/ [4] https://pubmed.ncbi.nlm.nih.gov/22190485/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	STAT3 / p-STAT3 / Cyclin D1 / Bcl-2 / Nanog / OCT4 / ALDH1 / CD44 PD-L1	26556875
Immunofluorescence	p-STAT3 Oct4 / Twist	26556875
Growth inhibition assay	Cell viability	26813676

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):

NSC 74859 (S3I-201) STAT3 억제제

분자량: 365.36

품질 관리 (Quality Control)

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)

NSC 74859 (S3I-201) STAT3 억제제

분자량: 365.36

품질 관리 (Quality Control)

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)

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