Home Stem Cells & Wnt PARP inhibitor XAV-939

연구용

XAV-939 WNT Pathway Inhibitor

제품 번호S1180

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.
XAV-939 PARP inhibitor Chemical Structure

화학 구조

분자량: 312.31

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품질 관리 (Quality Control)

배치: 순도: 99.95%
99.95

함께 자주 사용되는 제품 XAV-939

SU 5402

It promotes anterior central nervous system identity, while SU5402 accelerates hPSC differentiation toward neuroectodermal lineages.

LDN-193189

It and LDN-193189 are the least effective in improving the morphology of low-density P0 RPE cultures to varying extents.

SB431542

It and SB431542 significantly suppress MSC gene expression.

ICG-001

It and ICG-001 decrease the proliferation of the IGROV1 and SKOV3 ovarian cancer cell lines.

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
Sf-21 Kinase Assay 18.75 μM 60 min DMSO Inhibition of N-terminal GST-tagged TNKS2 expressed with IC50 of 0.0053 μM 23879431
HEK293T Function Assay DMSO Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM 23879431
HEK293T Function Assay 10 μM DMSO Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM 22191557
HEK293T Function Assay 24 h DMSO Inhibition of mouse Wnt3A signaling with IC50 of 0.078 μM 22260203
SW480 Function Assay 10 μM 24 h DMSO Stabilization of Axin2 with EC50 of 0.371 μM 22260203
HEK293T Function Assay 50 μM DMSO Has no Effect on forskolin-induced cAMP signaling in human HEK293T cells coexpressing CRE 22260203
IEC-6 Function Assay 6 h Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced axin2 expression with IC50 of 0.64 μM 24060489
IEC-6 Function Assay 6 h Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced lgr5 expression with IC50 of 2.9 μM 24060489
DLD1 Function Assay 20 μM 24 h DMSO Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity 24527792
DLD1 Cytotoxic Assay 20 μM 10 d DMSO Cytotoxicity assessed as growth inhibition 24527792
VERO Function Assay 25 μM DMSO Disturbes PAR belt synthesis, affecting the actin cytoskeleton, cell shape and cell adhesion 25332845
HeLa Function Assay 10 μM 48 h Reduction of cytoplasmic distribution and nuclear translocation of β-catenin 25061499
SiHa Function Assay 10 μM 48 h Reduction of cytoplasmic distribution and nuclear translocation of β-catenin 25061499
HEK293 Function assay Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50 = 0.078 μM. 23844574
DLD1 Function assay 24 hrs Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay, IC50 = 0.707 μM. 25299683
Sf21 Function assay 2 hrs Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins, IC50 = 0.017 μM. 27163581
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
A549 Growth inhibition assay 72 hrs Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 12.3 μM. 29934219
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 312.31 화학식

C14H11F3N2OS

 보관 (수령일로부터)
CAS 번호 284028-89-3 SDF 다운로드 원액 보관

동의어 NVP-XAV939 Smiles C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F

용해도 (Solubility)

In vitro
배치:

DMSO : 12 mg/mL (38.42 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:

생체 내 제형 계산기 (투명한 용액)

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

mg/kg g μL

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
TNKS2
(Cell-free assay)
4 nM
TNKS1
(Cell-free assay)
11 nM
시험관 내(In vitro)

XAV-939 specifically inhibits tankyrase PARP activity. This compound dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM exposure. Treatment of human lymphoblasts with 1.0 μM this chemical results in marked elevation of tankyrase 1 levels.

This agent is axin stabilizing agent. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. This compound stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. This chemical deregulates the Wnt/b-catenin pathway which has been implicated in many cancers.

생체 내(In vivo)

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.
참조

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot β-catenin / E-cadherin / N-cadherin β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin
S1180-WB1
31060551
Immunofluorescence β-catenin / E-cadherin Actin / PAR Hes1 / β-catenin / p-STAT3
S1180-IF1
31060551

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
I want to inject it (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this compound.

답변:
S1180 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve it in DMSO clearly first. You can sonicate and warm this compound in water bath at about 45 degree to help dissolving. Then dilute with corn oil.