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Stem Cells / Wnt

Stem Cells / Wnt

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U18666A

Catalog No. A20195
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cholesterol synthesis/Hedgehog inhibitor

U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor. 了解更多

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Mebendazole

Catalog No. A16606
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Hedgehog inhibitor

Mebendazole is a highly effective, broad-spectrum antihelmintic indicated for the treatment of nematode infestations; has been found as a hedgehog inhibitor. 了解更多

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Cyclopamine

Catalog No. A10249
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Hedgehog signaling 抑制剂

Cyclopamine是一种特异性的Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，IC50为46 nM。Cyclopamine 抑制Hedgehog信号通路， IC50 为46 nM。了解更多

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TAK-441

Catalog No. A11351
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Hedgehog 抑制剂

TAK-441是吡咯并[3，2-c]吡啶衍生物，作为高效口服活性hedgehog信号抑制剂。了解更多

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SANT-1

Catalog No. A13095
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Sonic hedgehog 抑制剂

SANT-1是有效的细胞渗透性Sonic刺猬（Shh）信号传导抑制剂；平滑活性的高亲和力拮抗剂（KD = 1.2 nM）。以20 nM的IC50抑制平滑的激动剂作用（在Shh-LIGHT2细胞中）。了解更多

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Hh-Ag1.5

Catalog No. A12920
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Hedgehog 抑制剂

Hh-Ag1.5是Hedgehog途径中最有效，选择性最强的小分子激动剂之一，靶向EC50?1 nM的平滑（Smo）。了解更多

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JK 184

Catalog No. A12925
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Hedgehog 抑制剂

JK 184是有效的下游hedgehog (Hh)信号抑制剂，可防止Gli依赖性转录活性(IC50 = 30 nM)。了解更多

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MK-4101

Catalog No. A16111
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Hedgehog 抑制剂

MK-4101是Hedgehog通路的有效和选择性抑制剂。了解更多

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RU-SKI 43

Catalog No. A16229
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Hhat 抑制剂

RU-SKI 43是Hhat（刺猬酰基转移酶）的小分子抑制剂，该酶负责将棕榈酸酯附着到Shh上。了解更多

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HPI-4

Catalog No. A16349
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hedgehog 抑制剂

HPI-4是一种刺猬（Hh）信号通路抑制剂，中位抑制浓度（IC50）小于10μM。了解更多

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IWP-3

Catalog No. A13192
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Wnt 抑制剂

IWP-3是Wnt产生的抑制剂。在体外阻断Wnt途径的活性（IC 50 = 40 nM）。IWP-3使豪猪（Porcn）失活，豪猪（Porcn）是一种膜结合的O-酰基转移酶，负责棕榈酸化Wnt蛋白，这对于其信号传导能力和分泌至关重要。通过阻断Wnt信号传导，IWP-3已被用于促进人类胚胎干细胞（EC??= 1.2μM）产生心肌细胞。了解更多

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ETC-159

Catalog No. A15840
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Wnt 抑制剂

ETC-159是Wnt分泌的有效和特异性抑制剂。ETC-159以剂量依赖性方式抑制β-catenin报告基因的活性，IC50为2.9 nM。了解更多

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IQ-1

Catalog No. A16064
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Wnt/beta-catenin 抑制剂

IQ-1是可透过细胞的四氢异喹啉亚基化合物，可调节Wnt/β-catenin信号传导。了解更多

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CCT251545

Catalog No. A16216
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Wnt 抑制剂

CCT251545是口服有效的WNT信号抑制剂，IC50值为5 nM。了解更多

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Hexachlorophene

Catalog No. A16217
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Wnt/beta-catenin 抑制剂

Hexachlorophene是一种有效的KCNQ1/KCNE1钾通道激活剂，EC50为4.61±1.29 uM。也是Wnt/β-catenin信号的抑制剂。了解更多

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JW74

Catalog No. A16219
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Wnt 抑制剂

JW74是典型的Wnt信号传导的有效和特异性抑制剂。JW74显示ST-Luc分析中规范Wnt信号的减少，IC50值为790 nM。了解更多

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- Yang JM, .et al. LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway, Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
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ICG-001

Catalog No. A11039
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Wnt/beta-catenin 抑制剂

ICG-001是Wnt/β-catenin信号传导途径的特异性抑制剂，可抑制β-catenin/环状AMP响应元件结合（CREB）蛋白的转录（IC50 = 3 uM）。了解更多

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- Seonmin Choi, .et al. Indocyanine Green-Loaded PLGA Nanoparticles Conjugated with Hyaluronic Acid Improve Target Specificity in Cervical Cancer Tumors, Yonsei Med J, 2021, Nov;62(11):1042-1051 PMID: 34672138
- Jasper C.Munro, .et al. Cardiac function and feed efficiency: increased right-heart workload in feed inefficient beef cattle, Livest Sci, 2019, 229 (2019) 159-169
- Kim JH, .et al. Small Heterodimer Partner Controls the Virus-Mediated Antiviral Immune Response by Targeting CREB-Binding Protein in the Nucleus, Cell Rep, 2019, May 14;27(7):2105-2118.e5 PMID: 31091449
- Yamaoka R, .et al. CD90 expression in human intrahepatic cholangiocarcinoma is associated with lymph node metastasis and poor prognosis, J Surg Oncol, 2018, Sep;118(4):664-674 PMID: 30196535
- Aida Y, .et al. Wnt3a promotes differentiation of human bone marrow-derived mesenchymal stem cells into cementoblast-like cells, In Vitro Cell Dev Biol Anim, 2018, Jun;54(6):468-476 PMID: 29785536
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XAV 939

Catalog No. A10994
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PARP 抑制剂

XAV 939是TNKS抑制剂（TNKS1和TNKS2的IC50值分别为0.011和0.004μM）。了解更多

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- Shizu Aikawa, .et al. Autotaxin-lysophosphatidic acid-LPA 3 signaling at the embryo-epithelial boundary controls decidualization pathways, EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- Mikaël M. Martino, .et al. Inhibition of IL-1R1/MyD88 signalling promotes mesenchymal stem cell-driven tissue regeneration, Nat Commun, 2016, 7: 11051 PMID: 27001940
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KY02111

Catalog No. A12362
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Wnt 抑制剂

KY02111是一种有效的选择性wnt信号通路抑制剂，通过基于细胞的筛选发现，当用于分化的第二阶段时，它促进hesc/ipscs向心肌细胞的分化。是一种有效的选择性wnt信号通路抑制剂，通过基于细胞的筛选发现，当用于分化的第二阶段时，它促进hesc/ipscs向心肌细胞的分化。了解更多

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LGK-974

Catalog No. A12816
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PORCN 抑制剂

LGK974是高效，选择性和口服生物利用性的豪猪抑制剂（Wnt信号拮抗剂），在Wnt信号报告基因测定和豪猪结合测定中IC50 <1 nM。了解更多

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- A-Ri Cho, .et al. RNF43 R117fs mutant positively regulates Wnt/β-catenin signaling by failing to internalize FZD expressed on the cell surface, Sci Rep, 2022, Apr 29;12(1):7013 PMID: 35487932
- Yang JM, .et al. LGK974, a PORCUPINE inhibitor, mitigates cytotoxicity in an in vitro model of Parkinson's disease by interfering with the WNT/β-CATENIN pathway, Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
- E Lemieux, .et al. Oncogenic KRAS signalling promotes the Wnt/β-catenin pathway through LRP6 in colorectal cancer, Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
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IWR-1-endo

Catalog No. A12737
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Wnt 抑制剂

IWR-1-endo是Wnt应答的有效抑制剂，可阻断基于细胞的Wnt /β-catenin途径报道分子应答，IC50值为180 nM。 Wnt蛋白与细胞表面的受体结合，启动信号级联反应，从而导致β-catenin激活基因转录。了解更多

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- Charles A.Herring, .et al. Human prefrontal cortex gene regulatory dynamics from gestation to adulthood at single-cell resolution, Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
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IWP-2

Catalog No. A12707
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Wnt 抑制剂

IWP-2是Porcn功能的灭活剂和Wnt生成的抑制剂，无细胞试验中IC50为27 nM,并阻止β-catenin的积累。Wnt/b-catenin途径维持使干细胞保持多能性的转录程序。了解更多

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Wnt-C59

Catalog No. A12951
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PORCN/Wnt 抑制剂

Wnt-C59是一种非常有效且高度选择性的Wnt信号拮抗剂，在Wnt信号报告基因分析中的IC50?74 pM。了解更多

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- Laksitorini MD, .et al. Modulation of Wnt/β-catenin signaling promotes blood-brain barrier phenotype in cultured brain endothelial cells, Sci Rep, 2019, Dec 23;9(1):19718 PMID: 31873116
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IWP-L6

Catalog No. A13978
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PORCN 抑制剂

IWP-L6是豪猪(Porcn) (一种膜结合的O-酰基转移酶（MBOAT)，EC50 = 0.5 nM) 的有效抑制剂。了解更多

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KYA1797K

Catalog No. A16353
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Wnt/beta-catenin 抑制剂

KYA1797K是一种高效且选择性的Wnt/β-catenin抑制剂，IC50为0.75 μM（TOPflash分析）。了解更多

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LF3

Catalog No. A16851
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Wnt 抑制剂

LF3通过破坏β-catenin和TCF4之间的相互作用（IC50小于2 uM）是典型Wnt信号传导的特异性抑制剂。了解更多

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IWP-4

Catalog No. A17004
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Wnt/β-catenin signaling 抑制剂

IWP-4是Wnt /β-catenin信号传导的新型有效抑制剂。了解更多

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pyrvinium

Catalog No. A17784
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Wnt 抑制剂

Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling. 了解更多

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Longdaysin

Catalog No. A21022
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Wnt/??-catenin signaling inhibitor

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. 了解更多

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FH535

Catalog No. A13795
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β-Catenin/Tcf 抑制剂

FH535是Wnt/β-catenin和PPAR的抑制剂，具有抗肿瘤活性。了解更多

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- Dongdong Fang, etc. Epithelial-Mesenchymal Transition of Ovarian Cancer Cells Is Sustained by Rac1 through Simultaneous Activation of MEK1/2 and Src Signaling Pathways. Oncogene. 2017 Mar; 36(11): 1546–1558.
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WAY-316606

Catalog No. A13986
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sFRP-1 抑制剂

WAY-316606是分泌蛋白sFRP-1的小分子抑制剂，sFRP-1是分泌糖蛋白Wnt的内源性拮抗剂。了解更多

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BC2059

Catalog No. A14381
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beta-catenin inhibitor

BC2059 is an orally bioavailable and potent beta-catenin inhibitor. 了解更多

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- Ji-Hye Jung, .et al. CXCR2 Inhibition in Human Pluripotent Stem Cells Induces Predominant Differentiation to Mesoderm and Endoderm Through Repression of mTOR, β-Catenin, and hTERT Activities, Stem Cells Dev, 2016, Jul 1; 25(13): 1006-1019 PMID: 27188501
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iCRT 14

Catalog No. A16218
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CRT 抑制剂

iCRT 14是一种新型的有效的β-catenin反应转录（CRT）抑制剂（在Wnt途径活性测定中IC50 = 40.3 nM）。了解更多

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CX-4945 (Silmitasertib)

Catalog No. A11060
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CK2 抑制剂

CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，可抑制人脐静脉内皮细胞迁移，管形成，并阻止癌细胞中CK2依赖性缺氧诱导的因子1α（HIF-1α）转录。了解更多

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- Xixi Zhao, .et al. Phosphorylation and Stabilization of PD-L1 by CK2 Suppresses Dendritic Cell Function, Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. CX-4945 and siRNA-Mediated Knockdown of CK2 Improves Cisplatin Response in HPV(+) and HPV(-) HNSCC Cell Lines, Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. PRMT6 methylation of RCC1 regulates mitosis, tumorigenicity, and radiation response of glioblastoma stem cells, Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. Protein kinase CK2 impact on intracellular calcium homeostasis in prostate cancer, Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. Protein kinase CK2 is involved in zinc homeostasis in breast and prostate cancer cells, Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. Human Rad17?C-terminal tail is phosphorylated by concerted action of CK1δ/ε and CK2 to promote interaction with the 9-1-1 complex, Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. Casein kinase 2 promotes interaction between Rad17 and the 9-1-1 complex through constitutive phosphorylation of the C-terminal tail of human Rad17, Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. Casein kinase 2 controls the survival of normal thymic and leukemic γδ T cells via promotion of AKT signaling, Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. mTORC1 and CK2 coordinate ternary and eIF4F complex assembly, Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. Protein Kinase CK2 Regulates Leukocyte-Endothelial Cell Interactions during Ischemia and Reperfusion in Striated Skin Muscle, Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. Role of protein kinase CK2 in the dynamic interaction of platelets, leukocytes and endothelial cells during thrombus formation., Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. Inhibition of protein kinase CK2 suppresses tumor necrosis factor (TNF)-α-induced leukocyte-endothelial cell interaction., Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. Adult B-cell acute lymphoblastic leukemia cells display decreased PTEN activity and constitutive hyperactivation of PI3K/Akt pathway despite high PTEN protein levels, Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
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LH 846

Catalog No. A13574
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CK1 抑制剂

LH 846是酪蛋白激酶（CK）1δ的选择性抑制剂（CK1δ，ε和α的IC50值为290 nM，1.3μM和2.5μM）。了解更多

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D4476

Catalog No. A13949
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CK1 抑制剂

D4476是酪蛋白激酶1的细胞渗透抑制剂。了解更多

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TTP-22

Catalog No. A14101
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CK2 抑制剂

TTP 22是一种高亲和力的酪蛋白激酶2（CK2）抑制剂（IC50 = 0.1uM，Ki = 40nM）。另外，TTP 22显示出对CK2的选择性超过JNK3，ROCK1和MET（显示出的抑制作用大于10 uM）。TTP 22是高度保守的丝氨酸/苏氨酸蛋白激酶，也参与细胞增殖，细胞分化和凋亡。了解更多

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DMAT

Catalog No. A15069
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CK2 抑制剂

DMAT是一种有效的特异性CK2抑制剂，IC50为0.13 uM。了解更多

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TBB

Catalog No. A15257
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CK2 抑制剂

TBB是酪蛋白激酶2（CK2）的高选择性，ATP/GTP竞争性抑制剂，对大鼠肝脏和人重组CK2的IC50分别为0.9和1.6 uM。了解更多

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IC 261

Catalog No. A15764
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CK1δ and CK1ε 抑制剂

IC 261是CK1δ和CK1ε抑制剂。IC261对CK1的IC50为16 μM，对Cdk5的IC50为4.5 mM。了解更多

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CX-4945 sodium salt

Catalog No. A16234
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CK2 抑制剂

CX-4945 sodium salt是一种有效的选择性ATP竞争性小分子蛋白激酶CK2抑制剂，对重组人CK2α的Ki和IC50分别为0.38和1 nM。了解更多

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SR-3029

Catalog No. A16235
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CK1δ/CK1ε 抑制剂

SR-3029是一种有效且高度特异性的CK1δ/CK1ε抑制剂，IC50为97 nM。了解更多

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TA-01

Catalog No. A16236
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CK 抑制剂

TA-01有效抑制CK1ε，CK1δ和p38α（IC50值分别为6.4、6.8和6.7 nM）。了解更多

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PF 670462

Catalog No. A11781
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Casein kinase 抑制剂

PF-670462是有效的、选择性CK1ε和CK1δ抑制剂，IC50分别为7.7和14 nM，其选择性是其他42种常见激酶的30倍以上。了解更多

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A-3 Hydrochloride

Catalog No. A13584
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PKA, PKG, Casein Kinase I and II 抑制剂

A-3 Hydrochloride是PKA（cAMP依赖性蛋白激酶，Ki =4.3μM）和cGMP依赖性蛋白激酶，Ki =3.8μM，PKC（蛋白激酶C，Ki =47μM），酪蛋白激酶I和II的抑制剂，和MLCK（肌球蛋白轻链激酶）（Ki =7.4μM）。了解更多

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TMCB

Catalog No. A13977
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CK2/ERK8 抑制剂

MCB抑制酪蛋白激酶2（CK2）和细胞外信号调节激酶8（ERK8/MAPK15）（CK2和ERK8的IC50 = 0.50 uM）。了解更多

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LDE225 Diphosphate

Catalog No. A12774
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Smoothened 抑制剂

LDE225 Diphosphate 是一种具有潜在抗肿瘤活性的口服生物利用小分子平滑（Smo）拮抗剂。抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。了解更多

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PF-5274857

Catalog No. A12775
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Smoothened 抑制剂

PF-5274857是一种新型Smo拮抗剂，它以4.6±1.1 nmol/L的K（i）特异性结合Smo，并以2.7±1.4 nmol/L的IC（50）完全阻断下游基因Gli1的转录活性。在细胞中。了解更多

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BMS-833923 (XL-139)

Catalog No. A13204
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Smoothened 抑制剂

BMS-833923 (XL-139)是一种生物可利用的小分子SMO(平滑)抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
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Glasdegib (PF-04449913)

Catalog No. A13881
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Smoothened 抑制剂

PF-04449913是有效且口服可生物利用的平滑化抑制剂。了解更多

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