-
Gamma-secretase inhibitor
BMS-708163 is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta synthesis. -
GSK-3 Inhibitor
CHIR99021 is an aminopyrimidine derivative that inhibits GSK3α and GSK3β with IC50 values of 10 and 6.7 nM, respectively.- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Claudia Z Han, .et al. , Immunity, 2023, Sep 12;56(9):2152-2171 PMID: 37582369
- Eric Lian, .et al. , STAR Protoc, 2023, May 22;4(2):102314 PMID: 37220001
- Tomoki Murata, .et al. , Int Immunol, 2023, Apr 13 PMID: 37052267
- Shunsuke Murakami, .et al. , Regen Ther, 2022, Nov 25;21:574-583 PMID: 36475025
- Adam Pietrobon, .et al. , Cell Rep, 2022, Jul 5;40(1):111048 PMID: 35793620
- Takayuki Miyoshi, .et al. , J Gastroenterol, 2022, Jun;57(6):441-452 PMID: 35294680
- Tomoki Kamatani, .et al. , Inflamm Regen, 2022, Feb 2;42(1):4 PMID: 35105370
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Otsuka R, .et al. , Sci Rep, 2020, Jan 14;10(1):224 PMID: 31937817
- Yu Huang, .et al. , Stem Cells Int, 2019, 2019: 3975689 PMID: 31565060
-
Hedgehog signaling inhibitor
Cyclopamine is a Smo or hedgehog signaling pathway inhibitor. -
Hedgehog antagonist
GDC-0449 (Vismodegib) is a more potent novel and specific synthetic oral hedgehog pathway inhibitor with an IC50 of 3 nM.- Yichuan You, .et al. , J Hazard Mater, 2023, Oct 15:460:132489 PMID: 37688871
- Yan Guo, .et al. , Differentiation, 2023, May-Jun;131:82-88 PMID: 37178555
- Mucahit Varli, .et al. , Sci Rep, 2023, Feb 16;13(1):2811 PMID: 36797277
- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Yi Yang, .et al. , Molecules, 2018, Nov; 23(11): 2968 PMID: 30441806
- Olesen UH, .et al. , Lasers Surg Med, 2018, Aug 28 PMID: 30152536
-
Gamma secretase inhibitor
DAPT (GSI-IX) is an inhibitor of γ-secretase that causes a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures with IC50 values of 115 and 200 nM for total Aβ and Aβ42 respectively.- Kubra Telli, .et al. , Turkish Journal of Biochemistry, 2023, February 6
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Ellagic acid is a natural phenol antioxidant found in numerous fruits and vegetables. The antiproliferative and antioxidant properties of ellagic acid have spurred preliminary research into the potential health benefits of ellagic acid consumption.
-
Emodin is a purgative resin, from rhubarb, the buckthorn and Japanese Knotweed (Fallopia japonica). It belongs to a family of compounds called anthraquinones, which have shown anti-inflammatory and anticancer effects
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
-
Gamma-secretase inhibitor
RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
-
Gamma-secretase inhibitor
Semagacestat (LY450139) is a γ-secretase blocker for Aβ42, Aβ40 and Aβ38 with IC50 of 10.9 nM, 12.1 nM and 12.0 nM, respectively. Semagacestat also inhibits Notch signaling with IC50 of 14.1 nM.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
-
PARP inhibitor
XAV 939 is a TNKS inhibitor (IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively).- Shizu Aikawa, .et al. , EMBO J, 2017, Jul 14; 36(14): 2146-2160 PMID: 28588064
- Mikaël M. Martino, .et al. , Nat Commun, 2016, 7: 11051 PMID: 27001940
-
Wnt/beta-catenin inhibitor
ICG-001 is a specific inhibitor of Wnt/β-catenin signaling pathway that inhibits β-catenin/cyclic AMP response element-binding (CREB) protein transcription (IC50=3 microM) .- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- Seonmin Choi, .et al. , Yonsei Med J, 2021, Nov;62(11):1042-1051 PMID: 34672138
- Jasper C.Munro, .et al. , Livest Sci, 2019, 229 (2019) 159-169
- Kim JH, .et al. , Cell Rep, 2019, May 14;27(7):2105-2118.e5 PMID: 31091449
- Yamaoka R, .et al. , J Surg Oncol, 2018, Sep;118(4):664-674 PMID: 30196535
- Aida Y, .et al. , In Vitro Cell Dev Biol Anim, 2018, Jun;54(6):468-476 PMID: 29785536
-
SMO Antagonist
LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein. -
CK2 inhibitor
CX-4945 is a potent and selective orally bioavailable small molecule inhibitor of CK2 that inhibits human umbilical vein endothelial cell migration, tube formation, and blocks CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells.- Michael Ohene-Nyako, .et al. , ASN Neuro, 2023, Jan-Dec;15:17590914231158218 PMID: 36890725
- Wenjie Huang, .et al. , Am J Pathol, 2023, May;193(5):567-578 PMID: 37080661
- Xixi Zhao, .et al. , Cancer Res, 2022, Jun 6;82(11):2185-2195 PMID: 35385574
- Janeen H. Trembley, .et al. , Biomedicines, 2021, May; 9(5): 571 PMID: 34070147
- Tianzhi Huang, .et al. , Mol Cell, 2021, Mar 18;81(6):1276-1291 PMID: 33539787
- M Afzal, .et al. , Molecular and Cellular Biochemistry, 2020, 470, pages131-143
- Zaman MS, .et al. , Biometals, 2019, Oct 3 PMID: 31583500
- Fukumoto Y, .et al. , Biochem Biophys Res Commun, 2019, Sep 17;517(2):310-316 PMID: 31353086
- Fukumoto Y, .et al. , Biochem Biophys Res Commun, 2018, Oct 2;504(2):380-386 PMID: 29902452
- ST Ribeiro, .et al. , Leukemia, 2017, Jul; 31(7): 1603-1610 PMID: 27899804
- Valentina Gandin, .et al. , Nat Commun, 2016, 7: 11127 PMID: 27040916
- Ampofo E, .et al. , Eur Surg Res, 2016, 57(1-2):111-24 PMID: 27287005
- Emmanuel Ampofo, .et al. , Thromb Res., 2015, Nov;136(5):996-1006 PMID: 26381437
- Emmanuel Ampofo, .et al. , Biochim Biophys Acta., 2015, Oct;1852(10 Pt A):2123-36 PMID: 26189586
- A. Margarida Gomes, .et al. , Haematologica, 2014, 99(6): 1062-1068 PMID: 24561792
-
GSK-3 inhibitor
CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. -
γ-secretase inhibitor
YO-01027 is a dipeptidic γ-secretase inhibitor, an antiAlzheimer agent.- Weijun Zhang, .et al. , Stem Cell Rev Rep, 2023, Jan 7 PMID: 36609902
-
Gamma secretase inhibitor
LY-411575 is a selective, cell permeable, small molecule gamma secretase inhibitor.
- Haiwen Yu, .et al. , Immunol Invest, 2023, Feb;52(2):241-255 PMID: 36562737
- Wojciech J Szlachcic, .et al. , iScience, 2022, Jul 15;25(7) PMID: 35756892
- Zhang ZH, .et al. , APMIS, 2019, Jul 5 PMID: 31274210
- Bo Pang, .et al. , Biosci Rep, 2018, Dec 21; 38(6): BSR20181922 PMID: 30473538
- Shuo Li, .et al. , Int Immunopharmacol, 2018, Oct;63:129-136 PMID: 30086535
- Jiang BC, .et al. , Viral Immunol, 2017, Sep;30(7):522-532 PMID: 28410452
-
γ-secretase inhibitor
Begacestat is a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease. -
γ-secretase inhibitor
PF-03084014 is a reversible and selective inhibitor of γ-secretase with IC50 value of 6.2 nM . -
γ-Secretase Inhibitor
BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease. -
gamma-secretase modulator
E 2012 is γ-secretase inhibitor.- Yesuvadian R, .et al. , Biochem Biophys Res Commun., 2014, May 16;447(4):590-5 PMID: 24747079
-
Gamma-secretase modulator
gamma-secretase modulator 1 is a gamma-secretase modulator, gamma-secretase modulator 1 is useful for Alzheimer's disease. -
Gamma-secretase modulator
gamma-secretase modulator 2 is a potent and selective gamma-secretase modulator for treatment of Alzheimer's disease. -
Hedgehog signaling activator
Purmorphamine is a 2,6,9-trisubstituted purine that promotes the differentiation of both human and mouse mesenchymal progenitor cells into osteoblasts.- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
-
GSK-3 Inhibitor
Tideglusib is a GSK-3 inhibitor currently in phase II clinical trials for the treatment of Alzheimer disease and progressive supranuclear palsy- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
-
Casein kinase inhibitor
Potent and selective casein kinase 1ε (CK1ε) and CK1δ inhibitor (IC50 values are 7.7 and 14 nM respectively) that displays > 30-fold selectivity over 42 other common kinases. Inhibits PER protein nuclear translocation (EC50 = 290 nM) causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo. -
Wnt inhibitor
KY02111 is a potent and selective Wnt signaling pathway inhibitor discovered by a cell-based screening, which promotes differentiation of hESCs/iPSCs to cardiomyocytes when used at the second stage of differenitation.- Abinayaselvi Murugan, .et al. , bioRxiv, 2024, February 22
-
γ-secretase inhibitor
BMS 299897 is an orally active, potent γ-secretase inhibitor (IC50 = 12 nM). Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo.- Chao Liu, .et al. , Cell Death Differ, 2018, Apr; 25(4): 661-676 PMID: 29238071
-
Epidermal keratinocyte differentiation inducer
Casein Kinase II Inhibitor IV is a small-molecule inducer of epidermal keratinocyte differentiation. -
YAP inhibitor
Verteporfin is a small molecule that inhibits TEAD, YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin.
- Yu Ren, .et al. , Eur J Med Res, 2024, May 30;29(1):303 PMID: 38812041
- Po-Ju Lee, .et al. , J Exp Clin Cancer Res, 2022, Aug 20;41(1):254 PMID: 35986369
- Ling-Yan Liu, .et al. , Int J Mol Med, 2020, Dec;46(6):2235-2250 PMID: 33125123
- Wang Y, .et al. , Toxicol Appl Pharmacol, 2019, 2019 Dec 5;387:114852 PMID: 31812773
- Abe T, .et al. , Toxicol Sci, 2018, Oct 1;165(2):408-419 PMID: 29893953
-
Wnt inhibitor
IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. Wnt proteins bind to receptors on the cell surface, initiating a signaling cascade that leads to β-catenin activation of gene transcription.- Charles A.Herring, .et al. , Cell, 2022, Oct 27;S0092-8674(22)01258-2 PMID: 36318921
-
GSK-3 inhibitor
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.- Yuki Shimizu, .et al. , NPJ Precis Oncol, 2022, Mar 17;6(1):16 PMID: 35301419
-
Smoothened Inhibitor
LDE225 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. -
Smoothened Inhibitor
PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells. -
PORCN inhibitor
LGK974 is a highly potent, selective and orally bioavailable Porcupine inhibitor (Wnt signaling antagonist) with an IC50 <1 nM in the Wnt signaling reporter assay and Porcupine binding assay.- Sho Tsukamoto, .et al. , Development, 2023, Aug 1;150(15):dev201734 PMID: 37539462
- Bopei Cui, .et al. , Signal Transduct Target Ther, 2023, Sep 25;8(1):366 PMID: 37743418
- A-Ri Cho, .et al. , Sci Rep, 2022, Apr 29;12(1):7013 PMID: 35487932
- Yang JM, .et al. , Toxicology, 2018, Dec 1;410:65-72 PMID: 30205152
- E Lemieux, .et al. , Oncogene, 2015, Sep 17; 34(38): 4914-4927 PMID: 25500543
-
GSK3 inhibitor
AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.- Shengzhong Liu, .et al. , J Cell Biochem, 2019, 2019 PMID: 30887575
-
PORCN/Wnt inhibitor
Wnt-C59 is a very potent and highly selective Wnt signaling antagonist with an IC50 ~ 74 pM in the Wnt signaling reporter assay.- Laksitorini MD, .et al. , Sci Rep, 2019, Dec 23;9(1):19718 PMID: 31873116