DiscoveryProbe™ FDA-approved Drug Library
Catalog No.
L1021
2320个获得上市批准以及药典收录的原料药
Featured Products
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
DiscoveryProbe™ FDA-approved drug library includes 2320 approved drugs and API from pharmacopoeia for high throughput screening (HTS) and high content screening (HCS). All drugs were from approved institutions such as FDA, EMA, HMA, CFDA, PMDA, or pharmacopoeia such as USP, BP, EP, JP, Ph.Int, etc. The bioactivity and safety of these drugs were confirmed in vitro or in vivo. So, it can be used to find new targets for old drugs.
- 1. De-Ping Wang, Fang-Ying Jiang, et al. "Crystal structure of RNA helicase from Saint Louis encephalitis virus and discovery of its inhibitors." Genes Dis. 2022 Jul 31;10(2):389-392. PMID: 37223502
- 2. Jingjing Zhang, Yingpei Jiang, et al. "Development of FRET and Stress Granule Dual-Based System to Screen for Viral 3C Protease Inhibitors." Molecules. 2023 Mar 28;28(7):3020. PMID: 37049786
- 3. Fabrizio Fierro, Lior Peri, et al. "Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor ligands." Cell Mol Life Sci. 2023 Apr 3;80(4):114. PMID: 37012410
- 4. Zhiyu Song, Chenglong Zhao, et al. "Carbenoxolone disodium suppresses the migration of gastric cancer by targeting HDAC6." Future Med Chem. 2023 Feb;15(4):333-344. PMID: 36946221
- 5. Liuqing Chen, Meiting Chen, et al. "Ratiometric NAD+ Sensors Reveal Subcellular NAD+ Modulators." ACS Sens. 2023 Apr 28;8(4):1518-1528. PMID: 36931900
- 6. Beatrice Alexander-Howden, Li Zhang, et al. "A screen for MeCP2-TBL1 interaction inhibitors using a luminescence-based assay." Sci Rep. 2023 Mar 8;13(1):3868. PMID: 36890145
- 7. Eirini D Tseligka, Stéphanie Conzelmann, et al. "Identification of selective hepatitis delta virus ribozyme inhibitors by high-throughput screening of small molecule libraries." JHEP Rep.2022 Dec 17;5(3):100652. PMID: 36704052
- 8. Dandan Jiang, Peizhi Ma. "Canagliflozin, characterized as a HDAC6 inhibitor, inhibits gastric cancer metastasis." Front Oncol. 2022 Nov 15;12:1057455. PMID: 36457493
- 9. Elizabeth R Sharlow, Danielle C Llaneza, et al. "High content screening miniaturization and single cell imaging of mature human feeder layer-free iPSC-derived neurons." SLAS Discov. 2022 Oct 21;S2472-5552(22)13703-2. PMID: 36273809
- 10. Xianglian Zhou, Yuting Pan, et al. "Tideglusib Inhibits Pif1 Helicase of Bacteroides sp. via an Irreversible and Cys-380-Dependent Mechanism." ACS Omega. 2022 Aug 25;7(35):31289-31298. PMID: 36092604
- 11. Jhin Jieh Lim, Lissa Hooi, et al. "Rational drug combination design in patient-derived avatars reveals effective inhibition of hepatocellular carcinoma with proteasome and CDK inhibitors." J Exp Clin Cancer Res. 2022 Aug 15;41(1):249. PMID: 35971164
- 12. Youjie Yin, Peng Ma, et al. "The CRTC-CREB axis functions as a transcriptional sensor to protect against proteotoxic stress in Drosophila." Cell Death Dis. 2022 Aug 6;13(8):688 PMID: 35933423
- 13. Can Cui, Yuting Pan, et al. "Eltrombopag binds SDC4 directly and enhances MAPK signaling and macropinocytosis in cancer cells." American Journal of Cancer Research, 15 Jun 2022, 12(6):2697-2710. PMID: 35812066
- 14. David Pladevall-Morera, María Castejón-Griñán, et al. "ATRX-Deficient High-Grade Glioma Cells Exhibit Increased Sensitivity to RTK and PDGFR Inhibitors." Cancers (Basel) 2022 Mar 31;14(7):1790. PMID: 35406561
- 15. Jian Guo, Sam Shen, et al. "JPA: Joint Metabolic Feature Extraction Increases the Depth of Chemical Coverage for LC-MS-Based Metabolomics and Exposomics." Metabolites. 2022 Feb 26;12(3):212. PMID: 35323655
- 16. Shiu-Wan Chan, Talha Shafi, et al. "Kite-Shaped Molecules Block SARS-CoV-2 Cell Entry at a Post-Attachment Step." Viruses.2021 Nov 19;13(11):2306. PMID: 34835112
- 17. Narmeen S Rashid, Nicole S Hairr, et al. "Identification of nuclear export inhibitor-based combination therapies in preclinical models of triple-negative breast cancer." Transl Oncol.2021 Dec;14(12):101235. PMID: 34628286
- 18. Yunxia Xu, Ke Chen, et al. "Repurposing clinically approved drugs for COVID-19 treatment targeting SARS-CoV-2 papain-like protease." Int J Biol Macromol2021 Oct 1;188:137-146. PMID: 34364941
- 19. Jing Nan, Shaoran Zhang, et al. "Discovery of Novel GMPS Inhibitors of Candidatus Liberibacter Asiaticus by Structure Based Design and Enzyme Kinetic." Biology (Basel).20212021 Jun 28;10(7):594. PMID: 34203217
- 20. Yan Ling Ng, Cyrill Kafi Salim, et al. "Drug repurposing for COVID-19: Approaches, challenges and promising candidates." Pharmacol Ther.2021 Dec;228:107930. PMID: 34174275
- 21. Xianglian Zhou, Yuting Pan, et al. "Tanshinones induce tumor cell apoptosis via directly targeting FHIT." Sci Rep. 2021 Jun 9;11(1):12217. PMID: 34108553
- 22. Alon Ben David, Eran Diamant, et al. "Identification of SARS-CoV-2 Receptor Binding Inhibitors by In Vitro Screening of Drug Libraries." Molecules.20202021 May 27;26(11):3213. PMID: 34072087
- 23. James M. Havrilla, Cong Liu, et al. "PhenCards: a data resource linking human phenotype information to biomedical knowledge." Genome Med. 2021 May 25;13(1):91. PMID: 34034817
- 24. Peizhi Ma, Gang Jia, et al. "Monobenzone, a Novel and Potent KDM1A Inhibitor, Suppresses Migration of Gastric Cancer Cells." Front Pharmacol. 2021 Apr 15;12:640949. PMID: 33935733
- 25. Lesley-Anne Pearson, Charlotte J Green, et al. "Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7-Methyltransferase Using RapidFire Mass Spectrometry." SLAS Discov.2021 Jul;26(6):749-756. PMID: 33724070
- 26. Adam Pickard, Ben C Calverley, et al. "Discovery of re-purposed drugs that slow SARS-CoV-2 replication in human cells." bioRxiv. 2021 Mar 10;2021.01.31.428851. PMID: 33564760
- 27. Gur D, Chitlaru T, Mamroud E, et al. "Screening of an FDA-Approved Library for Novel Drugs against Y. pestis." Antibiotics (Basel). 2021 Jan 3;10(1):40. PMID: 33401634
- 28. Moore JA, Meakin M, et al. "Effects of Caspofungin, Tolcapone, and Other FDA-Approved Medications on MRSA Susceptibility to Vancomycin." J Glob Antimicrob Resist. 2020;S2213-7165(20)30078-3. PMID: 32247076
- 29. Turner TH, Alzubi MA, et al. "Identification of synergistic drug combinations using breast cancer patient-derived xenografts." Sci Rep. 2020 Jan 30;10(1):1493. PMID: 32001757
- 30. Yang JJ, Han Y, et al. "Streamlined MRM method transfer between instruments assisted with HRMS matching and retention-time prediction." Anal Chim Acta. 2020;1100:88–96. PMID: 31987156
| Catalog No. | Product Name | Summary | Targets | CAS Number | Smiles | |
| A3298 | Cetirizine | Antihistamine | Neuroscience|Histamine Receptor | 83881-51-0 | C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl | |
| A3789 | Salmeterol xinafoate | β2-adrenergic receptor agonist | GPCR/G protein|Adrenergic Receptor | 94749-08-3 | C1=CC=C(C=C1)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O.C1=CC=C2C(=C1)C=CC(=C2O)C(=O)O | |
| A4363 | Fluvastatin Sodium | HMG-CoA reductase inhibitor | Metabolism|HMG-CoA Reductase | 93957-55-2 | CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)[O-])O)O)C3=CC=C(C=C3)F.[Na+] | |
| A4370 | Moclobemide (Ro 111163) | Reversible inhibitor of MAO-A | Metabolism|MAO | 71320-77-9 | C1COCCN1CCNC(=O)C2=CC=C(C=C2)Cl | |
| A8252 | Nintedanib(BIBF 1120) | VEGFR/PDGFR/FGFR inhibitor | Tyrosine Kinase/Adaptors|PDGFR | 928326-83-4 | CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)NC(=C3C4=C(C=C(C=C4)C(=O)OC)NC3=O)C5=CC=CC=C5 | |
| B1792 | Montelukast Sodium | Leukotriene receptor antagonist | GPCR/G protein|CysLT1 receptor | 151767-02-1 | CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)[O-])O.[Na+] | |
| N1674 | Piperine | MAPK inhibitor | Natural Products | 94-62-2 | C1CCN(CC1)C(=O)C=CC=CC2=CC3=C(C=C2)OCO3 | |
| N1707 | Coumarin | Precursor in chemical reaction | Natural Products | 91-64-5 | C1=CC=C2C(=C1)C=CC(=O)O2 | |
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下载 APExBIO化合物库使用说明 下载 DiscoveryProbe™ FDA-approved Drug Library（SDF & XLSX） |
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" to show IC50| Form | Pre-dissolved DMSO solutions | Stability | Solution: -20°C for 12 months, -80°C for 24 months |
| Packaging | 96-well Microplate format with peelable foil seal and EVA cap (20 μL/well, 10 mM DMSO); 96-well DeepWell format with peelable foil seal and EVA cap (100 μL/well, 10 mM DMSO); 96-well rack with Matrix 2D Barcoded ScrewTop Storage tubes (250 μL or 100 μL/well, 10 mM DMSO). |
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| Shipping Condition | Evaluation sample solution: ship with blue ice All other available size: ship with RT, or blue ice upon request |
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1. Barrows NJ, Campos RK, Powell ST, et al. A Screen of FDA-Approved Drugs for Inhibitors of Zika Virus Infection. Cell Host Microbe. 2016 Jul 27. pii: S1931-3128(16)30303-1.
Abstract
We interrogated a FDA-approved chemicals library for their ability to block infection of human HuH-7 cells by a newly isolated ZIKV strain (ZIKV MEX_I_7). In our in vitro screening assay, more than 20 out of 774 tested compounds reduced ZIKV infection. Then these compounds were further validated for inhibition of ZIKV infection in human neural, cervical and placental stem cell lines, as well as primary human amnion cells. We found that others that had no previously known antiviral activity (e.g., daptomycin) and anti-flaviviral drugs (e.g., bortezomib and mycophenolic acid) were identified as inhibitors of ZIKV infection. There were several drugs that reduced ZIKV infection across multiple cell types, which could be tested in clinical studies of ZIKV infection and provided small molecules to study ZIKV pathogenesis.
Abstract
We interrogated a FDA-approved chemicals library for their ability to block infection of human HuH-7 cells by a newly isolated ZIKV strain (ZIKV MEX_I_7). In our in vitro screening assay, more than 20 out of 774 tested compounds reduced ZIKV infection. Then these compounds were further validated for inhibition of ZIKV infection in human neural, cervical and placental stem cell lines, as well as primary human amnion cells. We found that others that had no previously known antiviral activity (e.g., daptomycin) and anti-flaviviral drugs (e.g., bortezomib and mycophenolic acid) were identified as inhibitors of ZIKV infection. There were several drugs that reduced ZIKV infection across multiple cell types, which could be tested in clinical studies of ZIKV infection and provided small molecules to study ZIKV pathogenesis.
2. Stavrovskaya IG, Narayanan MV, Zhang W, et al. Clinically approved heterocyclics act on a mitochondrial target and reduce stroke-induced pathology. J Exp Med. 2004 Jul 19;200(2):211-22.
Abstract
Mitochondria are a major checkpoint in several pathways leading to neuronal cell death and the mitochondrial permeability transition (mPT) may be critical in stroke-related injury. In order to prove this hypothesis, 1,040 FDA-approved drugs and other bioactive compounds were tested as potential mPT inhibitors. We found that 28 structurally related drugs, including tricyclic antipsychotics and antidepressants, capable of delaying the mPT. Clinically achievable doses of promethazine inhibited mPT and were protective in both in vitro and mouse models of stroke. Also, promethazine protected primary neuronal cultures subjected to oxygen-glucose deprivation and reduced neurological impairment and infarct size in mice subjected to middle cerebral artery occlusion/reperfusion. These results provided a class of safe, tolerable drugs for stroke and neurodegeneration and also provided new tools for understanding mitochondrial roles in neuronal cell death.
Abstract
Mitochondria are a major checkpoint in several pathways leading to neuronal cell death and the mitochondrial permeability transition (mPT) may be critical in stroke-related injury. In order to prove this hypothesis, 1,040 FDA-approved drugs and other bioactive compounds were tested as potential mPT inhibitors. We found that 28 structurally related drugs, including tricyclic antipsychotics and antidepressants, capable of delaying the mPT. Clinically achievable doses of promethazine inhibited mPT and were protective in both in vitro and mouse models of stroke. Also, promethazine protected primary neuronal cultures subjected to oxygen-glucose deprivation and reduced neurological impairment and infarct size in mice subjected to middle cerebral artery occlusion/reperfusion. These results provided a class of safe, tolerable drugs for stroke and neurodegeneration and also provided new tools for understanding mitochondrial roles in neuronal cell death.
