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JNJ-47117096 (trifluoroacetate salt)
Item number: Cay41605-1
A MELK inhibitor (IC50 = 37 nM), selective for MELK over CAMKIIdelta, MNK2, CAMKIIgamma, and MLCK (IC50s = 810, 760, 1,000, and 1,000 nM, respectively) but does inhibit FLT3 (IC50 = 18 nM), inhibits MELK autophosphorylation (IC50 = 0.52 µM) and MELK proteasome-dependent degradation in MCF-7 cells, induces cellular...
| Keywords: | 2-methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)-benzamide, trifluoroacetate salt |
| Application: | MELK inhibitor |
| MW: | 476.4 D |
From 74.00€
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Werner Syndrome RecQ Helicase-IN-4
Item number: Cay41679-10
An inhibitor of WRN (IC50 = 60 nM), selectively inhibits the growth of SW48 cells over DLD-1-WRN-KO cells (GI50s = 70 and >10,000 nM, respectively), reduces tumor volume in an SW48 mouse xenograft model at 240 mg/kg per day. Formulation: A solid. InChI:...
| Keywords: | Werner Syndrome RecQ Helicase Inhibitor 4, WS RecQ Helicase Inhibitor 4, WS RecQ Helicase-IN-4,... |
| Application: | WRN inhibitor |
| CAS | 2869954-53-8 |
| MW: | 666.7 D |
From 610.00€
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Lucitanib
Item number: Cay41711-1
A dual inhibitor of VEGFR and FGFR, inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50s = 7, 25, and 10 nM, respectively) and FGFR1 and FGFR2 (IC50s = 17.5 and 82.5 nM, respectively), selective for VEGFR1-3 and FGFR1-2 over FGFR3 and FGFR4 (IC50s = 237.5 and >1,000 nM, respectively), as well c-Kit, PDGFRalpha, and PDGFRbeta...
| Keywords: | AL 3810, E-3810, 6-[[7-[(1-aminocyclopropyl)methoxy]-6-methoxy-4-quinolinyl]oxy]-N-methyl-1-naphthalenecarboxamide |
| Application: | VEGFR / FGFR dual inhibitor |
| CAS | 1058137-23-7 |
| MW: | 443.5 D |
From 40.00€
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Lenacapavir
Item number: Cay41830-10
An inhibitor of HIV capsid protein-protein interactions, inhibits viral replication in HIV-1-infected primary human CD4+ T cells and macrophages (mean IC50s = 32 and 56 pM, respectively), two HIV-2 clinical isolates (mean IC50 = 885 pM), and 23 HIV-1 clinical isolates (mean IC50 = 50 pM), prevents stHIV-A19...
| Keywords: | GS-6207, GS-714207, GS-CA2,... |
| Application: | HIV capsid protein-protein interaction inhibitor |
| CAS | 2189684-44-2 |
| MW: | 968.28 D |
From 269.00€
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Palazestrant
Item number: Cay41843-1
An ERalpha antagonist (IC50 = 6.4 nM), induces degradation of ERalpha in MCF-7 cells (EC50 = 0.52 nM), decreases the proliferation of MCF-7 and CAMA-1 breast cancer cells (IC50s = 1.8 and 1.7 nM, respectively), inhibits estradiol-induced cell cycle progression in the same cells at 100 nM, reduces tumor growth and...
| Keywords: | OP-1250,... |
| Application: | ERalpha antagonist |
| CAS | 2092925-89-6 |
| MW: | 449.6 D |
From 45.00€
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AMG 511
Item number: Cay41853-1
An inhibitor of class I PI3Ks, selective for PI3K over 372 other protein kinases at 1 µM, inhibits Akt phosphorylation in U87MG cells (IC50 = 4 nM), reduces tumor growth in a U87MG mouse xenograft model at doses of 1, 3, and 10 mg/kg per day. Formulation: A solid. InChI:...
| Keywords: | 4-[2-[(5-fluoro-6-methoxy-3-pyridinyl)amino]-5-[(1R)-1-[4-(methylsulfonyl)-1-piperazinyl]ethyl]-3-pyridinyl]-6-methyl-1,3,... |
| Application: | Class I PI3K inhibitor |
| CAS | 1253573-53-3 |
| MW: | 517.58 D |
From 116.00€
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JNJ-42847922
Item number: Cay41854-10
An orexin receptor 2 antagonist (Ki = 10 nM), selective for OX2R over OX1R (Ki = 794 nM) and a panel of 50 receptors, ion channels, and transporters at 1 µM, reduces the latency to NREM sleep onset and increases the duration of NREM sleep in rats at 3, 10, and 30 mg/kg. Formulation: A solid. InChI:...
| Keywords: | MIN-202,... |
| Application: | Orexin receptor 2 antagonist |
| CAS | 1293281-49-8 |
| MW: | 407.5 D |
From 116.00€
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YH-306
Item number: Cay41874-10
An anticancer agent, reduces TGF-beta-induced transcriptional activity by 72.4% in a reporter assay using HaCaT cells at 1 µM, inhibits the proliferation of PC-9, H1299, and A549 cells (IC50s = 5.87, 8.07, and 7.9 µM, respectively), decreases migration of H1299 cells in a wound healing assay at 0.1, 0.5, or 1 µM,...
| Keywords: | 2-(4-hydroxyphenyl)-1-(1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-ethanone |
| Application: | Anticancer agent |
| CAS | 1373764-75-0 |
| MW: | 306.4 D |
From 85.00€
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SQ-609
Item number: Cay41875-10
An antibacterial agent, reduces the proliferation of M. tuberculosis in M. tuberculosis-infected J774 macrophages (MIC = 4 µg/ml), increases survival time in M. tuberculosis-infected female mice at 10 mg/kg per day. Formulation: A solid. InChI:...
| Keywords: | 1-[[1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-4-piperidinyl]methyl]-4-piperidinol |
| Application: | Antibacterial agent |
| CAS | 627052-25-9 |
| MW: | 346.6 D |
From 76.00€
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ISRIB
Item number: Cay41879-10
A mixture of cis-IRIB and trans-ISRIB, trans-ISRIB decreases ATF4-induced increases in gene transcription more effectively than cis-ISRIB in a reporter assay using HEK293T cells (IC50s = 5 and 600 nM, respectively), trans-ISRIB decreases the latency to escape in the Morris water maze and increases the length of...
| Keywords: | N,N'-1,4-cyclohexanediylbis[2-(4-chlorophenoxy)-acetamide |
| Application: | Cis-IRIB / trans-ISRIB mixture |
| CAS | 548470-11-7 |
| MW: | 451.3 D |
From 76.00€
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Macimorelin (acetate)
Item number: Cay41886-10
A growth hormone secretagogue and ghrelin receptor agonist, binds to GHS-R1a (IC50 = 123 nM for the human receptor), oral administration increases plasma growth hormone levels in dogs at 1 mg/kg, decreases gastric acid secretion in pylorus-ligated rats at 0.01 or 1 nmol/animal, i.c.v., increases acute food intake...
| Keywords: | AEZS-130, Aib-D-Trp-D-gTrp-CHO, Aib-D-Trp-D-gTrp-formyl, D 87575, EP 1572, JMV1843,... |
| Application: | Growth hormone secretagogue, ghrelin receptor agonist |
| CAS | 945212-59-9 |
| MW: | 534.61 D |
From 223.00€
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CM-4620
Item number: Cay41977-10
An inhibitor of Orai1/STIM1-containing SOCs (IC50 = 120 nM), selective for Orai1/STIM1-containing SOCs over Orai2/STIM2-containing SOCs (IC50 = 900 nM), decreases cholecystokinin- or taurolithocholic acid 3-sulfate-induced cell death in isolated mouse, rat, and human acini at 3 µM, reduces blood amylase and lipase...
| Keywords: | Zegrocractin, N-[5-(6-chloro-2,2-difluoro-1,3-benzodioxol-5-yl)-2-pyrazinyl]-2-fluoro-6-methyl-benzamide |
| Application: | Orai1/STIM1-containing SOC (store-operated calcium channel) inhibitor |
| CAS | 1713240-67-5 |
| MW: | 421.8 D |
From 116.00€
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