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GSK973
Item number: Cay42057-10
A BET BD2 inhibitor (IC50s = 31.62, 15.85, 15.85, and 39.81 nM for BRD2, BRD3, BRD4, and BRDTBD2, respectively), selective for BD2 in BRD2, BRD3, BRD4, and BRDT over BD1 in the same BRDs (IC50s = >10,000 nM for all). Formulation: A solid. InChI:...
| Keywords: | (2S,3S)-2-(fluoromethyl)-2,3-dihydro-N7-methyl-N5-(1a,5beta,6beta)-3-oxabicyclo[3.1.0]hex-6-yl-3-phenyl-5,7-benzofurandica... |
| Application: | BET BD2 inhibitor |
| CAS | 2138473-38-6 |
| MW: | 410.44 D |
From 244.00€
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PS-10
Item number: Cay42068-1
A PDHK inhibitor (IC50s = 2.07, 0.8, 21.3, and 0.77 µM for PDHK1, -2, -3, and -4, respectively), selectively binds to PDHK2 over Hsp90 (Kds = 0.239 and 47 µM, respectively), increases heart, liver, and kidney pyruvate dehydrogenase complex activity, decreases blood glucose levels in a glucose tolerance test, and...
| Keywords: | 2-[(2,4-dihydroxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindole-4,6-diol |
| Application: | PDHK inhibitor |
| CAS | 1564265-82-2 |
| MW: | 323.3 D |
From 45.00€
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Methylliberine
Item number: Cay42071-10
A methylxanthine alkaloid. Formulation: A solid. InChI: InChI=1S/C9H12N4O3/c1-11-5-6(12(2)9(11)15)10-8(16-4)13(3)7(5)14/h1-4H3. InChIKey: ZVQXCXPGLSBNCX-UHFFFAOYSA-N. SMILES: CN(C1=C2C(N(C(OC)=N1)C)=O)C(N2C)=O
| Keywords: | 7,9-dihydro-2-methoxy-1,7,9-trimethyl-1H-purine-6,8-dione |
| Application: | Methylxanthine alkaloid |
| CAS | 51168-26-4 |
| MW: | 224.2 D |
From 55.00€
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TrkB Agonist Prodrug R13
Item number: Cay42074-1
A prodrug form of 7,8-dihydroxyflavone, increases hippocampal phosphorylated levels of TrkB, ERK, and Akt in 5XFAD mice at 43.6 mg/kg per day, p.o., decreases the number of malformed neurons and increases the number of neurons and active synapses in the hippocampus in 5XFAD mice, decreases the number of plaques and...
| Keywords: | TrkB-IN-1, Tropomyosin-related Kinase B Agonist Prodrug R13, Tropomyosin-related Kinase B Inhibitor 1,... |
| Application: | 7,8-dihydroxyflavone prodrug |
| CAS | 1609067-49-3 |
| MW: | 368.3 D |
From 153.00€
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BMS 466442
Item number: Cay42075-1
An Asc-1 inhibitor, selectively inhibits Asc-1 in HEK293 cells expressing Asc-1 (IC50 = 36.8 nM) over 40 other transporters (IC50s = >10 µM), inhibits serine, cysteine, glycine, and alanine import and cAMP-induced increases in the OCR and decreases UCP1 levels in primary human white and brown adipose cells at 100...
| Keywords: | N-[[5-methoxy-6-(phenylmethoxy)-1H-indol-2-yl]carbonyl]-1-(phenylmethyl)-L-histidine, methyl ester |
| Application: | Asc-1 inhibitor |
| CAS | 1598424-76-0 |
| MW: | 538.6 D |
From 45.00€
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diABZI STING Agonist-1
Item number: Cay42079-1
An activator of the STING pathway, induces secretion of IFN-beta in human PBMCs (EC50 = 130 nM), increases serum levels of Ifn-beta, Il-6, Tnf, and Cxcl1 in wild-type, but not Sting-/-, mice at 2.5 mg/kg, inhibits the cytopathic effect of HCoV-229E in infected MRC-5 cells (EC50 = 3 nM), decreases the level of...
| Keywords: | diABZI Stimulator of Interferon Genes Agonist 1, Diamidobenzimidazole Stimulator of Interferon Genes Agonist 1,... |
| Application: | STING pathway activator |
| CAS | 2138498-18-5 |
| MW: | 849.9 D |
From 147.00€
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TGN 073
Item number: Cay42086-10
An AQP4 facilitator, increases glymphatic transport and parenchymal penetration of a gadolinium-based tracer in rats at 200 mg/kg, increases AQP4 polarization and reduces brain retention of exogenous Aß40 in mice fed a high-fat diet. Formulation: A solid. InChI:...
| Keywords: | N-[3-(phenylmethoxy)-2-pyridinyl]-benzenesulfonamide |
| Application: | AQP4 facilitator |
| CAS | 877459-36-4 |
| MW: | 340.4 D |
From 85.00€
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FX12
Item number: Cay42089-1
An RNF5 inhibitor and degrader, binds to RNF5 and inhibits its E3 ligase activity in cell-free assays, induces proteasomal degradation of RNF5 via the ERAD pathway in HeLa cells from 1.25-20 µM,. Formulation: A solid. InChI: InChI=1S/C10H8O4S/c1-14-10(11)9-6-7-4-2-3-5-8(7)15(9,12)13/h2-6H,1H3. InChIKey:...
| Keywords: | 1,1-dioxide, benzo[b]thiophene-2-carboxylic acid, methyl ester |
| Application: | RNF5 inhibitor / degrader |
| CAS | 1807639-36-6 |
| MW: | 224.2 D |
From 76.00€
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Prostaglandin D2 Inhibitor
Item number: Cay42095-1
A PGD2 receptor antagonist (DP, IC50 = 0.3 nM), inhibits PGD2-induced cAMP accumulation in LS 174T cells that endogenously express the DP receptor. Formulation: A solid. InChI:...
| Keywords: | PGD2 Inhibitor, PGD2 Inhibitor 1, PGD2-IN-1, Prostaglandin D2 Inhibitor 1, Prostaglandin D2-IN-1,... |
| Application: | Prostaglandin D2 receptor (PTGDR) antagonist |
| CAS | 885066-67-1 |
| MW: | 460.35 D |
From 65.00€
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KU-0058948
Item number: Cay42098-1
A PARP1 and PARP2 inhibitor (IC50s = 3.4 and 1.5 nM, respectively), selective for PARP1 over PARP3, PARP4, and tankyrase (IC50s = 40, 1,200, and >10,000 nM, respectively), selectively inhibits the survival of embryonic stem cells lacking Brca1 or Brca2 over embryonic stem cells expressing wild-type Brca1 or Brca2,...
| Keywords: | 4-[[4-fluoro-3-[(hexahydro-1H-1,4-diazepin-1-yl)carbonyl]phenyl]methyl]-1(2H)-phthalazinone |
| Application: | PARP1 / PARP2 inhibitor |
| CAS | 763111-49-5 |
| MW: | 380.4 D |
From 60.00€
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AZD 3458
Item number: Cay42104-1
A PI3Kgamma inhibitor (IC50 = 0.79 nM), selective for PI3Kgamma over PI3Kalpha, PI3Kbeta, and PI3Kdelta (IC50s = 7.94, >31.62, and 0.316 µM, respectively), PI3KC2alpha, PI3KC2gamma, and PI3KC3 (IC50s = >10, 3.16, and 7.94 µM, respectively), and a panel of 395 kinases at 1 µM but does inhibit PI3KC2beta (IC50 = 31.62...
| Keywords: | N-[5-[2-[(1S)-1-cyclopropylethyl]-2,3-dihydro-7-(methylsulfonyl)-1-oxo-1H-isoindol-5-yl]-4-methyl-2-thiazolyl]-acetamide |
| Application: | PI3Kgamma inhibitor |
| CAS | 2132961-46-5 |
| MW: | 433.55 D |
From 116.00€
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GS-9901
Item number: Cay42105-1
A PI3Kdelta inhibitor (IC50 = 1 nM), selective for PI3Kdelta over PI3Kalpha, PI3Kbeta, and PI3Kgamma (IC50s = 750, 100, and 190 nM, respectively) and a panel of 456 additional kinases, including 11 lipid and 56 mutant kinases, at 10 µM, activates basophils in isolated human whole blood (EC50 = 1 nM), decreases ankle...
| Keywords: | 2,4-diamino-6-[[(S)-[5-chloro-8-fluoro-3,4-dihydro-4-oxo-3-(3-pyridinyl)-2-quinazolinyl]cyclopropylmethyl]amino]-5-pyrimid... |
| Application: | PI3Kdelta inhibitor |
| CAS | 1640247-87-5 |
| MW: | 477.9 D |
From 122.00€
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