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Item number: Cay41978-1
An inhibitor of the Bcl-2-Bim and Bcl-xL-Bim protein-protein interactions (IC50s = 3.9 and 4.5 nM, respectively, in fluorescence polarization assays), induces apoptosis in MLL-AF9,NrasG12D mouse AML cells overexpressing human Bcl-2 or Bcl-xL but not Mcl-1, Bfl-1, or Bcl-W at 1 µM, induces apoptosis in wild-type but...
| Keywords: | 4-[4-[(R)-(4'-chloro[1,1'-biphenyl]-2-yl)hydroxymethyl]-1-piperidinyl]-N-[[4-[[(1R)-3-[(2-hydroxyethyl)methylamino]-1-[(ph... |
| Application: | Bcl-2-Bim / Bcl-xL-Bim protein-protein interactions inhibitor |
| CAS | 1357576-48-7 |
| MW: | 945.5 D |
From 60.00€
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Item number: Cay41980-10
A P2X7 receptor antagonist (IC50 = 3.2 nM for the human receptor), inhibits LPS- and BzATP-induced increases in ROS levels in THP-1 macrophages at 1 µM, decreases the accumulation of misfolded tau aggregates in the brain and improves learning and memory in the Y-maze and contextual fear conditioning tests in human...
| Keywords: | (2S)-N-[[2-chloro-3-(trifluoromethyl)phenyl]methyl]-1-methyl-5-oxo-2-pyrrolidinecarboxamide |
| Application: | P2X7 receptor antagonist |
| CAS | 1001389-72-5 |
| MW: | 334.72 D |
From 120.00€
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Item number: Cay41981-1
A precursor in the synthesis of delafloxacin. Formulation: A solid. InChI: InChI=1S/C24H23F3N4O5/c1-4-35-24(34)14-10-31(22-17(27)6-16(26)21(28)29-22)18-7-19(15(25)5-13(18)20(14)32)30-8-12(9-30)36-23(33)11(2)3/h5-7,10-12H,4,8-9H2,1-3H3,(H2,28,29). InChIKey: VMXLACIKUJJQTC-UHFFFAOYSA-N. SMILES:...
| Keywords: | 1-(6-amino-3,5-difluoro-2-pyridinyl)-6-fluoro-1,4-dihydro-7-[3-(2-methyl-1-oxopropoxy)-1-azetidinyl]-4-oxo-3-quinolinecarb... |
| Application: | Delafloxacin synthesis precursor |
| CAS | 442526-91-2 |
| MW: | 504.46 D |
From 70.00€
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Item number: Cay41990-1
A RET inhibitor (IC50 = 0.26 nM for the wild-type enzyme), selective for RET over a panel of 217 additional kinases but does inhibit 39 tyrosine kinases by > 50% at 26 nM, inhibits the phosphorylation of wild-type RET (IC50 = 21.9 nM) and 15 RET mutants (IC50s = 2.69-108 nM) in Ba/F3 cells. Formulation: A solid....
| Keywords: | Enbezotinib,... |
| Application: | RET inhibitor |
| CAS | 2359650-19-2 |
| MW: | 424.4 D |
From 139.00€
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Item number: Cay42011-10
A probe for protein sulfenylation. Formulation: A solid. InChI: InChI=1S/C23H20O2P.BrH/c1-2-18-25-23(24)19-26(20-12-6-3-7-13-20,21-14-8-4-9-15-21)22-16-10-5-11-17-22,/h1,3-17H,18-19H2,1H/q+1,/p-1. InChIKey: BXRYUYJDTSNWNI-UHFFFAOYSA-M. SMILES: O=C(OCC#C)C[P+](C1=CC=CC=C1)(C2=CC=CC=C2)C3=CC=CC=C3.[Br-]
| Keywords: | Wittig-alkyne O, [2-oxo-2-(2-propyn-1-yloxy)ethyl]triphenyl-phosphonium, monobromide |
| Application: | Protein sulfenylation probe |
| CAS | 1648555-11-6 |
| MW: | 439.28 D |
From 153.00€
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Item number: Cay42029-1
An NK1 receptor antagonist (Ki = 0.03 nM), selective for NK1 over NK2 and NK3 receptors (IC50s = >10,000 nM for both), 5-HT1A, 5-HT1D, and 5-HT2A receptors (Kis = 501, 251, and 316 nM, respectively), and histamine H1 and H2 receptors (Kis = 316 and 251 nM, respectively), inhibits resiniferatoxin-induced systemic...
| Keywords: | GR 205171, N-[[2S-methoxy-5-[5-(trifluoromethyl)-1H-tetrazol-1-yl]phenyl]methyl]-2-phenyl-3S-piperidinamine |
| Application: | NK1 receptor antagonist |
| CAS | 168266-90-8 |
| MW: | 432.4 D |
From 137.00€
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Item number: Cay42034-1
A P2X4 receptor antagonist (IC50 = 0.75 µM), selective for P2X4 over P2X1, P2X2a, P2X2b, and P2X7 but does inhibit P2X3 by 35.9% at 10 µM, decreases fEPSP slopes in rat hippocampal slices at 10 µM, inhibits nitroglycerin-induced mechanical hyperalgesia in a mouse model of chronic migraine at 28 mg/kg, decreases...
| Keywords: | 5-(3-bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one |
| Application: | P2X4 receptor antagonist |
| CAS | 768404-03-1 |
| MW: | 355.2 D |
From 40.00€
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Item number: Cay42035-1
An inactive metabolite of quetiapine, formed from quetiapine via CYP3A. Formulation: A solid. InChI: InChI=1S/C21H25N3O3S/c25-14-16-27-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)28(26)20-8-4-2-6-18(20)22-21/h1-8,25H,9-16H2. InChIKey: FXJNLPUSSHEDON-UHFFFAOYSA-N. SMILES:...
| Keywords: | 11-(4-(2-(2-hydroxyethoxy)ethyl)piperazin-1-yl)dibenzo[b,f][1,4]thiazepine 5-oxide |
| Application: | Inactive quetiapine metabolite |
| CAS | 329216-63-9 |
| MW: | 399.51 D |
From 147.00€
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Item number: Cay42037-1
A nonpeptide antagonist of BB1 and BB2 (Kis = 0.17 and 1 nM, respectively), induces calcium mobilization in HL-60 cells expressing FPR1 or FPR2/ALX (EC50s = 0.31 and 0.66 µM, respectively), inhibits the proliferation of C6 glioma cells (IC50 = 2 µM), increases social interaction in the social interaction test in...
| Keywords: | (aS)-N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-a-methyl-a-[[[(4-nitrophenyl)amino]carbonyl]amino]-1H-indole-3-propan... |
| Application: | Neuromedin B receptor (BB1) / gastrin-releasing peptide receptor (BB2) nonpeptide antagonist |
| CAS | 204067-01-6 |
| MW: | 584.7 D |
From 40.00€
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Item number: Cay42038-1
A beta-catenin/CBP inhibitor and active metabolite of PRI-724, reduces the proliferation and protein levels of cyclin D1, alpha-smooth muscle actin (alpha-Sma), and Ki-67, a marker of cell proliferation, in primary mouse HSCs at 10 µM, decreases viability in continuous culture-activated primary mouse HSCs at 10 µM,...
| Keywords: | (6S,9S,9aS)-hexahydro-6-[(4-hydroxyphenyl)methyl]-2,9-dimethyl-4,7-dioxo-N-(phenylmethyl)-8-(8-quinolinylmethyl)-2H-pyrazi... |
| Application: | beta-catenin/CBP inhibitor, active PRI-724 metabolite |
| CAS | 1422253-37-9 |
| MW: | 578.7 D |
From 147.00€
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Item number: Cay42040-10
A 20S proteasome inhibitor (IC50 = ~1 µM), induces the accumulation of ubiquitinated proteins in HCT116 colon cancer cells at 1 µM, sensitizes HCT116 p53+/+ and HCT116 p53-/- cells to ionizing radiation-induced cytotoxicity in an additive and synergistic manner, respectively, decreases the viability of macrophages...
| Keywords: | Proteasome Inhibitor IX, B,B'-[(1-methyl-4-oxo-3,5-piperidinediylidene)bis(methylidyne-4,1-phenylene)]bis-boronic acid |
| Application: | 20S proteasome (chymotrypsin-like activity) inhibitor |
| CAS | 856849-35-9 |
| MW: | 377 D |
From 76.00€
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Item number: Cay42042-10
An ALK5 inhibitor (IC50 = 0.0015 µM), selective for ALK over TGF-betaRII (IC50 = > 15 µM) and a panel of 213 additional kinases at 1 µM, inhibits TGF-beta-induced increases in the nuclear translocation of phosphorylated SMAD2/3 in Mv 1 Lu cells (IC50 = 0.35 µM), decreases tumor growth in an MC-38 murine colon...
| Keywords: | 6-[4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl]-imidazo[1,2-b]pyridazine-3-carbonitrile |
| Application: | ALK5 inhibitor |
| CAS | 2001559-19-7 |
| MW: | 382.78 D |
From 143.00€
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