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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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X125609-1mg | 1mg | In stock | $14.90 | |
X125609-5mg | 5mg | In stock | $60.90 | |
X125609-10mg | 10mg | In stock | $85.90 | |
X125609-50mg | 50mg | In stock | $296.90 | |
X125609-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $494.90 |
ERK5/BMK1 inhibitor; also BRD4 inhibitor
Synonyms | XMD8-92|1234480-50-2|XMD 8-92|2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-B][1,4]benzodiazepin-6-one|2-{[2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino}-5,11-dimethyl-5,11-dihydro-6H-pyrimido[4,5-b][1 |
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Specifications & Purity | Moligand™, ≥97% |
Biochemical and Physiological Mechanisms | ERK5 (BMK1) and BRD4 inhibitor (Kdvalues are 80 and 190 nM, respectively). Also inhibits DCAMKL2, PLK4 and TNK1 (Kdvalues are 190, 600 and 890 nM). Blocks growth factor-induced activation of cellular BMK1 and reduces BMK1 activity inin vitrokinase assays. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of doublecortin like kinase 2;Inhibitor of mitogen-activated protein kinase 7;Inhibitor of polo like kinase 4;Inhibitor of tyrosine kinase non receptor 1 |
Product Description | XMD8-92 has been used as a specific extracellular signal regulated kinase 5 (ERK5) inhibitor in human umbilical vein endothelial cells (HUVECs) culture. |
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IUPAC Name | 2-[2-ethoxy-4-(4-hydroxypiperidin-1-yl)anilino]-5,11-dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one |
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INCHI | InChI=1S/C26H30N6O3/c1-4-35-23-15-17(32-13-11-18(33)12-14-32)9-10-20(23)28-26-27-16-22-24(29-26)30(2)21-8-6-5-7-19(21)25(34)31(22)3/h5-10,15-16,18,33H,4,11-14H2,1-3H3,(H,27,28,29) |
InChi Key | QAPAJIZPZGWAND-UHFFFAOYSA-N |
Canonical SMILES | CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C |
Isomeric SMILES | CCOC1=C(C=CC(=C1)N2CCC(CC2)O)NC3=NC=C4C(=N3)N(C5=CC=CC=C5C(=O)N4C)C |
PubChem CID | 46843772 |
Molecular Weight | 474.57 |
PubChem CID | 46843772 |
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ChEMBL Ligand | CHEMBL1673046 |
CAS Registry No. | 1234480-50-2 |
ChEBI | CHEBI:60325 |
RCSB PDB Ligand | 4WG |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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K2108433 | Certificate of Analysis | Aug 14, 2023 | X125609 |
K2108434 | Certificate of Analysis | Aug 14, 2023 | X125609 |
K2108436 | Certificate of Analysis | Aug 14, 2023 | X125609 |
K2108442 | Certificate of Analysis | Aug 14, 2023 | X125609 |
K2108798 | Certificate of Analysis | Aug 14, 2023 | X125609 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 18.98, Max Conc. mM: 40 |
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1. Yang Q, Deng X, Lu B, Cameron M, Fearns C, Patricelli MP, Yates 3rd JR, Gray NS, Lee JD. (2010) Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.. Cancer Cell, 18 (3): (258-67). [PMID:20832753] |