Product Name :
AX-15836
Description:
AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.
CAS:
2035509-96-5
Molecular Weight:
648.78
Formula:
C32H40N8O5S
Chemical Name:
5-({2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]phenyl}amino)-2-methanesulfonyl-9-methyl-2, 4, 6, 9-tetraazatricyclo[9.4.0.0, ]pentadeca-1(15), 3, 5, 7, 11, 13-hexaen-10-one
Smiles :
CCOC1=CC(=CC=C1NC1=NC2=C(C=N1)N(C)C(=O)C1=CC=CC=C1N2S(C)(=O)=O)C(=O)N1CCC(CC1)N1CCN(C)CC1
InChiKey:
HTFNVAVTYILUCF-UHFFFAOYSA-N
InChi :
InChI=1S/C32H40N8O5S/c1-5-45-28-20-22(30(41)39-14-12-23(13-15-39)38-18-16-36(2)17-19-38)10-11-25(28)34-32-33-21-27-29(35-32)40(46(4,43)44)26-9-7-6-8-24(26)31(42)37(27)3/h6-11,20-21,23H,5,12-19H2,1-4H3,(H,33,34,35)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥360 days if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.|Product information|CAS Number: 2035509-96-5|Molecular Weight: 648.78|Formula: C32H40N8O5S|Chemical Name: 5-({2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]phenyl}amino)-2-methanesulfonyl-9-methyl-2, 4, 6, 9-tetraazatricyclo[9.4.0.0, ]pentadeca-1(15), 3, 5, 7, 11, 13-hexaen-10-one|Smiles: CCOC1=CC(=CC=C1NC1=NC2=C(C=N1)N(C)C(=O)C1=CC=CC=C1N2S(C)(=O)=O)C(=O)N1CCC(CC1)N1CCN(C)CC1|InChiKey: HTFNVAVTYILUCF-UHFFFAOYSA-N|InChi: InChI=1S/C32H40N8O5S/c1-5-45-28-20-22(30(41)39-14-12-23(13-15-39)38-18-16-36(2)17-19-38)10-11-25(28)34-32-33-21-27-29(35-32)40(46(4,43)44)26-9-7-6-8-24(26)31(42)37(27)3/h6-11,20-21,23H,5,12-19H2,1-4H3,(H,33,34,35)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 100 mg/mL (154.14 mM; Need ultrasonic)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Amivantamab} medchemexpress|{Amivantamab} JAK/STAT Signaling|{Amivantamab} Technical Information|{Amivantamab} In Vitro|{Amivantamab} supplier|{Amivantamab} Autophagy} |Shelf Life: ≥360 days if stored properly.{{Efruxifermin} site|{Efruxifermin} Protein Tyrosine Kinase/RTK|{Efruxifermin} Biological Activity|{Efruxifermin} Data Sheet|{Efruxifermin} custom synthesis|{Efruxifermin} Epigenetics} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:33205667 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|AX-15836 shows more than 1, 000-fold selectivity for ERK5 over a panel of over 200 kinases. It also exhibits selectivity over BRD4 with a Kd of 3, 600 nM. AX15836 shows similar intracellular potency (4–9 nM) across all cells tested, including peripheral blood mononuclear cells (PBMCs), endothelial cells, and oncogenic cell lines. AX15836 was completely ineffective (EC50>10 μM) to suppress inflammatory cytokine response, suggesting that it was the BRD inhibition component of the compounds that mediated cytokine reduction. In HUVEC and HeLa cell types, samples treated with AX15836 shows very few genes to be differentially expressed. AX15836 could clearly inhibit the EGF-stimulated, phosphorylated form of ERK5 in HeLa cells.|References:|Lin EC, et al. ERK5 kinase activity is dispensable for cellular immune response and proliferation. Proc Natl Acad Sci U S A. 2016 Oct 18;113(42):11865-11870.Products are for research use only. Not for human use.|
