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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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P333866-5mg | 5mg | In stock | $76.90 | |
P333866-10mg | 10mg | In stock | $138.90 | |
P333866-25mg | 25mg | In stock | $311.90 | |
P333866-50mg | 50mg | In stock | $560.90 | |
P333866-100mg | 100mg | In stock | $1,009.90 | |
P333866-200mg | 200mg | In stock | $1,817.90 |
a free base is a selective inhibitor of PI 3-kinase p110α
Synonyms | N'-[(1E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride | DS-15894 | N-[(E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide | NCGC00346500-05 | UNII-9058I |
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Specifications & Purity | Moligand™, ≥98% |
Storage Temp | Store at -20°C,Desiccated |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit alpha;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit beta;Inhibitor of phosphatidylinositol-4;5-bisphosphate 3-kinase catalytic subunit delta;Inhi |
Product Description | PIK-75, free base is a selective inhibitor of PI 3-kinase p110α (IC50 values are 5.8, 76 nM and 1.3 μM at PI 3-kinase p110α, PI 3-kinase p110γ and PI 3-kinase p110β respectively). Inhibits production of PIP2 and PIP3 in adipocytes, phosphorylation of Akt and activation of mTORC1. Cell-permeable. |
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IUPAC Name | N-[(E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylideneamino]-N,2-dimethyl-5-nitrobenzenesulfonamide |
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INCHI | InChI=1S/C16H14BrN5O4S/c1-11-3-5-13(22(23)24)7-15(11)27(25,26)20(2)19-9-14-8-18-16-6-4-12(17)10-21(14)16/h3-10H,1-2H3/b19-9+ |
InChi Key | QTHCAAFKVUWAFI-DJKKODMXSA-N |
Canonical SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)N=CC2=CN=C3N2C=C(C=C3)Br |
Isomeric SMILES | CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)/N=C/C2=CN=C3N2C=C(C=C3)Br |
PubChem CID | 10275789 |
Molecular Weight | 452.28 |
PubChem CID | 10275789 |
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ChEMBL Ligand | CHEMBL393525 |
CAS Registry No. | 372196-67-3 |
RCSB PDB Ligand | F4N |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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C23071081 | Certificate of Analysis | Nov 19, 2022 | P333866 |
C23071095 | Certificate of Analysis | Nov 19, 2022 | P333866 |
C23071107 | Certificate of Analysis | Nov 19, 2022 | P333866 |
C23071109 | Certificate of Analysis | Nov 19, 2022 | P333866 |
C23071129 | Certificate of Analysis | Nov 19, 2022 | P333866 |
C23071132 | Certificate of Analysis | Nov 19, 2022 | P333866 |
Solubility | Soluble in DMSO (5 mM). |
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Starting at $103.90
1. Hayakawa M, Kawaguchi K, Kaizawa H, Koizumi T, Ohishi T, Yamano M, Okada M, Ohta M, Tsukamoto S, Raynaud FI et al.. (2007) Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.. Bioorg Med Chem, 15 (17): (5837-44). [PMID:17601739] |
2. Knight ZA, Gonzalez B, Feldman ME, Zunder ER, Goldenberg DD, Williams O, Loewith R, Stokoe D, Balla A, Toth B et al.. (2006) A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.. Cell, 125 (4): (733-47). [PMID:16647110] |
3. Zheng Z, Amran SI, Thompson PE, Jennings IG. (2011) Isoform-selective inhibition of phosphoinositide 3-kinase: identification of a new region of nonconserved amino acids critical for p110α inhibition.. Mol Pharmacol, 80 (4): (657-64). [PMID:21778304] |