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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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I128086-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $94.90 | |
I128086-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $427.90 | |
I128086-100mg | 100mg | In stock | $533.90 |
Synonyms | 2-Benzoxazolamine, 5-(4-amino-1-(1-methylethyl)-1H-pyrazolo(3,4-d)pyrimidin-3-yl)- | 3-(2-aminobenzo[d]oxazol-5-yl)-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine | 5-(4-azanyl-1-propan-2-yl-pyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine | J-00481 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | INK 128 exhibits an enzymatic inhibition activity against mTOR and more than 100-fold selectivity to PI3K kinases [1]. As TORC1/2 inhibitor, INK 128 inhibits both the phosphorylation of S6 and 4EBP1, the downstream substrates of TORC1, and selectively inh |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Serine/threonine-protein kinase mTOR inhibitor |
Note | 5mg卖完停产,不再备货 |
Product Description | INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). |
ALogP | 1.7 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine |
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INCHI | InChI=1S/C15H15N7O/c1-7(2)22-14-11(13(16)18-6-19-14)12(21-22)8-3-4-10-9(5-8)20-15(17)23-10/h3-7H,1-2H3,(H2,17,20)(H2,16,18,19) |
InChi Key | GYLDXIAOMVERTK-UHFFFAOYSA-N |
Canonical SMILES | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N |
Isomeric SMILES | CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(C=C3)OC(=N4)N)N |
PubChem CID | 45375953 |
Molecular Weight | 309.33 |
PubChem CID | 45375953 |
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CAS Registry No. | 1224844-38-5 |
RCSB PDB Ligand | FE5 |
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Solubility | DMSO |
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1. Liu Q, Thoreen C, Wang J, Sabatini D, Gray NS. (2009) mTOR Mediated Anti-Cancer Drug Discovery.. Drug Discov Today Ther Strateg, 6 (2): (47-55). [PMID:20622997] [10.1021/op500134e] |
2. Schenone S, Brullo C, Musumeci F, Radi M, Botta M. (2011) ATP-competitive inhibitors of mTOR: an update.. Curr Med Chem, 18 (20): (2995-3014). [PMID:21651476] [10.1021/op500134e] |
3. Hsieh AC, Liu Y, Edlind MP, Ingolia NT, Janes MR, Sher A, Shi EY, Stumpf CR, Christensen C, Bonham MJ et al.. (2012) The translational landscape of mTOR signalling steers cancer initiation and metastasis.. Nature, 485 (7396): (55-61). [PMID:22367541] [10.1021/op500134e] |
4. Arendse LB, Murithi JM, Qahash T, Pasaje CFA, Godoy LC, Dey S, Gibhard L, Ghidelli-Disse S, Drewes G, Bantscheff M et al.. (2022) The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages.. Sci Transl Med, 14 (667): (eabo7219). [PMID:36260689] [10.1021/op500134e] |