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AKT Inhibitor VIII - ≥97%, high purity , CAS No.612847-09-3, Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3

≥97%

CAS#: 612847-09-3
Formula: C₃₄H₂₉N₇O
Molecular Weight: 551.66
MDL number: MFCD09026909
PubChem CID: 135398501

Item Number

B304138

Grouped product items
SKU	Size	Availability	Price
B304138-5mg	5mg	In stock	$129.90
B304138-25mg	25mg	In stock	$585.90
B304138-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$848.90

Potent isozyme selective Akt1/2 kinase inhibitor

View related series

AKT serine/threonine kinase 1 Allosteric modulator AKT serine/threonine kinase 2 Allosteric modulator AKT serine/threonine kinase 3 Allosteric modulator

Basic Description

Synonyms	Akt inhibitor VIII\|612847-09-3\|Akti-1/2\|YX4CPQ6V6X\|Akt-I 1,2\|1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one\|1-(1-(4-(6-Phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)benzyl)-piperidin-4-yl)-1H-
Specifications & Purity	≥97%
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Action Type	ALLOSTERIC MODULATOR
Mechanism of action	Allosteric modulator of AKT serine/threonine kinase 1;Allosteric modulator of AKT serine/threonine kinase 2;Allosteric modulator of AKT serine/threonine kinase 3
Product Description	product description： Akti-1/2 (Akt Inhibitor VIII) is a highly selective Akt1/Akt2 inhibitor with IC50 of 58 nM/210 nM, respectively, about 36-fold selectivity for Akt1 over Akt3. Akti-1/2 induces apoptosis.

Associated Targets

AKT3 Tchem RAC-gamma serine/threonine-protein kinase 1 Activities

Discover Target: AKT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT2 Tchem RAC-beta serine/threonine-protein kinase 1 Activities

Discover Target: AKT2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AKT1 Tchem RAC-alpha serine/threonine-protein kinase 1 Activities

Discover Target: AKT1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	3-[1-[[4-(6-phenyl-8H-imidazo[4,5-g]quinoxalin-7-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
INCHI	InChI=1S/C34H29N7O/c42-34-39-26-8-4-5-9-31(26)41(34)25-14-16-40(17-15-25)20-22-10-12-24(13-11-22)33-32(23-6-2-1-3-7-23)37-29-18-27-28(36-21-35-27)19-30(29)38-33/h1-13,18-19,21,25,38H,14-17,20H2,(H,39,42)
InChi Key	IWCQHVUQEFDRIW-UHFFFAOYSA-N
Canonical SMILES	C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=C(N=C6C=C7C(=NC=N7)C=C6N5)C8=CC=CC=C8
Isomeric SMILES	C1CN(CCC1N2C3=CC=CC=C3NC2=O)CC4=CC=C(C=C4)C5=C(N=C6C=C7C(=NC=N7)C=C6N5)C8=CC=CC=C8
PubChem CID	135398501
Molecular Weight	551.66

PubChem CID

ChEMBL Ligand

CAS Registry No.

RCSB PDB Ligand

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2 results found

Lot Number	Certificate Type	Date	Item
J2114042	Certificate of Analysis	Aug 09, 2024	B304138
J2114043	Certificate of Analysis	Aug 09, 2024	B304138

References

1. Lindsley CW, Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE et al.. (2005) Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.. Bioorg Med Chem Lett, 15 (3): (761-4). [PMID:15664853]
2. Nagae K et al.. (2018) Glucagon-like peptide-1 analogue liraglutide facilitates wound healing by activating PI3K/Akt pathway in keratinocytes.. Diabetes Res Clin Pract, 146 (155-161). [PMID:30367901]
3. Tutunea-Fatan E et al.. (2015) GRK2 targeted knock-down results in spontaneous hypertension, and altered vascular GPCR signaling.. J Biol Chem, 290 (8): (5141-55). [PMID:25561731]
4. Lai Y et al.. (2016) Inhibition of mTOR sensitizes breast cancer stem cells to radiation-induced repression of self-renewal through the regulation of MnSOD and Akt.. Int J Mol Med, 37 (2): (369-77). [PMID:26707081]
5. Xu P et al.. (2022) Hypoxia-mediated YTHDF2 overexpression promotes lung squamous cell carcinoma progression by activation of the mTOR/AKT axis.. Cancer Cell Int, 22 (13). [PMID:34996459]
6. Naspi A et al.. (2017) IGFBP-3 inhibits Wnt signaling in metastatic melanoma cells.. Mol Carcinog, 56 (2): (681-693). [PMID:27377812]
7. Revu S et al.. (2018) IL-23 and IL-1ß Drive Human Th17 Cell Differentiation and Metabolic Reprogramming in Absence of CD28 Costimulation.. Cell Rep, 22 (10): (2642-2653). [PMID:29514093]
8. Sun H et al.. (2016) Let-7 miRNAs sensitize breast cancer stem cells to radiation-induced repression through inhibition of the cyclin\xa0D1/Akt1/Wnt1 signaling pathway.. Mol Med Rep, 14 (4): (3285-92). [PMID:27574028]
9. Wang Y et al.. (2017) PI3K inhibitor LY294002, as opposed to wortmannin, enhances AKT phosphorylation in gemcitabine-resistant pancreatic cancer cells.. Int J Oncol, 50 (2): (606-612). [PMID:28000865]
10. Foxall E et al.. (2019) PAK4 Kinase Activity Plays a Crucial Role in the Podosome Ring of Myeloid Cells.. Cell Rep, 29 (11): (3385-3393.e6). [PMID:31825823]
11. Cui J et al.. (2019) Proteomic Identification of Pathways Responsible for the Estradiol Therapeutic Window in AD Animal Models.. Front Cell Neurosci, 13 (437). [PMID:31680862]
12. Mao XQ et al.. (2022) RNA-seq and ATAC-seq analyses of multilineage differentiating\xa0stress enduring\xa0cells: Comparison with dermal fibroblasts.. Cell Biol Int, 46 (9): (1480-1494). [PMID:35673985]
13. Yang Y et al.. (2016) The PDGF-BB-SOX7 axis-modulated IL-33 in pericytes and stromal cells promotes metastasis through tumour-associated macrophages.. Nat Commun, 7 (11385). [PMID:27150562]
14. Tutunea-Fatan E et al.. (2015) The role of CCL21/CCR7 chemokine axis in breast cancer-induced lymphangiogenesis.. Mol Cancer, 14 (35). [PMID:25744065]
15. Li N et al.. (2019) The role of Zeb1 in the pathogenesis of morbidly adherent placenta.. Mol Med Rep, 20 (3): (2812-2822). [PMID:31322233]
16. Meng C et al.. (2020) White Spot Syndrome Virus Benefits from Endosomal Trafficking, Substantially Facilitated by a Valosin-Containing Protein, To Escape Autophagic Elimination and Propagate in the Crustacean Cherax quadricarinatus.. J Virol, 94 (24): [PMID:32967962]

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