A6730

Akt1/2 kinase inhibitor

Name: Akt1/2 kinase inhibitor
Brand: SIGMA

≥98% (HPLC), Akt1/2 kinase inhibitor, powder

동의어(들):

1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one trifluoroacetate salt hydrate, Akt Inhibitor VIII trifluoroacetate salt hydrate, Akti-1/2 trifluoroacetate salt hydrate

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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):

C₃₄H₂₉N₇O · xC₂HF₃O₂ · yH₂O

CAS 번호:

616871-83-1

Molecular Weight:

551.64 (anhydrous free base basis)

MDL number:

MFCD08705407

UNSPSC 코드:

12352200

PubChem Substance ID:

24891133

NACRES:

NA.77

주요 문서

모든 문서 보기

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제품 이름

Akt1/2 kinase inhibitor, ≥98% (HPLC)

Quality Level

100

분석

≥98% (HPLC)

양식

powder

색상

yellow

solubility

DMSO: ≥10 mg/mL

주관자

Merck & Co., Inc., Kenilworth, NJ, U.S.

저장 온도

2-8°C

SMILES string

[H]O[H].OC(=O)C(F)(F)F.O=C1Nc2ccccc2N1C3CCN(CC3)Cc4ccc(cc4)-c5nc6cc7nc[nH]c7cc6nc5-c8ccccc8

InChI

1S/C34H29N7O.C2HF3O2.H2O/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;3-2(4,5)1(6)7;/h1-13,18-19,21,25H,14-17,20H2,(H,35,36)(H,39,42);(H,6,7);1H2

InChI key

CRRPFKCJZALCLQ-UHFFFAOYSA-N

애플리케이션

Akt plays a role in signal transduction pathways of cell proliferation, apoptosis, angiogenesis, and diabetes. Akt1 and Akt2 dual kinase inhibitors are capable of sensitizing tumor cells to certain apoptotic stimuli, and inhibit Akt phosphorylation in vivo. Akt1 kinase activity and its regulation by extracellular signaling factors in vivo in hematopoietic cells suggests the activation of AKT1 involves intracellular translocation of the kinase from cytosol to membrane.

생화학적/생리학적 작용

Akt1/2 kinase inhibitor; isozyme selective with preference toward Akt1.

Isozyme selective Akt1/2 kinase inhibitor. In in vitro kinase assays, Akt1/2 kinase inhibitor shows IC₅₀ = 58 nM, 210 nM, and 2.12 mM for Akt1, Akt2, and Akt3, respectively, The inhibition appears to be pleckstrin homology (PH) domain-dependent and the Akt1/2 kinase inhibitor has no inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 μM.

특징 및 장점

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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Journal of enzyme inhibition and medicinal chemistry, 25(2), 204-215 (2010-03-13)

Attenuation of protein kinases by selective inhibitors is an extremely active field of activity in anticancer drug development. Therefore, Akt, a serine/threonine protein kinase, also known as protein kinase B (PKB), represents an attractive potential target for therapeutic intervention. Recent

A Simple and robust automated kinase profiling platform using luminescent ADP accumulation technology.

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Assay and drug development technologies, 7(6), 573-584 (2010-01-12)

Kinases continue to be one of the most important targets in today's drug discovery efforts. Following the identification of lead compounds through screening efforts, it is important to profile these leads against other kinases within that family, as well as

KPNA3 Confers Sorafenib Resistance to Advanced Hepatocellular Carcinoma via TWIST Regulated Epithelial-Mesenchymal Transition.

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Journal of Cancer, 10(17), 3914-3925 (2019-08-17)

Sorafenib, a multikinase inhibitor, is a new standard treatment for patients with advanced hepatocellular carcinoma (HCC). However, resistance to this regimen is frequently observed in clinical practice, and the molecular basis of this resistance remains largely unknown. Herein, the antitumor

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Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.

Zhijian Zhao et al.

Bioorganic & medicinal chemistry letters, 15(4), 905-909 (2005-02-03)

This letter describes the discovery of a novel series of dual Akt1/Akt2 kinase inhibitors, based on a 2,3,5-trisubstituted pyridine scaffold. Compounds from this series, which contain a 5-tetrazolyl moiety, exhibit more potent inhibition of Akt2 than Akt1.

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Akt1/2 kinase inhibitor

≥98% (HPLC), Akt1/2 kinase inhibitor, powder

크기 선택

제품정보 (DICE 배송 시 비용 별도)

주요 문서

속성

제품 이름

Quality Level

분석

양식

색상

solubility

주관자

저장 온도

SMILES string

InChI

InChI key

관련 카테고리

설명

애플리케이션

생화학적/생리학적 작용

특징 및 장점

안전성 정보

Storage Class Code

WGK

Flash Point (°F)

Flash Point (°C)

문서

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