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Merck

528116

Sigma-Aldrich

PI 3-Kα Inhibitor VIII

The PI 3-Kα Inhibitor VIII controls the biological activity of PI 3-Kα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

동의어(들):

PI 3-Kα Inhibitor VIII, N-((1E)-(6-Bromoimidazo[1,2-a]pyridin-3-yl)methylene)-Nʹ-methyl-Nʹʹ-(2-methyl-5-nitrobenzene)sulfonohydrazide, HCl, PIK-75, PI 3-K Inhibitor VIII

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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C16H14BrN5O4S · 2H2O · xHCl
CAS 번호:
372196-77-5
Molecular Weight:
488.31 (free base basis)
MDL number:
MFCD12546130
UNSPSC 코드:
12352200
NACRES:
NA.28

주요 문서

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기술 서비스
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도움 문의

Quality Level

100

분석

≥95% (HPLC)

양식

solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
desiccated (hygroscopic)
protect from light

색상

pale yellow

solubility

DMSO: 10 mg/mL

배송 상태

ambient

저장 온도

2-8°C

SMILES string

[S](=O)(=O)(N(\N=C\c2[n]3c(nc2)ccc(c3)Br)C)c1c(ccc(c1)[N+](=O)[O-])C.Cl

InChI

1S/C16H14BrN5O4S.ClH/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;1H/b19-9+;

InChI key

VOUDEIAYNKZQKM-MYHMWQFYSA-N

관련 카테고리

일반 설명

A cell-permeable imidazopyridine compound that acts as a highly potent and ATP-competitive DNA-PK and p110α-selective PI3-K inhibitor (IC50 = 0.3, 40, 100, and 850 nM for p110α, p110γ, PI 3-K C2β, and p110β, respectively). Shown to effectively block cellular PI3-K/Akt signaling and inhibit tumor growth both in vitro (IC50 ≤58 nM in MCF7, MCF7 ADR-res, HeLa, A375, and A549 cultures) and in mice in vivo (62% inhibition of HeLa xenograft in 2 weeks, 50 mg/kg/day, i.p.).

포장

Packaged under inert gas

제조 메모

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Kim, S., et al. 2007. Blood110, 4206.
Hayakawa, M., et al. 2007. Bioorg. Med. Chem.15, 5837.
Knight, Z.A., et al. 2007. Cell125, 733.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

면책조항

Toxicity: Regulatory Review (Z)

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.

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문서 라이브러리 방문

Soochong Kim et al.
Blood, 110(13), 4206-4213 (2007-09-11)
Platelets release insulin-like growth factor-1 (IGF-1) from alpha granules upon activation. We have investigated the regulation of IGF-1 in G(i)-dependent pathways leading to Akt activation and the role of IGF-1 in platelet activation. IGF-1 alone failed to induce platelet aggregation
Masahiko Hayakawa et al.
Bioorganic & medicinal chemistry, 15(17), 5837-5844 (2007-07-03)
We have previously reported the imidazo[1,2-a]pyridine derivative 4 as a novel p110alpha inhibitor; however, although 4 is a potent inhibitor of p110alpha enzymatic activity and tumor cell proliferation in vitro, it is unstable in solution and ineffective in vivo. To
Zachary A Knight et al.
Cell, 125(4), 733-747 (2006-05-02)
Phosphoinositide 3-kinases (PI3-Ks) are an important emerging class of drug targets, but the unique roles of PI3-K isoforms remain poorly defined. We describe here an approach to pharmacologically interrogate the PI3-K family. A chemically diverse panel of PI3-K inhibitors was

관련 콘텐츠

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

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