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Merck
CN

528111

PI 3-Kα Inhibitor IV

The PI 3-Kα Inhibitor IV, also referenced under CAS 1188890-32-5, controls the biological activity of PI 3-Kα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

别名:

PI 3-Kα Inhibitor IV, 3-(4-Morpholinothieno[3,2-d]pyrimidin-2-yl)phenol, 2HCl, PI 3-K Inhibitor IV

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关于此项目

经验公式(希尔记法):
C16H15N3O2S · 2HCl
化学文摘社编号:
分子量:
386.30
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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InChI key

WPSXNMUJNQUDND-UHFFFAOYSA-N

SMILES string

[s]1c2c(nc(nc2N4CCOCC4)c3cc(ccc3)O)cc1.Cl.Cl

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

off-white

solubility

DMSO: 10 mg/mL

shipped in

ambient

Quality Level

General description

A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-kinases (IC50 = 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively) and inhibits non-PI 3-K kinases only at much higher concentrations (IC50 ≥3.4 µM for Cdk2/E, KDR, PKA, and PKCα). Shown to inhibit cell proliferation (IC50 = 580 nM) and serum-stimulated Akt phosphorylation (IC50<3 µM) in A375 melanoma cells.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PI 3-Kα
Product does not compete with ATP.
Reversible: no
Target IC50: 2 nM, 16 nM, 660 nM, and 220 nM for p110α, p110β p110γ, and PI 3-K C2β, respectively

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

Hayakawa, M., et al. 2006. Bioorg. Med. Chem.14, 6847.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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相关内容

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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