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.
Synonym(s):
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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About This Item
Empirical Formula (Hill Notation):
C16H15N3O2S · 2HCl
CAS Number:
Molecular Weight:
386.30
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
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
storage temp.
2-8°C
General description
A cell-permeable morpholino-thienopyrimidine compound that acts as a potent and isoform-selective inhibitor of PI 3-Ks (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.
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
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
Warning
Toxicity: Irritant (B)
Reconstitution
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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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