PIK-75, hydrochlorideCAS: 372196-77-5
MF: C16H14BrN5O4S•HCl
MW: 488.74
A selective inhibitor of PI 3-kinase isoform p110α.

PIK-75, hydrochloride (CAS 372196-77-5)

PIK-75, hydrochloride | CAS 372196-77-5 is rated 5.0 out of 5 by 1.
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Synonym: 2-methyl-5-nitro-2-[(6- bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide-benzenesulfonic acid, monohydrochloride
Application: A selective inhibitor of PI 3-kinase isoform p110α
CAS Number: 372196-77-5
Purity: ≥98%
Molecular Weight: 488.74
Molecular Formula: C16H14BrN5O4S•HCl
* Refer to Certificate of Analysis for lot specific data (including water content).
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PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1 in adipocytes and myotubes. PI 3-kinase (PI3K) catalyzes the synthesis of the second messengers PtdIns-(3)-P, PtdIns-(3,4)-P2, and PtdIns-(3,4,5)-P3. The PI 3-kinase family of enzymes is comprised of 15 members that are divided into three classes according to their structure, substrate specificity, and mode of regulation. In the class I PI 3-kinases, p110α is the primary PI 3-kinase isoform required for insulin signaling in adipocytes and myotubes and is frequently mutated in primary tumors. Small molecule inhibitors of p110α are of interest in cancer treatment research. PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM. PIK-75 inhibits p110γ and p110β considerably less effectively.


References

1 Fan, Q., Knight, Z.A., Goldenberg, D.D., et al. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell 9 341-349 (2006). 2 Knight, Z.A., Gonzalez, B., Feldman, M.E., et al. A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Cell 125 733-747 (2006).

Physical State :
Solid
Solubility :
Soluble in DMSO (~0.25 mg/ml), and DMF (~0.5 mg/ml).
Storage :
Store at -20° C
Melting Point :
221-223° C
Density :
1.66 g/cm3
Refractive Index :
n20D ~1.70 (Predicted)
IC50 :
PI3-kinase p110-alpha subunit: IC50 = 0.3 nM (bovine); PI3-kinase p110-gamma subunit: IC50 = 40 nM (human); A375: IC50 = 58 nM (human); HeLa: IC50 = 51 nM (human); MCF7: IC50 = 19 nM (human)
pK Values :
pKb: 2.16 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
45265864
SMILES :
CC1=C(C=C(C=C1)[N+](=O)[O-])S(=O)(=O)N(C)/N=C/C2=CN=C3N2C=C(C=C3)Br.Cl

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Duong Duong, HQ. et al. (PubMed 24366069) reported that inhibition of NRF2 by PIK-75 augments the sensitivity of pancreatic cancer cells to gemcitabine. -SCBT Publication Review
Date published: 2015-05-17
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