CCT128930 hydrochloride

SKU: orb1300887

Description

CCT128930 hydrochloride is a potent and selective AKT inhibitor (IC50 = 6 nM) that induces cell cycle arrest, DNA damage, and autophagy. It demonstrates significant selectivity over PKA and p70S6K. This compound is a valuable research tool for studying AKT signaling in cancer biology, with applications in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2453324-32-6
• MW: 378.3
• Purity: 99.75% (May vary between batches)
• Formula: C₁₈H₂₁Cl₂N₅
• SMILES: Cl.NC1(Cc2ccc(Cl)cc2)CCN(CC1)c1ncnc2[nH]ccc12
• Target: Autophagy,PKA,mTOR,Akt,Apoptosis
• Solubility: DMSO:55 mg/mL (145.39 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.29 mM)

Bioactivity

• Target IC50:
  Akt2:6 nM|PKA:168 nM|p70 S6K:120 nM
• In Vivo:
  CCT128930 hydrochloride shows antitumor activities in U87MG and BT474 human breast cancer xenografts.
• In Vitro:
  In U87MG human glioblastoma cells, CCT128930 hydrochloride(0.1-60 μM; 1 hour) shows an initial induction of AKT phosphorylation at serine 473 up to 20 μM, followed by a decreased in phosphorylation at higher concentrations. CCT128930 (18.9 μM) hydrochloride causes an increase in phosphorylation of pSer473 AKT after 30 minutes, which is sustained for 48 hours. Total AKT protein signal decreases gradually from 8 hours to 48 hours of treatment. The GI50 values of CCT128930 hydrochloride for growth inhibition are 6.3 μM for U87MG human glioblastoma cells, 0.35 μM for LNCaP human prostate cancer cells, and 1.9 μM for PC3 human prostate cancer cells, all of which are PTEN-deficient human tumor cell lines. CCT128930 hydrochloride inhibits direct substrates of AKT (Ser9 GSK3β, pThr246 PRAS40 and pT24 FOXO1/p32 FOXO3a) at ≥5 μM, and the downstream target, pSer235/236 S6RP at ≥10 μM, with generally constant levels of the respective total proteins and GAPDH.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PTEN, selective, Protein kinase B, PKB, PKA, phosphorylation, U87MG, Akt2, Akt, BT474, Apoptosis, Autophagy, arrest, cell, breast cancer, CCT128930, CCT 128930, CCT 128930 Hydrochloride, CCT-128930, CCT128930 hydrochloride, CCT128930 Hydrochloride, CCT-128930 Hydrochloride, CCT-128930 hydrochloride, CCT128930 hydrochloride(885499-61-6 Free base), DNA damage, cycle, inhibit, p70S6K, glioblastoma, growth, Inhibitor

Compound Identifiers

PubChem CID

146013807