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CCT128930 hydrochloride

🥰Excellent
Catalog No. T6303LCas No. 2453324-32-6
Alias CCT128930 hydrochloride(885499-61-6 Free base)

CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).

CCT128930 hydrochloride

CCT128930 hydrochloride

🥰Excellent
Purity: 98.55%
Catalog No. T6303LAlias CCT128930 hydrochloride(885499-61-6 Free base)Cas No. 2453324-32-6
CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).
Pack SizePriceAvailabilityQuantity
1 mg$54In Stock
5 mg$98In Stock
10 mg$159In Stock
25 mg$267In Stock
50 mg$398In Stock
100 mg$582In Stock
1 mL x 10 mM (in DMSO)$118In Stock
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Purity:98.55%
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Product Introduction

Bioactivity
Description
CCT128930 hydrochloride (CCT128930 hydrochloride) is a potent and selective inhibitor of AKT with IC50 of 6 nM. CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50: 168 nM) through the targeting of Met282 of AKT, as well as 20-fold selectivity over p70S6K (IC50: 120 nM).
Targets&IC50
PKA:168 nM, p70 S6K:120 nM, Akt2:6 nM
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[1]. 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[1]. 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[1]. 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[1].
In vivo
CCT128930 hydrochloride shows antitumor activities in U87MG and BT474 human breast cancer xenografts[1].
AliasCCT128930 hydrochloride(885499-61-6 Free base)
Chemical Properties
Molecular Weight378.3
FormulaC18H21Cl2N5
Cas No.2453324-32-6
SmilesCl.NC1(Cc2ccc(Cl)cc2)CCN(CC1)c1ncnc2[nH]ccc12
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 55 mg/mL (145.39 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6434 mL13.2170 mL26.4340 mL132.1702 mL
5 mM0.5287 mL2.6434 mL5.2868 mL26.4340 mL
10 mM0.2643 mL1.3217 mL2.6434 mL13.2170 mL
20 mM0.1322 mL0.6609 mL1.3217 mL6.6085 mL
50 mM0.0529 mL0.2643 mL0.5287 mL2.6434 mL
100 mM0.0264 mL0.1322 mL0.2643 mL1.3217 mL

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