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CCT128930 hydrochloride

Catalog No. T6303L CAS 2453324-32-6

Synonyms: 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).

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CCT128930 hydrochloride Chemical Structure

CCT128930 hydrochloride, CAS 2453324-32-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 54.00
2 mg	In stock	$ 77.00
5 mg	In stock	$ 118.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 395.00
50 mg	In stock	$ 592.00
100 mg	In stock	$ 845.00
1 mL * 10 mM (in DMSO)	In stock	$ 143.00

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Purity: 98.55%

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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	p70 S6K:120 nM, PKA:168 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].

Synonyms	CCT128930 hydrochloride(885499-61-6 Free base)
Molecular Weight	378.3
Formula	C18H21Cl2N5
CAS No.	2453324-32-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (145.39 mM)

References and Literature

1. Wang FZ, et al. CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. Biochimie. 2014;103:118-125. 2. Yap TA et al. Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Autophagy Compound Library Cytoskeletal Signaling Pathway Compound Library PI3K-AKT-mTOR Compound Library Bioactive Compound Library Anti-Lung Cancer Compound Library Pyroptosis Compound Library

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Keywords

CCT128930 hydrochloride 2453324-32-6 Apoptosis Autophagy Cytoskeletal Signaling PI3K/Akt/mTOR signaling Tyrosine Kinase/Adaptors Akt PKA mTOR U87MG cell CCT128930 hydrochloride(885499-61-6 Free base) phosphorylation selective DNA damage CCT128930 glioblastoma arrest CCT 128930 Hydrochloride breast cancer Inhibitor BT474 PTEN growth CCT-128930 Hydrochloride CCT128930 Hydrochloride PKB inhibit CCT 128930 CCT-128930 hydrochloride cycle CCT-128930 Protein kinase B inhibitor

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