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Chemical Structure| 2453324-32-6 Chemical Structure| 2453324-32-6

Structure of CCT128930 HCl
CAS No.: 2453324-32-6

Chemical Structure| 2453324-32-6

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CCT128930 is a potent ATP-competitive, selective Akt2 inhibitor with an IC50 of 6 nM and > 28-fold selectivity for Akt2 than the closely related PKA kinase.

Synonyms: CCT128930 hydrochloride

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Product Details of CCT128930 HCl

CAS No. :2453324-32-6
Formula : C18H21Cl2N5
M.W : 378.30
SMILES Code : NC1(CC2=CC=C(Cl)C=C2)CCN(C3=C4C(NC=C4)=NC=N3)CC1.[H]Cl
Synonyms :
CCT128930 hydrochloride
MDL No. :MFCD32667039
InChI Key :OFLOSUNRPFWODP-UHFFFAOYSA-N
Pubchem ID :146013807

Safety of CCT128930 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of CCT128930 HCl

PI3K-AKT

Isoform Comparison

Biological Activity

Description
CCT128930 hydrochloride is a potent and selective AKT inhibitor, with an IC50 of 6 nM. It exhibits 28-fold selectivity against the closely related PKA kinase, with an IC50 of 168 nM, and 20-fold selectivity over p70S6K, with an IC50 of 120 nM. This selectivity is achieved through targeting Met282 of AKT (Met173 of PKA-AKT chimera). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy, demonstrating significant antitumor activity[1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
MG-63 cells 10 nM 1 hour Inhibited Wnt5a/ROR2-mediated cell migration Cancer Cell Int. 2017 Nov 29;17:112.
neonatal mouse cardiomyocytes (NMCs) 5 μM 4 h To investigate the role of Akt2 in H2-mediated protection against hypoxia/reoxygenation injury in cardiomyocytes. Results showed that CCT128930 (Akt2 selective inhibitor) did not significantly affect the protective effects of H2. Sci Rep. 2017 Nov 1;7(1):14871
SKOV3 cells 3.33 μM and 10 μM 24 h Inhibition of pS6 (S240/S244) and pS6 (S235/S236) expression, enhancing the effect of paclitaxel in reducing cancer cell viability PLoS One. 2016 May 5;11(5):e0155052
HeyA8 cells 3.33 μM and 10 μM 24 h Inhibition of pS6 (S240/S244) and pS6 (S235/S236) expression, enhancing the effect of paclitaxel in reducing cancer cell viability PLoS One. 2016 May 5;11(5):e0155052
HEK293T cells 10 μM To study the effect of CCT128930 on TRPM3 and TRPM8 channels Cell Rep. 2024 Apr 23;43(4):114108
HEK293T cells 10 μM To study the effect of CCT128930 on TRPM6 channels Cell Rep. 2024 Apr 23;43(4):114108
HEK293T cells 10 μM To study the inhibitory effect of CCT128930 on TRPM7 channels Cell Rep. 2024 Apr 23;43(4):114108
PC3 and LNCaP human prostate cancer cells 3 or 10 μM 1 h To evaluate the effect of CCT128930 on AKT and its downstream proteins in different cell lines. Results showed that CCT128930 significantly inhibited the phosphorylation of GSK3β and S6RP in PTEN-null PC3 and LNCaP cells. Mol Cancer Ther. 2011 Feb;10(2):360-71
U87MG human glioblastoma cells 18.9 μM 30 min to 48 h To evaluate the time-dependent effect of CCT128930 on AKT activity. Results showed that CCT128930 induced phosphorylation of AKT Ser473 within 30 min, which was sustained for 48 h. Meanwhile, CCT128930 significantly inhibited the phosphorylation of GSK3β, PRAS40, FOXO3a, and S6RP. Mol Cancer Ther. 2011 Feb;10(2):360-71
U87MG human glioblastoma cells 5-20 μM 1 h To evaluate the effect of CCT128930 on the phosphorylation of AKT and its downstream proteins. Results showed that CCT128930 significantly inhibited the phosphorylation of direct and indirect targets of AKT (e.g., GSK3β, S6RP, FOXO1, and PRAS40) at concentrations of 5-20 μM. Mol Cancer Ther. 2011 Feb;10(2):360-71

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Myocardial ischemia/reperfusion injury model Intravenous injection 50 mg/kg Once, 1 hour before reperfusion To investigate the role of Akt2 in HCH-induced cardioprotection against myocardial I/R injury. Results showed that CCT128930 treatment did not significantly affect the cardioprotective effects of HCH. Sci Rep. 2017 Nov 1;7(1):14871

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.64mL

0.53mL

0.26mL

13.22mL

2.64mL

1.32mL

26.43mL

5.29mL

2.64mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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