1. Cell Cycle/DNA Damage
  2. PERK
    Eukaryotic Initiation Factor (eIF)

CCT020312 

Cat. No.: HY-119240 Purity: 98.56%
Handling Instructions

CCT020312 is capable of delivering potent, and eukaryotic initiation factor 2-alpha kinase 3 (EIF2AK3) selective, proliferation control and also is an activator of RNA-like endoplasmic reticulum kinase (PERK).

For research use only. We do not sell to patients.

CCT020312 Chemical Structure

CCT020312 Chemical Structure

CAS No. : 324759-76-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 229 In-stock
Estimated Time of Arrival: December 31
5 mg USD 160 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CCT020312 is capable of delivering potent, and eukaryotic initiation factor 2-alpha kinase 3 (EIF2AK3) selective, proliferation control and also is an activator of RNA-like endoplasmic reticulum kinase (PERK).

IC50 & Target

EIF2AK3[1].
PERK[2].

In Vitro

Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM. CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis. Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells[1].

In Vivo

Treatment of mice with the PERK activator CCT020312 leads to increased levels of phosphorylated PERK and NRF2 in brain homogenates[2].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (192.19 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5375 mL 7.6876 mL 15.3752 mL
5 mM 0.3075 mL 1.5375 mL 3.0750 mL
10 mM 0.1538 mL 0.7688 mL 1.5375 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (3.20 mM); Suspended solution; Need ultrasonic

References
Animal Administration
[2]

Mice[2]
For the short-term target engagement trial with ascending doses, 15-week-old wild-type mice (n=3 per group) are treated on three consecutive days with intraperitoneal (i.p.) injections of either 1, 2, or 5 mg/kg/day of CCT020312. For the long-term target engagement trial, 9-week-old wild-type mice (n=3 per group) are treated i.p. for 6 weeks with either 2 mg/kg/day of CCT020312 or equivalent volumes of saline. For immunoblotting of tau species in mouse brains, 17-week-old P301S tau transgenic mice (n=3) are i.p. injected with 2 mg/kg/day of CCT020312 for 6 weeks. For the efficacy trial on behavioral deficits at the early disease stage, 9-week-old P301S tau transgenic mice (n=8 per group) and wild-type mice (n=9 per group) receive i.p. injections of 2 mg/kg/day CCT020312 or equivalent volumes of saline for 6 weeks[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

650.40

Formula

C₃₁H₃₀Br₂N₄O₂

CAS No.

324759-76-4

SMILES

O=C1NC2=C(C(C3=CC=CC=C3)=C1C4=NN(C(C4)C5=CC=C(C=C5)Br)C(CCN(CC)CC)=O)C=C(C=C2)Br

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CCT020312
Cat. No.:
HY-119240
Quantity:

CCT020312

Cat. No.: HY-119240