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666-15

Catalog No. T5318   CAS 1433286-70-4
Synonyms: CREB inhibitor

666-15 (CREB inhibitor) is a potent and selective CREB inhibitor (IC50: 81 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
666-15 Chemical Structure
666-15, CAS 1433286-70-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 52.00
5 mg In stock $ 113.00
10 mg In stock $ 178.00
25 mg In stock $ 363.00
50 mg In stock $ 578.00
100 mg In stock $ 833.00
1 mL * 10 mM (in DMSO) In stock $ 156.00
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Purity: 99.77%
Purity: 99.47%
Purity: 99.41%
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Biological Description
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Description 666-15 (CREB inhibitor) is a potent and selective CREB inhibitor (IC50: 81 nM).
Targets&IC50 CREB:81 nM (in HEK 293T cells)
In vitro 666-15 is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM). 666-15 also potently inhibited cancer cell growth without harming normal cells [1]. Isoproterenol (ISO) induced cardiac hypertrophy. The rate of ROS production, CREB phosphorylation, and miR-132 expression increased after the addition of ISO. Upregulation of miR-132 was blocked by the specific inhibitor of CREB transcription, 666-15 [2].
In vivo In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppressed the tumor growth without overt toxicity [1]. 666-15 was found to be readily bioavailable to achieve pharmacologically relevant concentrations for CREB inhibition. The mice treated with 666-15 showed no evidence of changes in body weight, complete blood count, blood chemistry profile, cardiac contractility and tissue histologies from liver, kidney, and heart [3].
Cell Research HEK 293T cells in a 10 cm plate were transfected with pCRE-RLuc (6 μg) with Lipofectamine2000 following the manufacturer's instructions. Three hours after transfection, the cells were collected and replated into 96-well plates at ~10?000 cells/well. The cells were allowed to attach to the bottom of the plates overnight. The cells were then treated with different concentrations of different compounds for 30 min when forskolin (10 μM) was added to each well. The cells were incubated for further 5 h before cell lysis using 1× 30 μL Renilla luciferase lysis buffer. An amount of 5 μL of the lysate was combined with 30 μL of benzyl-coelenterazine solution in PBS (pH 7.4, 10 μg/mL). The protein concentration in each well was determined. The Renilla luciferase activity was normalized to protein content in each well and expressed as relative luciferase unit/μg protein (RLU/μg protein). The IC50 was derived from nonlinear regression analysis of the RLU/μg protein–concentration curve [1].
Animal Research Each 6- to 8-week old BALB/c nude mouse was inoculated subcutaneously at the right flank with MDA-MB-468 cells (5 × 10^6) in 0.1 mL of HBSS with Matrigel (1:1) for tumor development. When the tumor volume reached approximately 100 mm3, the mice were randomized to be treated with either vehicle or 666-15 at 10 mg/kg. 3i was dissolved in 1% N-methylpyrrolidone (NMP), 5% Tween-80 in H2O. The dosing solution was prepared weekly. The mice were treated once a day for 5 consecutive days a week, and the treatment lasted for 5 weeks. During the treatment, the tumor size and body weight were measured 2–3 times a week. The tumors were measured in two dimensions using a digital caliper, and the volume was expressed in mm3 using the formula V = 0.5ab2, where a and b represent the long and short diameters of the tumor, respectively. The tumor volume was normalized to the initial tumor volume at the time of the first treatment [1].
Synonyms CREB inhibitor
Molecular Weight 620.52
Formula C33H31Cl2N3O5
CAS No. 1433286-70-4

Storage

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

Solubility Information

DMSO: 60 mg/mL (96.7 mM)

TargetMolReferences and Literature

1. Xie F, et al. Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. J Med Chem. 2015 Jun 25;58(12):5075-87. 2. Yang C, et al. Inhibition of Necroptosis Rescues SAH-Induced Synaptic Impairments in Hippocampus via CREB-BDNF Pathway. Front Neurosci. 2019 Jan 7;12:1990. 3. Li BX, et al. Systemic Inhibition of CREB is Well-tolerated in vivo. Sci Rep. 2016 Oct 3;6:34513. 4. Zhi Y, Lu C, Zhu G, et al. Positive regulation of the CREB phosphorylation via JNK-dependent pathway prevents antimony-induced neuronal apoptosis in PC12 cell and mice brain[J]. NeuroToxicology. 2020

TargetMolCitations

1. Ding D, Zheng R, Tian Y, et al. Retinoblastoma protein as an intrinsic BRD4 inhibitor modulates small molecule BET inhibitor sensitivity in cancer. Nature Communications. 2022, 13(1): 1-15. 2. Zheng Y, Ding W, Zhang T, et al. Antimony-induced astrocyte activation via mitogen-activated protein kinase activation-dependent CREB phosphorylation. Toxicology Letters. 2021 3. Zou L, Hong D, Li K, et al. Salt-inducible kinase 2 (SIK2) inhibitor ARN-3236 attenuates bleomycin-induced pulmonary fibrosis in mice. BMC Pulmonary Medicine. 2022, 22(1): 1-11 4. Zhi Y, Lu C, Zhu G, et al. Positive regulation of the CREB phosphorylation via JNK-dependent pathway prevents antimony-induced neuronal apoptosis in PC12 cell and mice brain. NeuroToxicology. 2020 Dec;81:101-108

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This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Bioactive Compounds Library Max Inhibitor Library Histone Modification Compound Library NO PAINS Compound Library Anti-Aging Compound Library Endoplasmic Reticulum Stress Compound Library Bioactive Compound Library Anti-Cancer Compound Library Anti-COVID-19 Compound Library

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Keywords

666-15 1433286-70-4 Chromatin/Epigenetic Epigenetic Reader Domain breast cancer CREB 66615 666 15 CREB inhibitor inhibit Inhibitor inhibitor

 

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