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666-15 

Cat. No.: HY-101120 Purity: 99.63%
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666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

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

666-15 Chemical Structure

666-15 Chemical Structure

CAS No. : 1433286-70-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 213 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Estimated Time of Arrival: December 31
25 mg USD 552 In-stock
Estimated Time of Arrival: December 31
50 mg USD 996 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

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Description

666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model[1][2].

IC50 & Target

IC50: 81 nM (CREB)[1]

In Vitro

666-15 (73 nM; for 12 hours) significantly blocks the effects caused by MSN overexpression, including cell proliferation, invasion, soft agar colony formation ability, and the expression of CREB downstream genes. 666-15 inhibits MSN overexpression-induced CREB phosphorylation[2].
666-15 (1μM; pretreated 2 hour) effectively inhibits PE-induced CREB phosphorylation. 666-15 significantly decreases the protein expression of ANP and β-MHC and inhibits the activation of ER stress, including the expression of GRP78, CHOP, ATF6, and the phosphorylation of IRE1 in PE + siRNA + 666-15 group and PE + si-CTRP3 + 666-15 group[3].
666-15 potently inhibits cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 is also found to be a rather weak inhibitor of CREB-CBP interaction with IC50 of 18.27 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction. 666-15 is very potent in inhibiting CREB’s transcription activity. 666-15 also inhibits endogenous CREB target gene expression, the transcript level of nuclear receptor related 1 protein (Nurr1/NR4A2)[1].

Cell Proliferation Assay[2]

Cell Line: CTRL or MSN-overexpressing MDA-MB-231 cells
Concentration: 73 nM
Incubation Time: For 12hours
Result: Significantly blocked the cell proliferation caused by MSN overexpression.

Western Blot Analysis[3]

Cell Line: NRCMs
Concentration: 1 μM
Incubation Time: 2 hour (pretreated)
Result: Effectively inhibited PE-induced CREB phosphorylation.
In Vivo

666-15 (10 mg/kg; IP; once a week; for 11 weeks) alone can play a good role in inhibiting the growth of breast cancer, and the combination with RP-56976 (DOC) shows a better effect[2].

Animal Model: 1-month-old female nude mice with MDA-MB-231 or T47D cells[2]
Dosage: 10 mg/kg
Administration: IP; once a week; for 11 weeks
Result: Played a good role in inhibiting the growth of breast cancer.
Molecular Weight

620.52

Formula

C₃₃H₃₁Cl₂N₃O₅

CAS No.

1433286-70-4

SMILES

O=C(NC1=CC=C(Cl)C=C1O)C2=CC3=CC=CC=C3C=C2OCCNC(C4=C(OCCCN)C=C(C=CC=C5)C5=C4)=O.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (48.35 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6116 mL 8.0578 mL 16.1155 mL
5 mM 0.3223 mL 1.6116 mL 3.2231 mL
10 mM 0.1612 mL 0.8058 mL 1.6116 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.63%

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Keywords:

666-15Epigenetic Reader DomainCREBbreastcancerInhibitorinhibitorinhibit

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666-15
Cat. No.:
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