In vitro: 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). In vivo: Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice. The tumor growth in the mice treated with 666-15 is efficaciously inhibited with complete tumor stasis. During the same period, the tumor volume in the vehicle-treated group is more than tripled. The body weights of 666-15-treated animals and vehicle-treated ones are indistinguishable from each other during the entire treatment period.
Bone Joint Res. 2024 Jan;2;13(1):4-18.
The CREB1 inhibitor 666-15 maintains cartilage homeostasis and mitigates osteoarthritis progression
666-15 purchased from AbMole
Neurourol Urodyn. 2020 Apr 24.
β-Adrenoceptors Regulate Matrix Metalloproteinase Expression in Human Urothelial Cells Under Hydrostatic Pressure.
666-15 purchased from AbMole
Life Sci. 2019 Dec 1;238:116979.
Effects of progesterone on glucose uptake in neurons of Alzheimer's disease animals and cell models.
666-15 purchased from AbMole
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Source | Neurourol Urodyn. 2020 Apr. Figure 4. 666‐15 (Abmole Bioscience, Houston, TX, USA) |
| Method | tested agonists and antagonists | |
| Cell Lines | HUCs | |
| Concentrations | 1×10^-9, 1×10^-8, 1×10^-7, 1×10^-6, and 1×10^-5 mol/L | |
| Incubation Time | 6h | |
| Results | Doses of 1×10^-9‐10^-6 mol/L for Formoterol, ICI 118551, BRL 37344, SR59230A, H89, and 666-15 did not significantly affect the viability of HUCs after 6hours. |
 |
Source | Sci Rep (2016). Figure 2. 666-15 |
| Method | The luciferase activity assay | |
| Cell Lines | HEK 293T cells | |
| Concentrations | 5.0 μM | |
| Incubation Time | 5–7 h | |
| Results | Together with previous results of 666-15’s effect on other transcription factors22, these data demonstrate that 666-15 had little or no effect on MLL, c-Myb, YAP/TEAD or p53 driven transcription, and only affected NF-κB and SRF driven transcription at concentrations ~100 fold higher than those required for CREB driven transcription. |
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231 and MDA-MB-468 cells |
| Preparation method | Cells are plated into 96-well plates and the cells are allowed to attach to the bottom of the plates overnight. Then the cells are treated with different concentrations of different drugs (666-15) for 72 h. The media are removed, and MTT reagent in complete tissue culture media is added to each well and incubated at 37 °C for 3 h. The incubation media are removed and 100 μL of DMSO is added to each well. The absorbance of the formed purple formazan solution is read at 570 nm using a plate reader. |
| Concentrations | 80 nM |
| Incubation time | 72 h. |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c nude mouse |
| Formulation | 1% N-methylpyrrolidone (NMP), 5% Tween-80 in water |
| Dosages | 10 mg/kg |
| Administration | i.v. |
| Molecular Weight | 620.52 |
| Formula | C33H31Cl2N3O5 |
| CAS Number | 1433286-70-4 |
| Solubility (25°C) | 30 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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