PeptideDB

DC-BPi-11 hydrochloride

DC-BPi-11 hydrochloride

CAS No.:

DC-BPi-11HCl is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698
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DC-BPi-11 HCl is an inhibitor (blocker/antagonist) of bromodomain PHD finger transcription factor (BPTF) with IC50 of 698 nM. DC-BPi-11 HCl has a significant inhibitory effect on leukemia cell proliferation/growth.

Physicochemical Properties


Molecular Formula C20H24CLN5O2S
Molecular Weight 433.95
Related CAS # DC-BPi-11;2758411-61-7
Appearance Off-white to light yellow solid powder
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets 698 nM (BPTF)[1]
ln Vitro In human leukemia MV-4-11 cells, DC-BPi-11 hydrochloride (0.1 nM-1 μM; 24 h) suppresses BPTF with an EC50 of 120 nM[1]. Human leukemia MV-4-11 cells' ability to proliferate is greatly inhibited by DC-BPi-11 hydrochloride (0.01 μM-100 μM; 24 h) (IC50=0.89 μM), and it also lowers the expression of downstream oncogenes [1] at 2.5 ~ 20 μM; 24 h. Dose-dependently, DC-BPi-11 hydrochloride (0.6–50 μM; 24 h) lowers the levels of c-Myc protein [1]. The hydrochloride of DC-BPi-11 is harmless and does not affect normal cells much [1].
References

[1]. Discovery of High-Affinity Inhibitors of the BPTF Bromodomain. J Med Chem. 2021 Aug 26;64(16):12075-12088.


Solubility Data


Solubility (In Vitro) DMSO :~10 mg/mL (~23.04 mM)
Solubility (In Vivo) Solubility in Formulation 1: ≥ 1 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 1 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3044 mL 11.5221 mL 23.0441 mL
5 mM 0.4609 mL 2.3044 mL 4.6088 mL
10 mM 0.2304 mL 1.1522 mL 2.3044 mL
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.