2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. VD/VDR Apoptosis
  4. PS121912

PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer.

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

PS121912 Chemical Structure

PS121912 Chemical Structure

CAS No. : 1529814-60-5

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5 mg USD 180 In-stock
10 mg USD 290 In-stock
25 mg USD 580 In-stock
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Based on 1 publication(s) in Google Scholar

PS121912 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer[1].

Cellular Effect
Cell Line Type Value Description References
HEK-293T IC50
0.59 μM
Compound: PS121912
Inhibition of 1,25(OH)2D3-induced VDR (unknown origin)-mediated CYP24A1 transcription expressed in HEK293T cells after 16 hrs by luciferase reporter gene assay
Inhibition of 1,25(OH)2D3-induced VDR (unknown origin)-mediated CYP24A1 transcription expressed in HEK293T cells after 16 hrs by luciferase reporter gene assay
[PMID: 24799995]
HEK-293T IC50
8.1 μM
Compound: PS121912
Inhibition of 1,25(OH)2D3-induced VDR-LBD (unknown origin)-mediated GAL4-labeled SRC1 transcription expressed in HEK293T cells after 16 hrs by two-hydrid luciferase reporter gene assay
Inhibition of 1,25(OH)2D3-induced VDR-LBD (unknown origin)-mediated GAL4-labeled SRC1 transcription expressed in HEK293T cells after 16 hrs by two-hydrid luciferase reporter gene assay
[PMID: 24799995]
HL-60 EC50
20 μM
Compound: PS121912
Cytotoxicity against human HL60 cells assessed as ATP level after 18 hrs by CellTiter-Glo assay
Cytotoxicity against human HL60 cells assessed as ATP level after 18 hrs by CellTiter-Glo assay
[PMID: 24799995]
HL-60 EC50
20 μM
Compound: PS121912
Cytotoxicity against human HL60 cells assessed as cell viability after 18 hrs by CellTiter-Fluor assay
Cytotoxicity against human HL60 cells assessed as cell viability after 18 hrs by CellTiter-Fluor assay
[PMID: 24799995]
In Vitro

PS121912 behaves like a VDR antagonist at low concentrations but interacts with more targets at higher concentrations leading to apoptosis mediated by caspase 3/7 activation[1].
PS121912 (combined with 1,25-(OH)2D3)reduces the transcription levels of cyclin A and D thus arresting HL-60 cells in the S or G2/M phase[1].

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

PS121912 Related Antibodies

Cell Viability Assay[1]

Cell Line: Cancer cells consisting of DU145 (prostate), Caco2 (colon), HL-60 (monocytes), and SKOV3 (ovary)
Concentration: 0-100 μM
Incubation Time: 18 h
Result: Induced apoptosis in all four cancer cells, with HL-60 cells being the most sensitive.

Cell Proliferation Assay[1]

Cell Line: Four different cancer cell lines (DU145 prostate cancer, Caco2 colon cancer, SKOV3 ovarian cancer and HL-60 monocytes)
Concentration: 0.5, 2 μM
Incubation Time: 5 days
Result: Amplified the growth inhibition of cancer cells caused by 1.25-(OH)2Ds without being antiproliferative by itself at sub-micromolar concentrations.

Apoptosis Analysis[1]

Cell Line: HL-60 cells
Concentration: 500 nM
Incubation Time: 18 h
Result: Reduced expression of HSP60 and Survivin and elevated the levels of pro-apoptotic BIM.

RT-PCR[1]

Cell Line: HL-60 cells
Concentration: 3 μM
Incubation Time: 18 h
Result: Induced the expression of caspase 3 and caspase 7 mRNA levels.
In Vivo

PS121912 shows an acceptable metabolic stability and can inhibit the metabolic enzyme CYP3A4 at higher concentrations in vivo cancer studies[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

410.43

Formula

C24H21F3N2O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC(C1=CC=C(NC(C2=CC=C(OC)C=C2)C3=C(C)NC4=C3C=CC=C4)C=C1)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (243.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4365 mL 12.1823 mL 24.3647 mL
5 mM 0.4873 mL 2.4365 mL 4.8729 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4365 mL 12.1823 mL 24.3647 mL 60.9117 mL
5 mM 0.4873 mL 2.4365 mL 4.8729 mL 12.1823 mL
10 mM 0.2436 mL 1.2182 mL 2.4365 mL 6.0912 mL
15 mM 0.1624 mL 0.8122 mL 1.6243 mL 4.0608 mL
20 mM 0.1218 mL 0.6091 mL 1.2182 mL 3.0456 mL
25 mM 0.0975 mL 0.4873 mL 0.9746 mL 2.4365 mL
30 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0304 mL
40 mM 0.0609 mL 0.3046 mL 0.6091 mL 1.5228 mL
50 mM 0.0487 mL 0.2436 mL 0.4873 mL 1.2182 mL
60 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7614 mL
100 mM 0.0244 mL 0.1218 mL 0.2436 mL 0.6091 mL
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PS121912 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PS1219121529814-60-5PS 121912PS-121912VD/VDRApoptosisVitamin DVitamin D receptorvitamin D receptor (VDR)metabolic stabilitycancerHL-60apoptosisInhibitorinhibitorinhibit

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