2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. VPC-14228

VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer[2].

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VPC-14228

VPC-14228 構造式

CAS 番号 : 19983-28-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 在庫あり
Solution
10 mM * 1 mL in DMSO USD 121 在庫あり
Solid
5 mg $110 在庫あり
10 mg $180 在庫あり
25 mg $380 在庫あり
50 mg $600 在庫あり
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Based on 1 publication(s) in Google Scholar

VPC-14228 関連抗体

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製品説明

VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer[1][2].

Cellular Effect
Cell Line Type Value Description References
LNCaP IC50
0.28 μM
Compound: 6
Inhibition of androgen receptor in human LNCaP cells assessed as inhibition of prostate-specific antigen secretion into media after 3 days
Inhibition of androgen receptor in human LNCaP cells assessed as inhibition of prostate-specific antigen secretion into media after 3 days
[PMID: 25062331]
LNCaP IC50
0.33 μM
Compound: 6
Inhibition of androgen receptor transcriptional activity in human LNCaP cells after 3 days by eGFP assay
Inhibition of androgen receptor transcriptional activity in human LNCaP cells after 3 days by eGFP assay
[PMID: 25062331]
体外実験

VPC-14228 inhibits hAR transcriptional activity in PC3 cells by targeting AR-DBD, with IC50s of 2.36 μM (hAR-WT), 3.70 μM (hAR-Y594A), and 3.70 μM (hAR-Q592A) for hAR[1].
VPC-14228 (25 μM; 6 h) did not induce apoptosis or affect AR protein expression[1].
VPC-14228 may degrade AR-V7 in 22Rv1 cells via VHL-like PROTACs, but has no effect at 10 μM concentration[2].

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

VPC-14228 関連抗体

Real Time qPCR[1]

Cell Line: PC3 (human prostate cancer cells)
Concentration: 0.01-100 μM
Incubation Time: 24 h
Result: Dose-dependently inhibited AR transcriptional activity in PC3 cells transfected with full-length AR, as measured by luciferase reporter assay, and no significant changes in AR protein levels[1].

Western Blot Analysis[2]

Cell Line: 22Rv1 (human castration-resistant prostate cancer cells)
Concentration: 1-10 μM
Incubation Time: 24 h
Result: Did not induce degradation of AR-V7 in 22Rv1 cells, with a DC50>10 μM.
分子量

246.33

分子式

C13H14N2OS
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

N1(C2=NC(C3=CC=CC=C3)=CS2)CCOCC1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (405.96 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 4.0596 mL 20.2980 mL 40.5959 mL
5 mM 0.8119 mL 4.0596 mL 8.1192 mL
10 mM 0.4060 mL 2.0298 mL 4.0596 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.

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一般には略語で表示されます：C1V1 = C2V2

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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 (10.15 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.15 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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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.
純度とドキュメンテーション
参考文献

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 4.0596 mL 20.2980 mL 40.5959 mL 101.4899 mL
5 mM 0.8119 mL 4.0596 mL 8.1192 mL 20.2980 mL
10 mM 0.4060 mL 2.0298 mL 4.0596 mL 10.1490 mL
15 mM 0.2706 mL 1.3532 mL 2.7064 mL 6.7660 mL
20 mM 0.2030 mL 1.0149 mL 2.0298 mL 5.0745 mL
25 mM 0.1624 mL 0.8119 mL 1.6238 mL 4.0596 mL
30 mM 0.1353 mL 0.6766 mL 1.3532 mL 3.3830 mL
40 mM 0.1015 mL 0.5074 mL 1.0149 mL 2.5372 mL
50 mM 0.0812 mL 0.4060 mL 0.8119 mL 2.0298 mL
60 mM 0.0677 mL 0.3383 mL 0.6766 mL 1.6915 mL
80 mM 0.0507 mL 0.2537 mL 0.5074 mL 1.2686 mL
100 mM 0.0406 mL 0.2030 mL 0.4060 mL 1.0149 mL
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VPC-14228 Related Classifications

  • Molarity Calculator

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The molarity calculator equation

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

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

VPC-1422819983-28-9VPC14228VPC 14228Androgen ReceptorARDBDtranscriptionalprostate cancerInhibitorinhibitorinhibit

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製品番号:
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