2. Epigenetics
  3. Epigenetic Reader Domain
  4. Y06036

Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.

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Y06036 Chemical Structure

Y06036 Chemical Structure

CAS No. : 1832671-96-1

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Based on 1 publication(s) in Google Scholar

Y06036 Related Antibodies

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Description

Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM[1]. Antitumor activity[1].

IC50 & Target[1]

BRD4(1)

82 nM (Kd)

In Vitro

Y06036 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC50: 0.29-2.6 μΜ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06036 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels[1].

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

Y06036 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells
Concentration: 0.001-100 μM
Incubation Time: 96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP
Result: Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 1.06, 2.62, 1.50, 0.63 μM, respectively.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 1,2,4,8, and 16 μM
Incubation Time: 48 hours
Result: Resulted in significant down-regulation of both AR-fl and AR variants levels
In Vivo

Y06036 (50 mg/kg, i.p. injection, 5 times per week, 25 days) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06036 is well tolerated in the treated mice, based on the weight of the animal body and their general behavior[1].

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

Animal Model: Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) with C4-2B mouse xenograft model[1]
Dosage: 50 mg/kg, 100 μL
Administration: Intraperitoneal (i.p.) injection, 5 times per week, 25 days
Result: Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 70%.
Molecular Weight

427.27

Formula

C16H15BrN2O5S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

BrC1=CC(S(=O)(NC2=C(OC)C=C(ON=C3C)C3=C2)=O)=C(OC)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 130 mg/mL (304.26 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 2.3404 mL 11.7022 mL 23.4044 mL
5 mM 0.4681 mL 2.3404 mL 4.6809 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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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: ≥ 2.17 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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% Corn Oil

    Solubility: ≥ 2.17 mg/mL (5.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3404 mL 11.7022 mL 23.4044 mL 58.5110 mL
5 mM 0.4681 mL 2.3404 mL 4.6809 mL 11.7022 mL
10 mM 0.2340 mL 1.1702 mL 2.3404 mL 5.8511 mL
15 mM 0.1560 mL 0.7801 mL 1.5603 mL 3.9007 mL
20 mM 0.1170 mL 0.5851 mL 1.1702 mL 2.9256 mL
25 mM 0.0936 mL 0.4681 mL 0.9362 mL 2.3404 mL
30 mM 0.0780 mL 0.3901 mL 0.7801 mL 1.9504 mL
40 mM 0.0585 mL 0.2926 mL 0.5851 mL 1.4628 mL
50 mM 0.0468 mL 0.2340 mL 0.4681 mL 1.1702 mL
60 mM 0.0390 mL 0.1950 mL 0.3901 mL 0.9752 mL
80 mM 0.0293 mL 0.1463 mL 0.2926 mL 0.7314 mL
100 mM 0.0234 mL 0.1170 mL 0.2340 mL 0.5851 mL
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Y06036 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:

Y060361832671-96-1Y 06036Y-06036Epigenetic Reader DomainInhibitorinhibitorinhibit

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