TPOP146

Name: TPOP146
Brand: MedChemExpress
SKU: HY-100697
Rating: 5.0 (4 reviews)

Cat. No.: HY-100697 Purity: 98.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K_d values of 134 nM and 5.02 μM for CBP and BRD4.

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

TPOP146 Chemical Structure

CAS No. : 2018300-62-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 111	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 111	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 105	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

3 Publications Citing Use of MCE TPOP146

: TPOP146 purchased from MedChemExpress. Usage Cited in: EMBO Rep. 2020 Mar 4;21(3):e48328. [Abstract]; Inhibiting acetyltransferases CBP/P300 by TPOP146 (134 nM) or PCAF by L-45 (126 nM) for 24 h did not significantly decrease the K49-acetylated b-cat level in Tau-overexpressing N2a cells (n = 3 biological replicates each group)

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K_d values of 134 nM and 5.02 μM for CBP and BRD4.

IC₅₀ & Target

CBP/p300

In Vitro

Exposure to 1 μM TPOP146 results in a significant decrease of recovery half-life that is comparable to the construct that contained the bromodomain inactivating mutation N1168F, demonstrating that TPOP146 targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments^[1].

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

Molecular Weight

481.58

Formula

C₂₇H₃₅N₃O₅

CAS No.

2018300-62-2

Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(OC)=CC(C2=CC(C(N[C@H]3CCCN(C)C3)=O)=C(OCCN(C(CC)=O)C4)C4=C2)=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 : 21.43 mg/mL (44.50 mM; ultrasonic and warming and heat to 60°C; 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	2.0765 mL	10.3825 mL	20.7650 mL
5 mM	0.4153 mL	2.0765 mL	4.1530 mL
10 mM	0.2076 mL	1.0382 mL	2.0765 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: 2.14 mg/mL (4.44 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.14 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.4 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: 2.14 mg/mL (4.44 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.14 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.4 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2.14 mg/mL (4.44 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.14 mg/mL. 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 (21.4 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)

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

Purity: 98.98%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (255 KB) LCMS (268 KB)

Handling Instructions (2659 KB)

References

[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912. [Content Brief]

Kinase Assay
^[1]

Proteins are buffered in 10 mM HEPES, pH 7.5, 500 mM NaCl and assayed in a 96-well plate at a final concentration of 2 μM in 20 μL volume. Compounds (TPOP146) are added at a final concentration of 10 μM. SYPRO Orange (Molecular Probes) is added as a fluorescence probe at a dilution of 1:1000. Excitation and emission filters for the SYPRO Orange dye are set to 465 and 590 nm, respectively. The temperature is raised with a step of 3°C per minute from 25 to 96°C, and fluorescence readings are taken at each interval^[1].

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

References

[1]. Popp TA, et al. Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors. J Med Chem. 2016 Oct 13;59(19):8889-8912. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0765 mL	10.3825 mL	20.7650 mL	51.9125 mL
	5 mM	0.4153 mL	2.0765 mL	4.1530 mL	10.3825 mL
	10 mM	0.2076 mL	1.0382 mL	2.0765 mL	5.1912 mL
	15 mM	0.1384 mL	0.6922 mL	1.3843 mL	3.4608 mL
	20 mM	0.1038 mL	0.5191 mL	1.0382 mL	2.5956 mL
	25 mM	0.0831 mL	0.4153 mL	0.8306 mL	2.0765 mL
	30 mM	0.0692 mL	0.3461 mL	0.6922 mL	1.7304 mL
	40 mM	0.0519 mL	0.2596 mL	0.5191 mL	1.2978 mL

TPOP146 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:

TPOP1462018300-62-2TPOP 146TPOP-146Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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TPOP146

Customer Review

TPOP146 Related Antibodies

3 Publications Citing Use of MCE TPOP146

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•Related Screening Libraries:

•Related Small Molecules:

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View All Histone Acetyltransferase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

TPOP146 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

TPOP146 Related Classifications

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