2. Epigenetics
  3. Epigenetic Reader Domain
  4. LP99

LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells.

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LP99 Chemical Structure

LP99 Chemical Structure

CAS No. : 1808951-93-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

LP99 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells[1].

IC50 & Target

Kd: 99 nM (BRD9)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
5.1 μM
Compound: LP99
Inhibition of human BRD9 isoform 1 co-expressed with H3 histone family 3A in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
Inhibition of human BRD9 isoform 1 co-expressed with H3 histone family 3A in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
[PMID: 26914985]
HEK293 IC50
6.2 μM
Compound: LP99
Inhibition of human BRD9 isoform 1 co-expressed with H4 histone in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
Inhibition of human BRD9 isoform 1 co-expressed with H4 histone in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
[PMID: 26914985]
HL-60 GI50
5.03 μM
Compound: 18; LP99
Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
[PMID: 33275431]
THP-1 IC50
< 10 μM
Compound: LP99
Inhibition of LPS-stimulated IL-6 secretion in human THP1 cells by ELISA
Inhibition of LPS-stimulated IL-6 secretion in human THP1 cells by ELISA
[PMID: 29170712]
In Vitro

LP99 disrupts BRD9 interactions with chromatin at a concentration of 0.8 μM. BRD7- and BRD9-NanoLuc luciferase fusion proteins and fluorescently labelled histone H3.3- and H4-HaloTag fusions were expressed in HEK293 cells. The addition of LP99 decreased BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose-dependent manner, with cellular IC50 values in the low micromolar range for both histone. Cytotoxicity tests in U2OS cells for 24 and 72 hours shows the inhibitor to be non-toxic at concentrations of <33 μM. LP99 inhibits IL-6 secretion from THP-1 cells in a dose-dependent manner[1].

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

LP99 Related Antibodies
Molecular Weight

516.05

Formula

C26H30ClN3O4S
CAS No.
Appearance

Solid

SMILES

O=C1N(C2=CC(N(C)C(C=C3C)=O)=C3C=C2)[C@H](C4=CC=C(Cl)C=C4)[C@@H](NS(CC(C)C)(=O)=O)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (96.89 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 1.9378 mL 9.6890 mL 19.3780 mL
5 mM 0.3876 mL 1.9378 mL 3.8756 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (4.84 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(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 1.9378 mL 9.6890 mL 19.3780 mL 48.4449 mL
5 mM 0.3876 mL 1.9378 mL 3.8756 mL 9.6890 mL
10 mM 0.1938 mL 0.9689 mL 1.9378 mL 4.8445 mL
15 mM 0.1292 mL 0.6459 mL 1.2919 mL 3.2297 mL
20 mM 0.0969 mL 0.4844 mL 0.9689 mL 2.4222 mL
25 mM 0.0775 mL 0.3876 mL 0.7751 mL 1.9378 mL
30 mM 0.0646 mL 0.3230 mL 0.6459 mL 1.6148 mL
40 mM 0.0484 mL 0.2422 mL 0.4844 mL 1.2111 mL
50 mM 0.0388 mL 0.1938 mL 0.3876 mL 0.9689 mL
60 mM 0.0323 mL 0.1615 mL 0.3230 mL 0.8074 mL
80 mM 0.0242 mL 0.1211 mL 0.2422 mL 0.6056 mL
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LP99 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:

LP991808951-93-0LP 99LP-99Epigenetic Reader Domainbromodomainepigeneticsorganocatalysisselectiveprobehistonespro-inflammatorycytokinesecretionInhibitorinhibitorinhibit

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