Art. -Nr.: HY-19553

LP99

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

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Reinheit: 99.18%
CAS. Nr.: 1808951-93-0
Formel: C₂₆H₃₀ClN₃O₄S
Molecular Weight:516.05

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LP99 Chemical Structure

CAS. Nr.: 1808951-93-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Kd: 99 nM (BRD9)^[1]

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

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	5.028 μM Compound: Chemical probe: LP99	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth for 7 days by cell titre glo assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth for 7 days by cell titre glo assay	[PMID: 27376689]
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]
Jurkat	GI₅₀	10.51 μM Compound: Chemical probe: LP99	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth for 7 days by cell titre glo assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth for 7 days by cell titre glo assay	[PMID: 27376689]
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.

Chemical Information

CAS. Nr. 1808951-93-0
Appearance Solid
Molecular Weight 516.05
Formel C₂₆H₃₀ClN₃O₄S
Color White to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9378 mL

9.6890 mL

19.3780 mL

5 mM

0.3876 mL

1.9378 mL

3.8756 mL

10 mM

0.1938 mL

0.9689 mL

1.9378 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Clark PG, et al. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LP99

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Histone Modification Research Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LP99 Related Classifications

HY-19553 Related Classifications