[CAS NO. 1808951-93-0] LP99

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PRODUCTS SPECIFICATIONS [1808951-93-0]

Catalog

HY-19553

Brand

MCE

CAS

1808951-93-0

DESCRIPTION [1808951-93-0]

Overview

MDL	MFCD28969655
Molecular Weight	516.05
Molecular Formula	C26H30ClN3O4S
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

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

Summary

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 ^[1] .

IC50 & Target

Kd: 99 nM (BRD9) ^[1]

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 IC ₅₀ 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] .

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

Appearance

Solid

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)

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
10 mM	0.1938 mL	0.9689 mL	1.9378 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.

References

[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.