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MedKoo Cat#: 407280 | Name: LP99
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

LP99 is the First Selective BRD7/9 Bromodomain Inhibitor. LP99 is a potent binder to BRD9 with a KD = 99 nM as shown by ITC and was found to bind to the family member BRD7 with 10 fold lower affinity. LP99 was shown to inhibit the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. Moreover, LP99 was used to demonstrate that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion.

Chemical Structure

LP99
LP99
CAS#1808951-93-0

Theoretical Analysis

MedKoo Cat#: 407280

Name: LP99

CAS#: 1808951-93-0

Chemical Formula: C26H30ClN3O4S

Exact Mass: 515.1646

Molecular Weight: 516.05

Elemental Analysis: C, 60.51; H, 5.86; Cl, 6.87; N, 8.14; O, 12.40; S, 6.21

Price and Availability

Size Price Availability Quantity
5mg USD 550.00 2 Weeks
50mg USD 1,250.00 2 Weeks
100mg USD 1,950.00 2 Weeks
1g USD 5,650.00 2 Weeks
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Related CAS #
1808951-93-0 1808948-28-8
Synonym
LP99; LP-99; LP 99.
IUPAC/Chemical Name
N-((2R,3S)-2-(4-chlorophenyl)-1-(1,4-dimethyl-2-oxo-1,2-dihydroquinolin-7-yl)-6-oxopiperidin-3-yl)-2-methylpropane-1-sulfonamide
InChi Key
LVDRREOUMKACNJ-BKMJKUGQSA-N
InChi Code
InChI=1S/C26H30ClN3O4S/c1-16(2)15-35(33,34)28-22-11-12-24(31)30(26(22)18-5-7-19(27)8-6-18)20-9-10-21-17(3)13-25(32)29(4)23(21)14-20/h5-10,13-14,16,22,26,28H,11-12,15H2,1-4H3/t22-,26+/m0/s1
SMILES Code
O=C(CC[C@H](NS(CC(C)C)(=O)=O)[C@H]1C2=CC=C(Cl)C=C2)N1C3=CC=C4C(N(C)C(C=C4C)=O)=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#C22M03C14
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9.
In vitro activity:
The quinolone-fused lactam LP99 is now reported as the first potent and selective inhibitor of the BRD7 and BRD9 bromodomains. This epigenetic probe was shown to inhibit the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. Moreover, LP99 was used to demonstrate that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion. Reference: Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. https://pubmed.ncbi.nlm.nih.gov/25864491/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 20.0 38.76
DMSO 35.0 67.82
Ethanol 20.0 38.76
Ethanol:PBS (pH 7.2) (1:9) 0.1 0.19
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 516.05 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. doi: 10.1002/anie.201501394. Epub 2015 Apr 13. PMID: 25864491; PMCID: PMC4449114.
In vitro protocol:
Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. doi: 10.1002/anie.201501394. Epub 2015 Apr 13. PMID: 25864491; PMCID: PMC4449114.
In vivo protocol:
TBD
1: Clark PG, Vieira LC, Tallant C, Fedorov O, Singleton DC, Rogers CM, Monteiro OP, Bennett JM, Baronio R, Müller S, Daniels DL, Méndez J, Knapp S, Brennan PE, Dixon DJ. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21. doi: 10.1002/anie.201501394. Epub 2015 Apr 13. PubMed PMID: 25864491; PubMed Central PMCID: PMC4449114.