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BiochemicalTargets

Epigenetics

Covalent modifications to DNA or histone proteins with various chemical groups can determine whether genes are turned on or off and can thus influence the production of proteins in a cell. This genetic control without altering DNA sequences is crucial in many normal cellular functions. Aberrant epigenetic alterations are present in myriad disease states. Pharmacological manipulation of the various enzymes involved in epigenetic changes in pathological states is an important new target in drug discovery. Writers (methyl and acetyl transferases) are enzymes capable of modifying nucleotide bases and amino acid residues on histones. Erasers (demethylases and deacetylases) remove these same modifications. Readers (bromodomains) are enzymes capable of recognizing specific epigenetic marks that direct a particular transcriptional outcome.

Bromodomains

GSK6853 | BRPF1 inhibitor

CAS:
1910124-24-1
Catalog Number:
10-4016
Activity:
BRPF1 inhibitor
Chemical Names:
N-[1,3-Dimethyl-6-[(2R)-2-methylpiperazin-1-yl]-2-oxobenzimidazol-5-yl]-2-methoxybenzamide
Molecular Weight:
409.49
Molecular Formula:
C22H27N5O3
Solubility:
Soluble in DMSO (25 mg/ml); ethanol (25 mg/ml)
Physical Properties:
White solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

PFI-3 | Selective Bromodomain family VIII inhibitor

CAS:
1819363-80-8
Catalog Number:
10-4034
Activity:
Selective Bromodomain family VIII inhibitor
Chemical Names:
(2E)-1-(2-Hydroxyphenyl)-3-[(1R,4R)-5-(pyridine-2-yl)-2,5-diazabicyclo{2.2.1]heptan-2-yl]prop-2-en-1-one
Molecular Weight:
321.37
Molecular Formula:
C19H19N3O2
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

JQ1 (+) | BET Bromodomain inhibitor

CAS:
1268524-70-4
Catalog Number:
10-1584
Activity:
BET Bromodomain inhibitor
Chemical Name:
(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester
Molecular Weight:
456.99
Molecular Formula:
C23H25ClN4O2S
Solubility:
Soluble in DMSO (up to 60 mg/ml) or in Ethanol (up to 46 mg/ml).
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
RT
VIEW ALL Bromodomains​ PRODUCTS

Deubiquitinase

Thiolutin | Inhibitor of the DUB PSMD14

CAS:  87-11-6
Catalog Number:
10-2106
Activity:
Inhibitor of the DUB PSMD14
Chemical Names:
N-(4,5-Dihydro-4-methyl-5-oxo-1,2-dithiolo[4,3-b]pyrrol-6-yl)acetamide;
Acetopyrrothin
Molecular Weight:
228.29
Molecular Formula:
C8H8N2O2S2
Solubility:
Soluble in DMSO (up to 15 mg/ml)
Physical Properties:
Yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 3 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
VIEW ALL Deubiquitinase PRODUCTS

DNA methylation

SGI-1027 | DNA methyl transferase inhibitor

CAS:
1020149-73-8
Catalog Number:
10-5488
Activity:
DNA methyl transferase inhibitor
Chemical Names:

N-[4-[(2-Amino-6-methyl-4-pyrimidinyl)amino]phenyl]-4-(4-quinolinylamino)benzamide

Molecular Weight:
461.52
Molecular Formula:
C27H23N7O
Solubility:
Soluble in DMSO (up to 35 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

PF-9366 | Methionine adenosyltransferase 2A inhibitor

CAS:
72882-78-1
Catalog Number:
10-4635
Activity:
Methionine adenosyltransferase 2A inhibitor
Chemical Name:
2-(7-Chloro-5-phenyl)-[1,2,4]triazolo[4,3-a]quinoline-1-yl)-N,N,dimethylethanamine
Molecular Weight:
350.85
Molecular Formula:
C20H19ClN4
Solubility:
Soluble in DMSO (up to 20 mg/ml).
Physical Properties:
Beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT

6-Thioguanine | Anticancer agent / Downregulates DNMT1

CAS:
154-42-7
Catalog Number:
10-1282
Activity:
Anticancer agent / Downregulates DNMT1
Chemical Name:
2-Amino-6-mercaptopurine
Alternate Names:
6-TG; NSC 752, NSC 76504
Molecular Weight:
167.19
Molecular Formula:
C5H5N5S
Solubility:
Soluble in DMF (up to 1.5 mg/ml with warming)
Physical Properties:
Pale yellow solid
Purity:
96% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMF may be stored at -20°C for up to 1 month.
Shipping Code:
RT
VIEW ALL DNA methylation PRODUCTS

DNA demethylation

VIEW ALL DNA demethylation PRODUCTS

Histone acetylation

Acetyl-Coenzyme A 3Li | Acetylation and fatty acid biosynthesis cofactor

CAS:
75520-41-1
Catalog Number:
10-5384
Activity:
Cofactor for cellular metabolism/Acetyl donor
Chemical Name:

Acetyl-CoA

Molecular Weight:
881.42
Molecular Formula:
C23H35Li3N7O17P3S·3H2O
Solubility:
Soluble in water (10 mg/ml)
Physical Properties:
White solid
Purity:
90% (enzymatic)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in water may be stored at -20°C for up to 2 weeks.
Shipping Code:
RT

Remodelin | Acetyltransferase NAT10 inhibitor

CAS:
949912-58-7
Catalog Number:
10-5085
Activity:
Acetyl-transferase NAT10 inhibitor
Chemical Name:
4-[2-(2-Cyclopentylidenehydrazinyl)-4-thiazolyl]-benzonitrile
Molecular Weight:
282.36
Molecular Formula:
C15H14N4S
Solubility:
Soluble in DMSO (up to 40 mg/ml).
Physical Properties:
Pale yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Anacardic Acid | HAT inhibitor

CAS:
16611-84-0
Catalog Number:
10-4015
Activity:
HAT inhibitor
Chemical Name:
2-Hydroxy-6-pentadecylbenzoic acid
Alternate Names:
6-Pentadecylsalicylic acid; 6-PDSA
Molecular Weight:
348.52
Molecular Formula:
C22H36O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to 15 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
VIEW ALL Histone acetylation PRODUCTS

Histone deacetylation

Tenovin-1 | SIRT1/2 inhibitor

CAS:
380315-80-0
Catalog Number:
10-2982
Activity:
SIRT1/2 Inhibitor
Chemical Names:
N-[(4-Acetamidophenyl)carbamothioyl]-4-tert-butylbenzamide
Molecular Weight:
369.48
Molecular Formula:
C20H23N3O2S
Solubility:
Soluble in DMSO (10 mg/ml with warming)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Nicotinamide | SIRT1 inhibitor/essential nutrient

CAS:
98-92-0
Catalog Number:
10-2840
Activity:
SIRT1 inhibitor/essential nutrient
Chemical Names:
Pyridine-3-carboxylic acid amide; Nicotinic acid amide; Niacinamide; Vitamin B3
Molecular Weight:
122.13
Molecular Formula:
C6H6N2O
Solubility:
Soluble in DMSO (50 mg/ml); water (50 ml)
Physical Properties:
White solid
Purity:
>99% HPLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

SRT1720 HCl | SIRT1 activator

CAS:
1001645-58-4
Catalog Number:
10-4628
Activity:
SIRT1 activator
Chemical Names:
N-[2-[3-(Piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]quinoxaline-2-carboxamide hydrochloride; SIRT 1933
Molecular Weight:
506.02
Molecular Formula:
C25H23N7OS·HCl
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
VIEW ALL Histone deacetylation PRODUCTS

Histone demethylation

Deferasirox | Iron Chelator

CAS:
201530-41-8
Catalog Number:
10-4949
Activity:
Iron chelator
Chemical Names:
4-[3,5-bis(2-Hydroxyphenyl)-1,2,4-triazol-1-yl]benzoic acid
Alternate Name:
ICL670
Molecular Weight:
373.36
Molecular Formula:
C21H15N3O4
Solubility:
Soluble in DMSO (10 mg/ml)
Physical Properties:
Off-white to white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT

CPI-455 | Lysine demethylase KDM5 inhibitor

CAS:
1628208-23-0
Catalog Number:
10-4035
Activity:
Lysine demethylase KDM5 inhibitor
Chemical Name:
7-Oxo-5-phenyl-6-propan-2-yl-1H-pyrazolo[1,5-a]pyrimidine-3-carbonitrile
Molecular Weight:
278.32
Molecular Formula:
C16H14N4O
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

GSK2879552 | Potent and selective LSD1 inhibitor

CAS:
1401966-69-5
Catalog Number:
10-4020
Activity:
Potent and selective LSD1 inhibitor
Chemical Name:
4-[[4-[[[(1R,2S)-2-Phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]benzoic acid dihydrochloride
Molecular Weight:
437.40
Molecular Formula:
C23H28N2O2 • HCl
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Water (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.
Shipping Code:
RT
VIEW ALL Histone demethylation​ PRODUCTS

Histone methylation

UNC7145 | Negative control for UNC6934

CAS:
2561494-78-6
Catalog Number:
10-4118
Activity:
Negative control for UNC6934
Chemical Names:
N-Isopropyl-3-oxo-N-(4-pyrimidin-4-ylcarbamoyl)benzyl)-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide
Molecular Weight:
445.48
Molecular Formula:
C24H23N5O4
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White to off-white solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

UNC6934 | NSD2 inhibitor

CAS:
2561494-77-5
Catalog Number:
10-4119
Activity:
NSD2 inhibitor
Chemical Names:
N-Cyclopropyl-3-oxo-N-(4-pyrimidin-4-ylcarbamoyl)benzyl)-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide
Molecular Weight:
443.46
Molecular Formula:
C24H21N5O4
Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
>98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
VIEW ALL Histone methylation PRODUCTS

Histone phosphorylation

VIEW ALL Histone phosphorylation​ PRODUCTS

Other

Nitazoxanide | Wnt signaling inhibitor

CAS:
55981-09-4
Catalog Number:
10-4633
Activity:
Wnt signaling inhibitor
Chemical Names:
O-[N-(5-Nitrothiazol-2-yl)carbamoyl]phenyl acetate; NTZ
Molecular Weight:
307.28
Molecular Formula:
C12H9N3O5S
Solubility:
Soluble in DMSO (>50 mg/ml)
Physical Properties:
Off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

PRT4165 | E3 ubiquitin ligase inhibitor

CAS:
31083-55-3
Catalog Number:
10-1478
Activity:
E3 ubiquitin ligase inhibitor
Chemical Name:
2-(3-Pyridinylmethylene)-1H-indene-1,3(2H)-dione
Molecular Weight:
235.24
Molecular Formula:
C15H9NO2
Solubility:
Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 6 mg/ml with warming).
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
VIEW ALL Other PRODUCTS

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