Modify Search
Select all
Products
Pages
Posts
Modify Search
Select all
Products
Pages
Posts
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

GSK620 | BD2 selective BET inhibitor

GSK620 (2088410-46-0) is a BET inhibitor 220-fold more selective for BD2 over BD1 (pIC50 BD2 = 7.1; BD1 = 4.8).1 It ameliorated collagen-induced arthritis in a rat model

CPI203 | BET bromodomain inhibitor

CPI203 (1446144-04-2), a JQ1 analog, is a potent and selective inhibitor of the BET bromodomain BRD4 (IC50 = 26 nM).1 It helps promote the maintenance of hematopoietic stem

BI 9564 | BRD9 bromodomain inhibitor

BI 9564 (1883429-22-8) is a potent, selective, and cell permeable inhibitor of the BRD9 bromodomain, a subunit of the switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complex (IC50 =

Deubiquitinase

OTUDin3 | OTUD3 inhibitor

OTUDin3 (441290-65-9) is a potent inhibitor of the deubiquitinase OTUD3, a member of the ovarian tumor proteases which plays a key role in tumorigenesis, neurodegeneration, metabolism,

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

DNA methylation

DBIC | DNMT3B S-nitrosylation inhibitor

DBIC (487026-67-5) specifically inhibits S-nitrosylation of DNA methyltransferase 3B (DNMT3B) at low concentrations, IC50≤100 nM, without affecting its enzymatic activity. Treatment with DBIC prevents nitric oxide-induced

DBIC-neg2 | DBIC negative control

CAS:
N/A
Catalog Number:
10-5162
Activity:
DBIC negative control
Chemical Names:
(E)-N’-(3,4-Dihydroxybenzylidene)acetohydrazide
Molecular Weight:
194.19
Molecular Formula:
C9H10N2O3
Solubility:
Soluble in DMSO (40 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
>98% TLC
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

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

DNA demethylation

TETi76 ester | TET inhibitor

TETi76 ester (1451750-73-4) is a cell permeable inhibitor of TET dioxygenases  (IC50s: TET1 = 1.5 µM; TET2 = 9.4 µM; TET3 = 8.8 µM), indirect (via cytosine

Histone acetylation

WM-1119 | HAT KAT6A inhibitor

WM-1119 (2055397-28-7) is a potent and selective inhibitor of the MYST family histone acetyltransferase (HAT) KAT6A (MOZ) – IC50 = 6.3 nM.1,2 Induces cell cycle exit and cellular

TTK21 | CBP/p300 histone acetyltransferase activator

CAS:
709676-56-2
Catalog Number:
10-5669
Activity:
Histone acetyltransferase CBP/p300 activator
Chemical Names:
N-[4-Chloro-3-(trifluoromethyl)phenyl]-2-propoxybenzamide
Molecular Weight:
357.76
Molecular Formula:
C17H15ClF3NO2
Solubility:
Soluble in DMSO (50 mg/ml)
Physical Properties:
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 1 month.
Shipping Code:
RT

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

Histone deacetylation

BG45 | HDAC3 selective inhibitor

BG45 (926259-99-6) is a potent and selective HDAC3 inhibitor (IC50 = 289 nM), IC50s for HDAC1, 2 and 6 = 2, 2.2 and >20 mM respectively.1 Inhibits tumor

OSS-128167 | SIRT6 Inhibitor

CAS:
887686-02-4
Catalog Number:
10-5197
Activity:
SIRT6 inhibitor
Chemical Names:
5-(3-(Furan-2-carboxamido)benzamido)-2-hydroxybenzoic acid
Molecular Weight:
366.33
Molecular Formula:
C19H14N2O6
Solubility:
Soluble in DMSO (25 mg/ml); Ethanol (25 mg/ml)
Physical Properties:
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 or ethanol may be stored at -20°C for up to 1 month.
Shipping Code:
RT

Histone demethylation

iJMJD6 | Arginine demethylase JMJD6 inhibitor

iJMJD6 (899548-78-8) is an inhibitor of the arginine demethylase JMJD6 (IC50 = 220 nM) with selectivity over other JmjC domain-containing proteins.1 Exhibited antiproliferative effects in HeLa (EC50 = 1.49

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

Histone methylation

GSK126 | EZH2 methyltransferase inhibitor

CAS:
1346574-57-9
Catalog Number:
10-3394
Activity:
EZH2 methyltransferase inhibitor
Chemical Names:
N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-[(1S)-1-methylpropyl]-6-[6-(1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
Molecular Weight:
526.69
Molecular Formula:
C31H38N6O2
Solubility:
Soluble in DMSO (16 mg/ml)
Physical Properties:
Cream solid
Purity:
>98% HPLC/TLC
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

Other

BRM014 | BRM/BRG1 ATPase inhibitor

SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homologue (BRM), together with its close homologue Brahma-related gene 1 (BRG1),

UZH2 | METTL3 inhibitor

UZH2 (2756566-45-5) is a potent (IC50 = 5 nM) and selective (against METTL1 and METTL16) inhibitor of the RNA methyltransferase METTL3, a key component of the

SGC-iMLLT | MLLT1/3 YEATS domain inhibitor

CAS:
2255338-25-9
Catalog Number:
10-4046
Activity:
MLLT1/3 YEATS domain inhibitor
Chemical Names:
(S)-1-Methyl-N-(2-((2-methylpyrrolidin-1-yl)methyl)-1H-benzo[d]imidazole-5-yl)-1H-indazole-5-carboxamide
Molecular Weight:
388.48
Molecular Formula:
C22H24N6O
Solubility:
Soluble in DMSO (at least 50 mg/ml)
Physical Properties:
Off-white to beige 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