Epigenetics & Gene Regulation

SRT1720

CAS 925434-55-5

SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities agaiinst SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.

Vorinostat (SAHA)

CAS 149647-78-9

Vorinostat is a potent and orally available inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV ), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.

SRT3025

CAS 1231952-55-8

Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss

CCG1423

CAS 285986-88-1

CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.

SIRT2 Inhibitor II, AK-1

CAS 330461-64-8

AK-1 is a potent, specific and cell-permeable SIRT2 inhibitor.

ITF2357

CAS 199657-29-9

Givinostat or gavinostat, aslo known as ITF2357, is a potent and orally active histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride.…

CPI-455

CAS 1628208-23-0

CPI-455 is a specific KDM5 inhibitor.

IBS007125

CAS 2941099-67-6

IBS007125 is a small molecule inhibitor of c-Maf, inhibits multiple myeloma proliferation by targeting cMaf transcriptional activity.

UNC926

CAS 1184136-10-4

UNC-926 is a methyl-lysine (Kme) reader domain inhibitor; inhibits L3MBTL1 with an IC50 of 3.9 μM.

RK-33

CAS 1070773-09-9

RK-33 is an RNA helicase inhibitor against DDX3, and inhibits its helicase activity.

MG149

CAS 1243583-85-8

MG149 is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF(IC50= 47 uM); little potent for PCAF and p300(IC50 >200 uM).IC50 value: 74/47 uM (Tip60/MOF) [1]Target: Tip60/MOFMG 149, at 200 μM, inhibited about 90% of Tip60…

iCRT 14

CAS 677331-12-3

iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.

3-TYP

CAS 120241-79-4

3-TYP is a selective SIRT3 inhibitor, with an IC50 of 16 nM, more potent over SIRT1 (IC50=88 nM), SIRT2 (IC50=92 nM).

AGK2

CAS 304896-28-4

AGK2 is a selective SIRT2 inhibitor with IC50 of 3.5 μM. AGK2 can also inhibit SIRT1 and SIRT3 with IC50 of 30 and 91 μM, respectively.

RGFP 966

CAS 1357389-11-7

RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM.

EED-226

CAS 2083627-02-3

EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.

ML-329

CAS 19992-50-8

ML329 is a small molecule inhibitor of MITF; inhibits TRPM-1 promoter activity with an IC50 of 1.2 μM.

Ezutromid

CAS 945531-77-1

Ezutromid is a novel Small utrophin's translation modulator with EC50 of 0.4 uM .In vitro: 1) SMT C1100 induces increased levels of utrophin RNA in human muscle cells.2) Treatment of human DMD cells with SMT C1100 lead to a 2-fold increase in utrophin protein…

MGCD0103 (Mocetinostat)

CAS 726169-73-9

Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7,…

RVX-208

CAS 1044870-39-4

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.

10074-G5

CAS 413611-93-5

10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.

Madrasin

CAS 374913-63-0

Madrasin is a potent and cell penetrant splicing inhibitor that interferes with the early stages of spliceosome assembly. Madrasin is cytotoxic at higher concentrations, although at lower concentrations it induces cell cycle arrest, promotes a specific…

CPI-637

CAS 1884712-47-3

CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.IC50:0.03±0.01μM (CBP/EP300)[1]IC50:11.0±0.6 μM(BRD4)[1]CPI-637, which demonstrated substantial biochemical…

Droxinostat

CAS 99873-43-5

Selective HDAC3, HDAC6 and HDAC8 inhibitor (IC50 values are 16.9, 2.47 and 1.46 μM for HDAC3, 6 and 8 respectively). Induces apoptosis. Shows antitumor effects in vivo. For the detailed information of Droxinostat, the solubility of Droxinostat in water, the…

Tubacin (BML-GR362)

CAS 537049-40-4

Tubacin is a potent and selective inhibitor of HDAC6, with an IC50 value of 4 nM and approximately 350-fold selectivity over HDAC1.

PTACH (NCH-51)

CAS 848354-66-5

PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human cancer cells, with EC50 values ranging from 1 to 10 μM.

SP2509

CAS 1423715-09-6

SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.

ML385

CAS 846557-71-9

ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.

Daprodustat

CAS 960539-70-2

Daprodustat (GSK1278863) is an orally active hypoxia-inducible factor prolyl hydroxylase inhibitor being developed for the treatment of anemia associated with chronic kidney disease.

LLY-507

CAS 1793053-37-8

LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2 with an IC50 of 15 nM.

CBL0137

CAS 1197996-80-7

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and…

Parthenolide

CAS 20554-84-1

Parthenolide is an NF-κB inhibitor, reduces histone deacetylase 1 (HDAC-1) and DNA methyltransferase 1 independent of NF-κB inhibition.

EX-527(Selisistat)

CAS 49843-98-3

Selisistat (EX-527) is a potent and selective SIRT1 inhibitor with IC50 of 98 nM.

A-196

A-196 is a potent and selective chemical inhibitor of SUV420H1 and SUV420H2 that inhibits the di- and trimethylation of H4K20me in multiple cell lines. Target: A-196 is a selective chemical probe for SUV420H1/H2. A-196 is the first potent and selective…

GSK8573

CAS 1693766-04-9

GSK8573 (compound 23) is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy[1].

HhAntag

CAS 496794-70-8

HhAntag is a small molecule inhibitor of GLI1-mediated transcription, an essential down-stream element of the Hedgehog (Hh) pathway; antitumor agent.IC50 value:Target: Gli

Homoharringtonine

CAS 26833-87-4

Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation.

UF010

CAS 537672-41-6

UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.IC50 value: 0.06 μM (HDAC3), 0.1 μM (HDAC2), 0.5 μM (HDAC1), 1.5 μM(HDAC 8)Target:…

CAY10683(Santacruzamate A)

CAS 1477949-42-0

Santacruzamate A is a potent and selective histone deacetylase inhibitor.

BML-210(CAY10433)

CAS 537034-17-6

BML-210 is a novel HDAC inhibitor, and its mechanism of action has not been characterized.

M 344

CAS 251456-60-7

M344 (D 237) is an inhibitor of histone deacetylase (IC50=100 nM) and an inducer of terminal cell fifferentiation.

HPOB

CAS 1429651-50-2

HPOB is a highly potent and selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 of 56 nM, >30 fold less potent against other HDACs.target: HDAC6 [1]IC 50: 56nM [1]In vitro: HPOB causes growth inhibition of normal and transformed cells but does not…

Ricolinostat (ACY-1215)

CAS 1316214-52-4

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

UU-T02

CAS 1500080-17-0

UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; displays 63-fold and 175-fold selectivity over β-catenin/E-cadherin and β-catenin/APC interactions, respectively.

OSS-128167(SIRT6-IN-1)

CAS 887686-02-4

OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.

STATTIC

CAS 19983-44-9

Stattic is a potent inhibitor of STAT3 activation and dimerization.

MK-8617

CAS 1187990-87-9

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.

AS-1517499

CAS 919486-40-1

AS1517499 is a potent STAT6 inhibitor with an IC50 of 21 nM.