Epigenetics & Gene Regulation

UNC3866

CAS 1872382-47-2

UNC3866 is a potent antagonist of the CBX7-H3 interaction as determined by AlphaScreen (IC50=66±1.2 nM) and is more than 100-fold selective for CBX7 over the other nine members of this methyl-lysine (Kme) reader panel.

SGC-0946

CAS 1561178-17-3

SGC 0946 is over 100-fold selective For other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL…

TG693

CAS 885272-55-9

TG693 is an orally available, selective, ATP-competitive CLK1 inhibitor with IC50 of 112.6 nM.

Anisomycin

CAS 22862-76-6

Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system.

Pinometostat(EPZ5676)

CAS 1380288-87-8

Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.

SR 8278

CAS 1254944-66-5

SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm[1][2].

preQ1 Dihydrochloride

CAS 86694-45-3

preQ1 is a precursor in the biosynthesis of queuosine, a bacterial nucleoside incorporated into tRNA by tRNA transglycosylase. preQ1 binds to an aptamer domain on tRNA that acts as a riboswitch to repress gene expression.

GSK-343

CAS 1346704-33-3

GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.

PTC-028

CAS 1782970-28-8

PTC-028 is an orally bioavailable inhibitor of stem cell factor BMI-1 in ovarian cancer. PTC-028 selectively inhibits cancer cells whereas normal cells remain unaffected. Depletion of BMI-1 by PTC-028 induces caspase-mediated apoptosis[1].

YF2

CAS 1311423-89-8

YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and…

Dimethyloxaloylglycine(DMOG)

CAS 89464-63-1

DMOG (Dimethyloxallyl Glycine) is a cell-permeable and competitive inhibitor of HIF-1α prolyl hydroxylase (HIF-PH).

OAC1

CAS 300586-90-7

OAC1 is a Octamer-binding transcription factor 4 (Oct4)-activating compound; enhances the iPSC reprogramming efficiency and accelerated the reprogramming process.

OICR9429

CAS 1801787-56-3

OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation

MI-2-2

CAS 1454920-20-7

MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (Kd=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia…

I-BRD9

CAS 1714146-59-4

I-BRD9 is the first selective cellular chemical probe for BRD9 (pIC50=7.3).IC50 value: 7.3 (pIC50) [1]Target: BRD9in vitro: I-BRD9 is a selective cell active chemical probe for bromodomain containing protein 9 inhibition. I-BRD9, the first selective cellular…

LMK-235

CAS 1418033-25-6

LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.

Pracinostat(SB939)

CAS 929016-96-6

Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research.

UNC669

CAS 1314241-44-5

UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).IC50 value: 4.2 uM/3.1 uM (L3MBTL1/L3MBTL3) [1]Target: L3MBTL1/L3MBTL3

BI-7273

BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor with Kd (BRD9, ITC) = 15 nM and Kd (BRD9, DiscoveRx) = 0.75 nM. IC50 (BRD9 alpha assay ) = 19nm. BI-7273 proves to be invaluable as tools to further explore BRD9 biology. Components of the…

BMS-P5

CAS 1550371-22-6

BMS-P5 is a Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor with pIC50 values in the range of 5-​7.5. BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma. Administration of BMS-P5 to multiple myeloma-be

Decitabine

CAS 2353-33-5

Decitabine (NSC 127716) is a DNA methyltransferase inhibitor commonly used to treat myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML).

KG-501(Naphthol AS-E phosphate)

CAS 18228-17-6

KG-501 is a CREB inhibitor, with an IC50 of 6.89 μM.

666-15

CAS 1433286-70-4

666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM.

CCG-203971

CAS 1443437-74-8

CCG-203971 is a second-generation RhoA/myocardin-related transcription factor A (MRTF-A) inhibitor. CCG-203971 potently targets RhoA/C-activated serum response element (SRE)-luciferase (IC50=6.2 μM).

AS1842856

CAS 836620-48-5

AS1842856 is a potent and cell-permeable Foxo1 inhibitor with an IC50 of 30 nM.

SRT2104

CAS 1093403-33-8

SRT 2104 is a brain-permeable activator of SIRT1, used for the research of type 2 diabetes mellitus and Huntington's disease.

MYCi975

CAS 2289691-01-4

MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good…

GSK620

CAS 2088410-46-0

GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620…

Supinoxin

CAS 888478-45-3

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces…

MM-401

CAS 1442106-10-6

A potent inhibitor of MLL1/WDR5 protein-protein interaction with IC50 of 0.9 nM.

Tegatrabetan

CAS 1227637-23-1

Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1)[1].

PF-9363

CAS 2569009-58-9

PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer[1][2].

Givinostat (ITF2357)

CAS 732302-99-7

Givinostat hydrochloride monohydrate is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.

MYF-01-37

CAS 2416417-65-5

MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction[1].

K-975

CAS 2563855-03-6

K-975 is a first-in-class TEAD inhibitor, directly inhibiting YAP/TAZ-TEAD protein-protein interaction and showing a potent anti-tumor effect in malignant pleural mesothelioma. K-975 was covalently bound to an internal cysteine residue located in the…

Tazemetostat(EPZ-6438)

CAS 1403254-99-8

Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor with Ki and IC50 of 2.5 and 11 nM, respectively.

Entinostat (MS-275)

CAS 209783-80-2

Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.

P300/CBP-IN-3

CAS 2299226-01-8

P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1[1].

PTC-209

CAS 315704-66-6

PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM.

Stat5 Inhibitor(STAT5-IN-1)

CAS 285986-31-4

Stat5 Inhibitor(STAT5-IN-1) is a STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform.

ZINC02092166

CAS 354543-09-2

ZINC02092166 is a novel potent, and selective small-molecule inhibitor for the β-catenin/Tcf4 protein-protein interaction with Ki of 1.7 and 7.0 uM in AlphaScreen and FP assay (wild-type β-catenin), respectively; remain affinity for muant catenin V511S,…

IRES-J007

CAS 155514-72-0

IRES-J007 ia an improved IRES inhibitor that blocks IRES-hnRNP A1 binding; binds to a small pocket structure within the RRM-containing fragment of hnRNP A1 (UP1 fragment), inhibits cyclin D1 and c-MYC IRES activity to a greater extent compared with C11…

TTK21(CBP-p300 activator TTK21)

CAS 709676-56-2

TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM; induces acetylation of histones H3 and H4 in vitro but not H2B and H2A; promotes neurogenesis and…

DNL343

CAS 2278265-85-1

DNL343 is a potent, selective, and brain-penetrant eukaryotic translation initiation factor 2B (eIF2B) activator with ATF4 IC50 of 9.8 nM.

EPZ-719

CAS 2697176-16-0

EPZ-719 is a novel and potent SETD2 inhibitor ( IC50 = 0.005 μM) with a high selectivity over other histone methyltransferases.

EGPI-1

CAS 2355263-33-9

EGPI-1 is a potent small molecule that inhibits the translation initiation factors eIF4E/eIF4G interaction.EGPI-1 has potent antiproliferative and proapoptotic activity in multiple myeloma cells, Jurkat cells, and A549 lung cancer cell lines, inhibts A549…

Cl-amidine hydrochloride

CAS 1373232-26-8

In Vitro Cl-amidine is a peptidylarginine deminase (PAD) inhibitor, with an IC50 of 5.9±0.3 μM for PAD4 and Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000…

ICG-001

CAS 780757-88-2

ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. It works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM.