Epigenetics & Gene Regulation

ML-264

CAS 1550008-55-3

ML264 is an antitumor agent that potently and selectively inhibits Krüppel-like factor five (KLF5) expression.

UNC-1999

CAS 1431612-23-5

UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH1/2 with IC50s of 10 nM and 45 nM, repectively.

QC-3611

CAS 1613410-75-5

QC-3611 is a selective inhibitor of JARID1A/1B, which is a target existing in various tumors (JARID1A IC50 = 13 nM ;JARID1B IC50 = 2 nM). QC-3611 is promisingly to be used as an antineoplastic drug.

TDI-011536

CAS 2687970-96-1

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

Bardoxolone methyl

CAS 218600-53-4

Bardoxolone is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.

Oltipraz

CAS 64224-21-1

Oltipraz has an inhibitory effect on HIF-1α activation by insulin in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM.

LW6(CAY10585)

CAS 934593-90-5

LW6 is a novel HIF-1 inhibitor with an IC50 of 4.4 μM.

GPS167

GPS167 is a specific small molecule splicing regulator SRSF10 inhibitor, modulates BCLAF1 splicing with IC50 of 2 uM in human colorectal HCT116 cells, directly inhibits CLK1, CLK2 and CLK4, but not SRPK1 and DYRK1A.GPS167 promotes the dephoshorylation of…

NSD1 inhibitor BT5

CAS 2351225-46-0

1. Huang H, et al. Nat Chem Biol. 2020 Dec;16(12):1403-1410. Chemical & Physical Properties

Dacinostat (NVP-LAQ824, LAQ824)

CAS 404951-53-7

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

HDAC3 inhibitor PT3

CAS 2710273-81-5

HDAC3 inhibitor PT3 is a novel potent, selective, BBB-permeable HDAC3 inhibitor.PT3 exhibited higher selectivity for HDAC3 over HDAC1, HDAC6, and HDAC8 compared to the reference compound CI994.PT3 upregulated H3K9 acetylation, CREB 1, BDNF, TRKB, Nr4a2,…

DP308

CAS 685884-37-1

DP308 is a novel and effective 53BP1 tandem Tudor domain (TTD) inhibitor, disrupts the binding between 53BP1 and H4K20me2 peptide with IC50 of 1.69 uM.

YTHDC1 inhibitor 40 (compound 40)

CAS 2995344-53-9

YTHDC1 inhibitor 40 is a potent, selective m6A reader YTHDC1 inhibitor with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) cell lines THP-1, MOLM-13, and NOMO-1.YTHDC1 inhibitor 40…

Disodium (R)-2-Hydroxyglutarate

CAS 103404-90-6

D-alpha-Hydroxyglutaric acid disodium salt is a weak competitive α-Ketoglutarate(α-KG)-dependent dioxygenase inhibitor with Ki of 10.87±1.85 mM. Ki for L-Hydroxyglutaric acid (L-2-HG) is 0.628±0.036 mM.

L002(NSC764414)

CAS 321695-57-2

L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM. L002 has weak inhibitory effects against PCAF and GCN5 (IC50s =35 and 34 µM, respectively) and is specific for p300 over a panel of additional…

BVT-948

CAS 39674-97-0

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.

Ezetimibe (Zetia)

CAS 163222-33-1

Ezetimibe (SCH 58235) is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor.

Fatostatin

CAS 298197-04-3

Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of…

UNC6934

CAS 2561494-77-5

UNC6934 is a potent and selective drug-like chemical probe to interrogate the function of NSD2-PWWP1 with Kd of 91 nM.UNC6934 disrupts the NSD2-PWWP1 interaction with H3K36me2 nucleosomes in U2OS cells as measured by a NanoBret assay with an IC50 of 1.09 ±…

UU-T03

CAS 1586007-00-2

UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin…

LDC195943(IMT1)

CAS 2304621-31-4

LDC195943(IMT1) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT).

FN1-8

CAS 1419258-63-1

FN1-8 is a novel, synthetic small molecule that efficiently interferes with Gli/TAF9 interaction and downregulate Gli/TAF9-dependent transcriptional activity (at 15 uM); inhibits non-canonical Gli activation and acts downstream of the canonical Hh pathway;…

PRL-295

CAS 2377770-85-7

PRL-295 is a small molecule Keap1-Nrf2 protein–protein interaction inhibitor.PRL-295 binds to Keap1 in the cellular environment, disrupting its interaction with Nrf2, which leads to enhanced gene expression of the classical Nrf2 target NQO1 in cells and in…

Citarinostat(ACY-241)

CAS 1316215-12-9

Citarinostat is a HDAC6 specific inhibitor, with IC50 of 4 nM and 76 nM for HDAC6 and HDAC3, respectively.IC50 value: 4 nM (HDAC6), 76 nM (HDAC3)Target: HDACThe detailed information please refer to WO2015061684A1 and 2015054197A1.

Peptide P60

CAS 1319725-20-6

Peptide P60 (FOXP3 inhibitor P60) is a 15-mer synthetic peptide, cell-permeable inhibitor of FOXP3, binds specifically to FOXP3; inhibits murine and human-derived Treg and improves effector T cell stimulation, overcomes the inhibitory effect of FOXP3 on the…

SMN2 splicing modulator TEC-1

CAS 2407723-70-8

SMN2 splicing modulator TEC-1 is a novel specific, CNS penetrant small molecule SMN2 splicing modulator, increases the expression level of FL-SMN2 mRNA and decreases the expression level of Δ7 mRNA.TEC-1 showed higher selectively (>60-fold) on…

TGP-29b-066

CAS 349429-86-3

TGP-29b-066 (Targapremir-29b-066) is a specfic small-molecule miR-29b inhibitor that targets miR29b hairpin precursor (pre-miR-29b), selectivity and effectively decreases miR-29b expression levels in C2C12 myoblast, attenuates muscle atrophy in vitro and

TMP195

CAS 1314891-22-9

TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor with an IC50 of 300 nM.

Tubastatin A

CAS 1252003-15-8

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).

Verteporfin (1:1 regioisomer mixture)

CAS 129497-78-5

Verteporfin is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions.

Iadademstat dihydrochloride (ORY-1001 dihydrochloride)

CAS 1431303-72-8

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

MS023

CAS 1831110-54-3

MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM.

GSK-J4 hydrochloride

CAS 1797983-09-5

GSK-J4 is a potent H3K27me3 histone lysine demethylase (KDM) inhibitor, with IC50s of 8.6 μM and 6.6 μM against KDM6B and KDM6A, respectively.

SRT1720 HCl

CAS 1001645-58-4

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

BRD7552

CAS 1137359-47-7

BRD7552 is an inducer of transcription factor PDX1, which increases insulin expression.

C646

CAS 328968-36-1

C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.

ARV-825

CAS 1818885-28-7

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome.…