Chromatin, transcription and epigenetic regulation.
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CAS 1672684-68-2
MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in…
CAS 1449228-40-3
Senexin B is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with Kds of 140 nM for CDK8 and 80 nM for CDK19.
CAS 2409965-28-0
SRX 3305 is a potent, triple BTK/PI3K/BRD4 inhibitor with IC50 of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ respectively, inhibits BRD4 BD1 and BD2 with IC50 of 77 and 95 nM.SRX3305 showed enhanced binding to the drug-resistant C481S mutant of BTK…
CAS 2734853-80-4
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases[1].
CAS 1474034-05-3
RTA-408 is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO).
CAS 1629160-83-3
MSU 38225 (MSU-38225) is a novel small molecule that inhibit the Nrf2 pathway, potentially inhibiting Nrf2 transcriptional activity and cancer cell growth; MSU38225 downregulates Nrf2 transcriptional activity and decreases the expression of Nrf2 downstream…
CAS 1809336-93-3
Valemetostat (DS-3201) tosylate, a first-in-class EZH1/2 dual inhibitor with IC50 values ＜10 nM. Valemetostat tosylate can be used for the research of relapsed/refractory peripheral T-cell lymphoma.
CAS 895460-70-5
BRD7586 is a cell-permeable small molecule inhibitor of SpCas9 with EC50 of 6.2 µM and 5.7 µM in the eGFP-disruption and HiBiT-knock-in assays, respectively. BRD7586 specifically engages SpCas9 but not Cas12a in cells and enhances SpCas9 specificity at…
CAS 2304621-06-3
LDC203974(IMT1B) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT) with improved pharmacokinetic profiles than LDC195943(IMT1).
CAS 1706738-98-8
CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors
CAS 2138861-99-9
ABBV-744 is a highly BDII-selective BET bromodomain inhibitor, used in the research of inflammatory diseases, cancer, and AIDS.
CAS 2270879-17-7
BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are…
CAS 1825302-42-8
H3B-8800 is an orally available splicing modulator that targets spliceosome SF3b complex containing either WT or mutant SF3B1 (binding IC50 of 0.3-2 nM); demonstrates dose-dependent inhibition of both canonical splicing and aberrant splicing induced by mutant…
CAS 2671128-05-3
FHD-286 is a BRG1/BRM ATPase inhibitor for the treatment of BAF-related disorders such as acute myeloid leukemia.
CAS 2476724-75-9
PTC-258 2HCl is a specific and orally active splicing modulator of Elongator complex protein 1 gene (ELP1). PTC258 increases the expression of ELP1 in vitro and in vivo. PTC258 is well tolerated in mouse model.
CAS 2276680-91-0
T-518 (T518) is a potent, highly selective, brain penetrant, oral HDAC6 inhibitor with IC50 of 36 nM.T-518 did not obviously inhibit human HDAC1, 4, or 7 at 10 uM, which belongs to Class I or Class IIa HDAC.T-518 showed brain penetration in an oral dose and…
CAS 2170137-61-6
GSK-3685032(GSK 3685032) is a first-in-class, potent, non-nucleoside, reversible, selective inhibitor of DNMT1 with IC50 of 0.036 μM. GSK3685032 induces robust loss of DNA methylation, transcriptional activation and cancer cell growth inhibition in vitro.
CAS 2714434-21-4
IAG933 (IAG-933) is a potent, selective and orally efficacious YAP1/WWTR1(TAZ)-panTEAD protein-protein interaction inhibitor (YAP/TAZ-TEADs PPI), inhibits TEAD-driven transcriptional activity and displays anti-cancer effects.
CAS 2417718-25-1
VT104 (VT-104) is a specific small molecule inhibitor of YAP/TAZ-TEAD-dependent transcription with IC50 of 10.4 nM in YAP reporter assay, pan-TEAD palmitoylation inhibitor.VT104 inhibited palmitoylation of both endogenous TEAD1, TEAD3 proteins in cells.VT104…
CAS 2378626-29-8
TED-347 (TED347) is an irreversible inhibitor of TEAD4-Yap1 protein-protein interaction (EC50=5.9 uM in FP asssays) via covalent modification of conserved cysteine (Cys367, Ki=1.3 uM), inhibits its binding to Yap1, blocked its transcriptional activity;…
CAS 28293-38-1
NSC112200 is a chemical inhibitor of the EZH2 deubiquitinase ZRANB1 (at 10 uM), destabilizes EZH2, promotes proteasomal degradation of EZH2 and inhibits the viability of TNBC cells; NSC112200 is a mixture of 2,5-dibromo-3,6-dimethyl-1,4- benzenediol and…
CAS 2855085-25-3
MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).
CAS 2169919-21-3
SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute…
CAS 1111234-96-8
UT-59 is a specific inhibitor that targets the cholesterol-sensing membrane protein Scap (SREBP cleavage-activating protein). It functions by binding to Scap's cholesterol-binding site, which prevents Scap from interacting with SREBPs (sterol regulatory…
CAS 931963-55-2
E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648…
CAS 2609675-22-9
SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM…
CAS 1357362-02-7
Vafidemstat is a dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
CAS 1154028-82-6
Molidustat (BAY 85-3934) is a novel inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with mean IC50 values of 480 nM for PHD1, 280 nM for PHD2, and 450 nM for PHD3.
DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal…
CAS 112522-64-2
CI-994 (Tacedinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.
CAS 1320288-17-2
UNC0646 is a potent and selective G9a inhibitor with IC50 of 6 nM.UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively). UNC0646 potently…
CAS 949912-58-7
Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.Remodelin can improve nuclear architecture, chromatin organization, and fitness of both human lamin A/C-depleted cells and HGPS-derived patient cells, and decrease…
CAS 1622921-15-6
Remodelin HBr salt is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.Remodelin can improve nuclear architecture, chromatin organization, and fitness of both human lamin A/C-depleted cells and HGPS-derived patient cells, and…
CAS 83280-65-3
Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
CAS 440662-09-9
CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC50 of 0.9 μM for TAF1, and a Kd of 1.8 μM for TAF1 (2).
CAS 1158279-20-9
HLCL-61 hydrochloride is a first-in-class small-molecule inhibitor of PRMT5. Target: PRMT5in vitro: HLCL-61 shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples, starting at 12 h post-treatment and…
CAS 790241-43-9
DB818 (DB-818, DB 818) is a small molecule inhibitor of HOXA9/DNA interaction through binding as minor groove DNA ligand on the HOXA9 cognate sequence; directly bind to HOXA9-cognate sequence with Kd value of 4.6 nM (HBS sequence); alters HOXA9-mediated…
CAS 16611-84-0
Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.
CAS 202592-23-2
JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.
CAS 500579-04-4
GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
CAS 432529-82-3
BCI-121 significantly inhibits SMYD3-substrate interaction and chromatin recruitment and is effective in reducing proliferation in various cancer cells types. BCI-121 significantly reduces proliferation of HT29 (by 46%) and HCT116 (by 54%) cells at 72 h and…
CAS 1423715-37-0
Seclidemstat (SP-2577) is a potent LSD1 inhibitor, with a mean IC50 of 127 nM.
CAS 86867-01-8
Methyl donor; cofactor for enzyme-catalyzed methylations, including catechol O-methyltransferase (COMT) and DNA methyltransferases (DNMT). Although present in all cells, it is concentrated in liver where 85% of all methylation reactions occur. It is also…
