Epigenetics & Gene Regulation
Chromatin, transcription and epigenetic regulation.
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Kinases & Cell SignalingKinase inhibitors and modulators of intracellular signaling pathways.936 products →Epigenetics & Gene RegulationChromatin, transcription and epigenetic regulation.277 products →DNA Damage, Repair & Cell CycleDNA replication, repair, mitosis and cell-cycle regulation.228 products →Cell Death & AutophagyApoptosis, ferroptosis, necroptosis and autophagy research.117 products →Protein Degradation & ProteostasisPROTACs, molecular glues, ubiquitin systems, chaperones and proteostasis.173 products →Immunology & InflammationInnate and adaptive immunity, inflammatory pathways and immune signaling.297 products →NeuroscienceNeurotransmission, neural targets and neurological research.363 products →GPCRs & Receptor BiologyG-protein-coupled, nuclear and other ligand-binding receptors and their modulators.428 products →Ion Channels & TransportersIon channels, membrane transporters and pumps.196 products →Metabolism & EndocrinologyMetabolic enzymes, lipid and glucose metabolism and hormone signaling.404 products →Cardiovascular & HematologyVascular biology, coagulation, cardiac function, blood-pressure and hematology research.141 products →Anti-infectivesAntibacterial, antiviral, antifungal and antiparasitic research tools.202 products →Cancer ResearchCompounds with documented oncology research applications.530 products →ADCs & BioconjugationADC payloads, linkers, drug-linker conjugates and conjugation reagents.38 products →Probes & Assay ReagentsFluorescent and imaging probes, enzyme substrates and assay reagents.82 products →Natural ProductsNaturally occurring compounds for biological and chemical research.73 products →Cell Biology & Intracellular TransportCytoskeletal dynamics, endocytosis, vesicle trafficking, organelle function and cell differentiation.61 products →
Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
Epigenetics & Gene Regulation products
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LF3
CAS 664969-54-4
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
Molibresib(I-BET-762）
CAS 1260907-17-2
GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
Tucidinostat(Chidamide)
CAS 743420-02-2
Chidamide is a synthetic benzamide-type HDAC inhibitor, inhibits HDAC1, HDAC2, HDAC3 and HDAC10 with IC50s of 95, 160, 67 and 78 nM, respectively.
MI-463
CAS 1628317-18-9
MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
IOX1
CAS 5852-78-8
IOX1 is the most potent broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases; IC50 for KDM4A/KDM3A is 0.6/0.1 uM.IC50 value: 0.6/0.1 uM(KDM4A/KDM3A) [1]Target: JmjC KDMs inhibitorIOX1 is the most potent against a representative panel of…
Pifithrin-α (hydrobromide)
CAS 63208-82-2
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis.
Roxadustat(FG-4592)
CAS 808118-40-3
Roxadustat (FG-4592) is an oral hypoxia-inducible factor (HIF) prolyl hydroxylase inhibitor developed for the treatment of anemia.
(+)-JQ1
CAS 1268524-70-4
(+)-JQ-1 is a BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)).
(-)-JQ-1
CAS 1268524-71-5
(-)-JQ-1 is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (−)-JQ1 has no effect.
AI-10-49
CAS 1256094-72-0
AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics,and delays leukemia…
T-5224
CAS 530141-72-1
T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1. It also inhibits MMP3/13 with IC50s of 10 nM.
R306465(JNJ-16241199)
CAS 604769-01-9
R306465, also known as JNJ-16241199, is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models.
GSK-LSD1
CAS 1431368-48-7
GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1).
GSK2801
CAS 1619994-68-1
GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.GSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively.…
GSK503
CAS 1346572-63-1
GSK503 is a potent and specific inhibitor of EZH2 methyltransferase with Kiapp values of 3 to 27 nM.
GSK1324726A (I-BET726)
CAS 1300031-52-0
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with high affinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
UNC-0642
CAS 1481677-78-4
UNC0642 is a potent and selective G9a/GLP inhibitor, with an IC50 of less than 2.5 nM.
BRD4770
CAS 1374601-40-7
BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).
Sirtinol
CAS 410536-97-9
Sirtinol is a sirtuin inhibitor, with IC50s of 48 μM, 57.7 μM and 131 μM for ySir2, hSIRT2 and hSIRT2, respectively.
4EGI-1
CAS 315706-13-9
4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
GSK2879552
CAS 1401966-69-5
GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
A-366
CAS 1527503-11-2
A-366 is a potent histone methyltransferase G9a inhibitor with an IC50 of 3.3 nM.
RG3039(PF-06687859)
CAS 1005504-62-0
RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.
(R)PFI-2 HCl
CAS 1627607-87-7
PFI-2 hydrochloride is a a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2.(R)-PFI-2 is highly selective (>1,000-fold) for SETD7, over a panel of…
SGC-707
CAS 1687736-54-4
SGC707 is a first-in-class PRMT3 chemical probe which is a potent, selective, and cell-active allosteric inhibitor of PRMT3 with IC50 of 31 nM.
MC1568
CAS 852475-26-4
MC1568 is a selective class II (IIa) histone deacetylas (HDAC II) inhibitor, used for cancer research.
I-BET151
CAS 1300031-49-5
I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
PF-CBP1(PF-06670910) hydrochloride
CAS 1962928-21-7
PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons.
RS-1
CAS 312756-74-4
RS-1 is a RAD51 activator, and also increases CRISPR/Cas9-mediated knock-in efficiencies.
EPZ015866
CAS 1616391-87-7
EPZ015866 is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 22 nM.
Scriptaid(GCK1026)
CAS 287383-59-9
Scriptaid is a potent histone deacetylase (HDAC) inhibitor, used in cancer research.
ML-324
CAS 1222800-79-4
ML324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.ML324 is a probe molecule that displays submicromolar inhibitory activity toward JMJD2E (in vitro) and possesses excellent in vitro ADME properties. In contrast to previously…
2-Methoxyestradiol
CAS 362-07-2
2-Methoxyestradiol is an angiogenesis inhibitor and apoptosis inducer with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.
TMP269
CAS 1314890-29-3
TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC50s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
KC7F2
CAS 927822-86-4
KC7F2 is a potent HIF-1 pathway inhibitor and that its potential as a cancer therapy agent warrants further study.Target：HIFin vitro: KC7F2 is the second HIF-1α inhibitor. KC7F2 is shown to inhibit the proliferation of cancer cells, an effect that is…
Quisinostat (JNJ-26481585) 2HCl
CAS 875320-29-9
Quisinostat (JNJ-26481585) is an orally available, potent HDAC inhibitor with an IC50 of 0.11 nM for HDAC1.
Trichostatin A (TSA)
CAS 58880-19-6
Trichostatin A is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
CUDC-101
CAS 1012054-59-9
CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively.
EPZ015938(pemrametostat)
CAS 1616392-22-3
GSK3326595 is a potent, selective, reversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 6.2 nM.
Briciclib(ON 013105,ON 014185)
CAS 865783-99-9
Briciclib is a water soluble derivative of ON 013100, and has the potential in targeting eIF4E for solid cancers.
MM-102
CAS 1417329-24-8
MM-102 is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
GSK6853
CAS 1910124-24-1
GSK6853 is a potent and selective inhibitor of the BRPF1 bromodomain. shows excellent BRPF1 potency (pKd 9.5) andgreater than 1600-fold selectivity over all other bromodomainstested.target: BRPF1.[1]In vivo: The ip route of administration would be suitable…
RN-1 Hydrochloride
CAS 1781835-13-9
RN-1 dihydrochloride is a potent, brain-penetrant, irreversible and selective lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 70 nM. RN-1 dihydrochloride exhibits selectivity for LSD1 over MAO-A and MAO-B with IC50 values of 0.51 μM and 2.785…
BI-9564
CAS 1883429-22-8
BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.
Browse target & topic index A–Z (366)
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