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Chromatin/Epigenetics

Epigenetics means above genetics. It determines how much and whether a gene is expressed without changing DNA sequences. Epigenetic regulations include, 1. DNA methylation: the addition of methyl group to DNA, converting cytosine to 5-methylcytosine, mostly at CpG sites; 2. Histone modifications: posttranslational modificationEpigeneticss of histone proteins including acetylation, methylation, ubiquitylation, phosphorylation and sumoylation; 3. miRNAs: non-coding microRNA downregulating gene expression; 4. Prions: infectious proteins viewed as epigenetic agents capable of inducing a phenotype without changing the genome.

Products for Chromatin/Epigenetics

Cat.No. Product Name Information
BCC5595 EX-527 R-enantiomer Selisistat R-enantiomer (EX-527 R-enantiomer) is much less active R-enantiomer of Selisistat, with an IC50 of > 100 μM for SIRT1.
BCC6355 TC-E 5001
BCC2170 MLN8054 MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
BCC2471 Thiolutin Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.
BCC2460 Fostriecin sodium salt Potent PP2A and PP4 inhibitor
BCC5626 WDR5 0103 WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.
BCC2433 DMOG DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1related signal. DMOG induces cell autophagy.
BCC2173 AT9283 AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
BCC2058 XL228 XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
BCC6484 PFI 4 PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4.
BCC5597 GSK 5959 GSK-5959 is a potent, selective and cell permeable BRPF1 bromodomain inhibitor with IC50 ~ 80 nM.
BCC2454 NU 1025 NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity.
BCC2197 AZ 960 AZ960 is a potent and specific inhibitor of the JAK2 kinase with a Ki of 0.45 nM.
BCC1267 ABT-888 (Veliparib) Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively.
BCC2076 Veliparib dihydrochloride Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
BCC4192 ABC294640 Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.
BCC5579 OF-1 OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.
BCC6469 BG45 BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM).
BCC2434 KC7F2 KC7F2 is a potent hypoxia inducible factor-1 (HIF-1) pathway inhibitor with an IC50 of 20 μM in LN229-HRE-AP cells, and with potential as a cancer therapy agent.
BCC2221 SGI-110 Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS).
BCC2211 A-966492 A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
BCC2186 ENMD-2076 ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
BCC2180 TAK-901 TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
BCC2191 AZD1480 AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively.
BCC1131 BIX 01294 BIX-01294 is an inhibitor of G9a Histone Methyltransferase with an IC50 of 1.9 μM.
BCC2190 TG101348 (SAR302503) Fedratinib (TG-101348) is a selective inhibitor of JAK2 with an IC50 of 3 nM, showing 35- and 334-fold selectivity over JAK1 and JAK3, respectively.
BCC7109 NSC 95397 NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
BCC1925 SB1317 SB1317 is a potent inhibitor of CDK2, JAK2, and FLT3 for the treatment of cancer, with IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively.
BCC1276 Ruxolitinib (INCB018424) Ruxolitinib (INCB18424) is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.
BCC2201 S-Ruxolitinib (INCB018424) Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib S enantiomer is a JAK inhibitor
BCC2184 PF-03814735 PF-03814735 is a potent, orally available and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
BCC2183 GSK1070916 GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
BCC2187 CCT129202 CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
BCC6503 Peficitinb (ASP015K, JNJ-54781532) Peficitinib is an oral JAK inhibitor, with IC50s of 3.9, 5.0, 0.7 and 4.8 nM for JAK1, JAK2, JAK3 and Tyk2, respectively.
BCC6456 Decernotinib(VX-509) Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.
BCC2175 AMG-900 AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
BCC2057 XL019 XL019 is a potent，orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
BCC6480 2-hexyl-4-Pentynoic Acid
BCC2442 SD 1008 JAK2/STAT3 signaling pathway inhibitor