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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
BCC2222 SRT1720 HCl SRT1720 HCl is a selective SIRT1 activator with EC50 of 0.16 μM in a cell-free assay, but is >230-fold less potent for SIRT2 and SIRT3.
BCC2176 MK-5108 (VX-689) MK-5108 is a highly potent and specific inhibitor of Aurora A kinase with an IC50 value of 0.064 nM.
BCC3667 Tenovin-6 Tenovin-6 is an inhibitor of SIRT1 and SIRT2, slightly inhibits HDAC8, and is also a potent activator of p53, with IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively.
BCC2457 Calyculin A Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM.
BCC4588 SGI-1027 SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC50s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.
BCC1129 3-Deazaneplanocin,DZNep 3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor.
BCC2232 SGI-1776 free base SGI-1776 is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
BCC5532 LB-100
BCC2166 MLN8237 (Alisertib) Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
BCC4264 AZ505
BCC4265 AZ505 ditrifluoroacetate AZ505 ditrifluoroacetate is a potent and selective SMYD2 inhibitor with IC50 of 0.12 μM.
BCC1761 MK-4827 Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
BCC4173 MK-4827 hydrochloride Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
BCC4174 MK-4827 tosylate Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate (MK-4827 tosylate) leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.
BCC5179 MK-4827 Racemate
BCC4475 RVX-208 Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC50s are 87±10 μM and 0.51±0.041 μM for BD1 and BD2, respectively.
BCC2213 UPF 1069 UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
BCC2196 CYT387 Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
BCC1506 CYT387 sulfate salt Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
BCC1815 NVP-BSK805 NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.
BCC1913 Ruxolitinib sulfate Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
BCC1912 Ruxolitinib phosphate Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
BCC1705 LKB1 (AAK1 dual inhibitor) Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
BCC1950 SRT2104 (GSK2245840) SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD+ dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease.
BCC1934 SCH-1473759 SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
BCC2188 CCT137690 CCT 137690 is a potent and orally available aurora kinase inhibitor with IC50s of 15, 25, and 19 nM for aurora A, B and C, respectively.
BCC2449 BYK 204165 BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.
BCC2440 Lestaurtinib
BCC7299 CI 976
BCC2177 SNS-314 Mesylate SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.
BCC6412 Molidustat (BAY85-3934) 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.
BCC3982 MCB-613 MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program.
BCC2461 Fumonisin B1 Fumonisin B1 is a mycotoxin produced from Fusarium moniliforme. Fumonisin B1 is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis. Fumonisin B1 is the most abundant and toxic fumonisin.
BCC2465 Sal 003 Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
BCC2214 AZD2461 AZD-2461 is a potent PARP inhibitor, with IC50s of 5 nM, 2 nM and 200 nM for PARP1, PARP2 and PARP3, respectively.
BCC2445 UNC 926 hydrochloride UNC-926 is a methyl-lysine (Kme) reader domain inhibitor; inhibits L3MBTL1 with an IC50 of 3.9 μM.
BCC5359 4SC-202 Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
BCC2195 Baricitinib (LY3009104, INCB028050) Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.
BCC1401 Baricitinib phosphate Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
BCC2452 EB 47 Potent PARP-1 inhibitor
BCC2430 UNC 0224 UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP
BCC7320 Tautomycetin
BCC8068 Cerdulatinib (PRT062070) Cerdulatinib (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.
BCC4569 Donepezil HCl Donepezil (Hydrochloride) (E-2020) is a noncompetitive acetylcholinesterase inhibitor, which can readily cross the blood brain barrier and increases the concentration of cortical acetylcholine.
BCC1504 CX-6258 CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
BCC2079 AZD1208 AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor.
BCC4145 GLPG0634 Filgotinib (GLPG0634) is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively.
BCC1422 BMN-673 8R,9S (8R,9S)-Talazoparib ((8R,9S)-BMN-673) is an enantiomer of Talazoparib, less active than Talazoparib on the inhibition of PARP1, with an IC50 of 144 nM.
BCC3604 3-Deazaneplanocin A (DZNep) hydrochloride 3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor.
BCC5575 ML324 ML324 is a potent JMJD2 demethylase inhibitor with demonstrated antiviral activity.
BCC8013 C 21 Selective PRMT1 inhibitor
BCC2200 LY2784544 Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.
BCC4142 UNC0321 UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
BCC5149 MG 149 MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50= 47 uM); little potent for PCAF and p300 (IC50 >200 uM).
BCC2418 TC-A 2317 hydrochloride Potent, selective Aurora kinase A inhibitor
BCC1135 UNC0638 UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively. UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities.
BCC2199 CEP-33779 CEP33779 is a selective JAK2 inhibitor with IC50 of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2.
BCC2443 TCS 21311 TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
BCC1603 GSK 525768A GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
BCC4474 I-BET-762 Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
BCC1132 Bromodomain Inhibitor, (+)-JQ1 (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
BCC3603 (-)-JQ1 (R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
BCC2185 ENMD-2076 L-(+)-Tartaric acid ENMD-2076 Tartrate 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.
BCC4476 I-BET151 (GSK1210151A) I-BET151 is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.
BCC4038 GSK1324726A 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).
BCC2217 Entacapone Entacapone is a specific, potent, peripherally acting catechol-O-methyltransferase (COMT) inhibitor with IC50 of 151 nM for PD treatment.
BCC3980 Sephin1
BCC3997 UNC669 UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).
BCC2438 Cercosporamide Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
BCC6460 ACY-241 Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects.
BCC2431 UNC 0646 UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
BCC4143 UNC 0631 UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM.
BCC2218 EPZ004777 EPZ004777 is a potent, selective DOT1L inhibitor with an IC50 of 0.4 nM.
BCC1505 CX-6258 hydrochloride hydrate CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.
BCC2435 ML 228 ML228 (CID-46742353) is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.
BCC4549 OG-L002 OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IE genes.
BCC2231 GSK J1 GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 of 60 nM towards KDM6B.
BCC2230 GSK J4 HCl Histone KDM inhibitor; cell permeable,GSK-J4 is a potent H3K27me3 demethylase inhibitor, with IC₅₀s of 8.6 µM and 6.6 µM towards KDM6B and KDM6A respectively.
BCC5524 CBB1003 CBB1003 is a novel histone demethylase LSD1 inhibitor with IC50 of 10.54 uM.
BCC4272 CBB1007 CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
BCC6426 BET bromodomain inhibitor CPI-0610 is a potent, selective, and cell-active BET inhibitor. CPI-0610 inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
BCC2215 EPZ5676 Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
BCC4550 EPZ004777 HCl
BCC7542 YM 750
BCC6264 GSK J5
BCC6263 GSK J2 GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
BCC4037 MS436 MS436 is a new class of bromodomain inhibitor, exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2.
BCC2219 EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
BCC6422 GSK2879552 GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
BCC2432 Chetomin
BCC3634 EPZ-6438 Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.
BCC2225 PFI-1 (PF-6405761) PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.
BCC5345 Nexturastat A Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.
BCC2436 PX 12 PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
BCC2023 UNC1215 UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
BCC4551 MM-102 MM-102 (HMTase Inhibitor IX) 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.
BCC5578 SP2509 SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with IC50 of 13 nM.
BCC5598 OXF BD 02
BCC5647 GSK-LSD1 2HCl
BCC4552 UNC1999 UNC1999 is a SAM-competitive, potent and selective inhibitor of EZH2/1 with IC50s of <10 nM and 45 nM, repectively.