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Results for "

Histone Methyltransferase

" in MedChemExpress (MCE) Product Catalog:

62

Inhibitors & Agonists

2

Screening Libraries

1

Fluorescent Dye

1

Biochemical Assay Reagents

8

Peptides

3

Natural
Products

8

Recombinant Proteins

3

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-136328
    EZM0414 TFA
    3 Publications Verification

    SETD2-IN-1 TFA

    		 Histone Methyltransferase Cancer
    EZM0414 TFA is a potent, selective and orally active inhibitor of SETD2 which is a human histone methyltransferase. EZM0414 TFA has anti-proliferative effects .
    EZM0414 TFA
  • HY-141430
    AS-85

    		Histone Methyltransferase Cancer
    AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 µM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 µM .
    AS-85
  • HY-121093
    DC-S239

    		Histone Methyltransferase Cancer
    DC-S239 is a selective histone methyltransferase SET7 inhibitor with an IC50 value of 4.59 μM. DC-S239 also displays selectivity for DNMT1, DOT1L, EZH2, NSD1, SETD8 and G9a. DC-S239 has anticancer activity .
    DC-S239
  • HY-10587A
    BIX-01294 hydrochloride hydrate

    		Histone Methyltransferase Apoptosis Autophagy Cancer
    BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells .
    BIX-01294 hydrochloride hydrate
  • HY-154854
    BBDDL2059

    		Histone Methyltransferase Cancer
    BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research .
    BBDDL2059
  • HY-141429
    AS-99 free base

    		Histone Methyltransferase Apoptosis Cancer
    AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
    AS-99 free base
  • HY-141429C
    AS-99

    		Histone Methyltransferase Apoptosis Cancer
    AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
    AS-99
  • HY-141429A
    AS-99 TFA

    		Histone Methyltransferase Apoptosis Cancer
    AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
    AS-99 TFA
  • HY-44062
    G9a-IN-1

    		Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
    G9a-IN-1
  • HY-12991A
    BIX-01338 hydrate

    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
    BIX-01338 hydrate
  • HY-15593
    Pinometostat
    15+ Cited Publications

    EPZ-5676

    		 Histone Methyltransferase Cancer
    Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.
    Pinometostat
  • HY-121493
    TM2-115

    		Histone Methyltransferase Parasite Infection
    TM2-115 inhibits malaria parasite histone methyltransferases, resulting in rapid and irreversible parasite death .
    TM2-115
  • HY-122182
    OTS193320

    		Histone Methyltransferase Apoptosis Cancer
    OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
    OTS193320
  • HY-114209
    MRK-740

    		Histone Methyltransferase Cancer
    MRK-740 is a potent, selective and substrate-competitive PRDM9 histone methyltransferase inhibitor with an IC50 of 80 nM. MRK-740 is more selective for PRDM9 than other histone methyltransferases and other non-epigenetic targets. MRK-740 reduces PRDM9-dependent trimethylation of H3K4 (IC50 = 0.8 µM) .
    MRK-740
  • HY-112445
    SGC3027
    3 Publications Verification

    		 Histone Methyltransferase Cancer
    SGC3027 is a histone methyltransferase inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .
    SGC3027
  • HY-142093
    NSD3-IN-1

    		Histone Methyltransferase Cancer
    NSD3-IN-1 (compound B1) is an inhibitor of histone methyltransferase NSD3 with an IC50 value of 28.58 μM .
    NSD3-IN-1
  • HY-100757
    CPUY074020

    		Histone Methyltransferase Cancer
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity .
    CPUY074020
  • HY-111390
    Dot1L-IN-2

    		Histone Methyltransferase Cancer
    Dot1L-IN-2 is a potent, selective and orally bioavailable inhibitor of Dot1L (a histone methyltransferase), with an IC50 and Ki of 0.4 nM and 0.08 nM, respectively.
    Dot1L-IN-2
  • HY-145813
    MU1656

    		Histone Methyltransferase Cancer
    MU1656 is a potent and selective inhibitor of histone methyltransferase DOT1L, with an IC50 of 2 nM. MU1656 can be used for the research of hematological malignancies .
    MU1656
  • HY-122936
    Tanshindiol C

    		Histone Methyltransferase Keap1-Nrf2 Sirtuin Cardiovascular Disease Cancer
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
    Tanshindiol C
  • HY-A0298
    EZH2-IN-2

    		Histone Methyltransferase Cancer
    EZH2-IN-2 is a EZH2 inhibitor extracted from patent WO2018133795A1, Compound Example 69, with an IC50 of 64 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .
    EZH2-IN-2
  • HY-148458
    EZH2-IN-14

    		Histone Methyltransferase Cancer
    EZH2-IN-14 is a selective EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 12 nM. EZH2-IN-14 inhibits the methyltransferase activity of EZH2/PRC2 (that is, reducing H3K27me3). EZH2-IN-14 shows >200-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 .
    EZH2-IN-14
  • HY-N2019
    Chaetocin
    4 Publications Verification

    		 Histone Methyltransferase Bacterial Antibiotic Infection Cancer
    Chaetocin is a specific inhibitor of the histone methyltransferase (HMT) SU(VAR)3-9 with an IC50 of 0.6 μM for SU(VAR)3-9. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM.
    Chaetocin
  • HY-13808
    UNC 0631
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    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 .
    UNC 0631
  • HY-15647
    BRD9539
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
    BRD9539
  • HY-10442
    3-Deazaneplanocin A
    Maximum Cited Publications
    22 Publications Verification

    DZNep; 3-Deazaneplanocin

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor. 3-Deazaneplanocin A shows anti-orthopoxvirus activity .
    3-Deazaneplanocin A
  • HY-12310
    RSC133

    		DNA Methyltransferase HDAC Others
    RSC133 exhibits dual activity by inhibiting histone deacetylase and DNA methyltransferase. RSC133 effectively facilitates reprogramming of human somatic cells to pluripotent stem cells and supports the maintenance of an undifferentiated state of human pluripotent stem cells .
    RSC133
  • HY-147230
    EZH2-IN-13

    		Histone Methyltransferase Cancer
    EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity .
    EZH2-IN-13
  • HY-15273
    UNC0638
    5+ Cited Publications

    		 VSV Histone Methyltransferase Autophagy Influenza Virus Infection Cancer
    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.
    UNC0638
  • HY-156455
    SETD7-IN-1

    		Histone Methyltransferase Cancer
    SETD7-IN-1 (compound 7) is a PFI-2 (HY-18627) analogue. SETD7-IN-1 is a substrate and inhibitor of histone lysine methyltransferase SETD7, with an IC50 of 0.96 ± 0.10 µM .
    SETD7-IN-1
  • HY-12186
    3-Deazaneplanocin A hydrochloride
    Maximum Cited Publications
    22 Publications Verification

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor . 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .
    3-Deazaneplanocin A hydrochloride
  • HY-117583
    cis-BG47

    		HDAC Histone Methyltransferase Neurological Disease
    cis-BG47 is an cis-isomer of BG47, BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. cis-BG47 can be used for neurological disease research .
    cis-BG47
  • HY-116971
    DCG066

    		Histone Methyltransferase Apoptosis Cancer
    DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .
    DCG066
  • HY-12186G
    3-Deazaneplanocin A hydrochloride

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    		 Histone Methyltransferase Orthopoxvirus Infection Cancer
    3-Deazaneplanocin A (DZNep) hydrochloride (GMP) is 3-Deazaneplanocin A hydrochloride (HY-12186) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 3-Deazaneplanocin A hydrochloride is a potent histone methyltransferase EZH2 inhibitor .
    3-Deazaneplanocin A hydrochloride
  • HY-135128
    Dot1L-IN-5

    		Histone Methyltransferase Cancer
    Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM .
    Dot1L-IN-5
  • HY-135129
    Dot1L-IN-6

    		Histone Methyltransferase Cancer
    Dot1L-IN-6 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.19 nM .
    Dot1L-IN-6
  • HY-135127
    Dot1L-IN-4

    		Histone Methyltransferase Cancer
    Dot1L-IN-4 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.11 nM .
    Dot1L-IN-4
  • HY-153390
    AMG-193

    		Histone Methyltransferase Cancer
    AMG-193 (compound 481) is an inhibitor of PRMT5. PRMT5-IN-27 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM .
    AMG-193
  • HY-160029
    PRMT5-IN-32

    		Histone Methyltransferase Cancer
    PRMT5-IN-32 is an inhibitor of PRMT5. PRMT5-IN-32 inhibits HCT116 cell proliferation with an IC 50 of 0.13 μM .
    PRMT5-IN-32
  • HY-N2345
    Procyanidin B3

    		Histone Acetyltransferase Cancer
    Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase) .
    Procyanidin B3
  • HY-16705
    BRD4770
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence .
    BRD4770
  • HY-10930
    UNC0321
    2 Publications Verification

    		 Histone Methyltransferase GCGR Apoptosis Cancer
    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 has anti-apoptotic activity and has potential application in diabetic vascular complications .
    UNC0321
  • HY-162003A
    DCPT1061 hydrochloride

    		Histone Methyltransferase Cancer
    DCPT1061 hydrochloride has a strong inhibitory effect on PRMT1, PRMT6, and PRMT8 in vitro, The epigenetic enzymes such as PRMT3, PRMT4 and PRMT5 had little inhibitory effect. DCPT1061 hydrochloride has antitumor effects .
    DCPT1061 hydrochloride
  • HY-111544
    EML741

    		Histone Methyltransferase Cancer
    EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated .
    EML741
  • HY-10929
    UNC0224
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    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 with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E .
    UNC0224
  • HY-125244
    LEM-14-1189

    		Histone Methyltransferase Cancer
    LEM-14-1189, a LEM-14 (HY-114340) derivative, is a NSDs inhibitor with IC50s of 418 μM (NSD1), 111 μM (NSD2), and 60 μM (NSD3), respectively. The NSDs, histone lysine methyltransferases (HMTases), are oncoproteins, drivers of a number of tumors. LEM-14-1189 can be used for multiple myeloma (MM) research .
    LEM-14-1189
  • HY-153331
    DDO-2213

    		WDR5 Cancer
    DDO-2213 is an orally active and potent WDR5-MLL1 inhibitor, with an IC50 of 29 nM and a Kd value of 72.9 nM for the WDR5 protein. DDO-2213 selectively inhibits MLL (mixed lineage leukemia) histone methyltransferase activity and the proliferation of MLL translocation-harboring cells. DDO-2213 can be used for MLL fusion leukemia research .
    DDO-2213
  • HY-156285
    ZZM-1220

    		Histone Methyltransferase Apoptosis Cancer
    ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase .
    ZZM-1220
  • HY-100201
    A-196
    4 Publications Verification

    		 Histone Methyltransferase Cancer
    A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
    A-196
  • HY-13807
    UNC0646
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    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 .
    UNC0646

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