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Results for "

Histone Methyltransferase

" in MedChemExpress (MCE) Product Catalog:

113

Inhibitors & Agonists

4

Screening Libraries

2

Fluorescent Dyes

2

Biochemical Assay Reagents

14

Peptides

2

Natural
Products

11

Recombinant Proteins

19

Antibodies

1

Click Chemistry

2

GMP Molecules

Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-15593
    Pinometostat
    25+ 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-10442
    3-Deazaneplanocin A
    Maximum Cited Publications
    35 Publications Verification

    DZNep; 3-Deazaneplanocin

    Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Metabolic Disease Inflammation/Immunology 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-136328
    EZM0414 TFA
    5+ Cited Publications

    SETD2-IN-1 TFA

    Histone Methyltransferase Cancer
    EZM0414 (SETD2-IN-1) TFA is the TFA salt form of EZM0414 (HY-144858). EZM0414 TFA is a potent, selective, orally active inhibitor of SETD2 (IC50=18 nM in SETD2 biochemical assay; IC50=34 nM in cellular assay). EZM0414 TFA can be used for the research of relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma .
    EZM0414 TFA
  • HY-153390

    Histone Methyltransferase Cancer
    AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
    AMG-193
  • HY-154812

    KTX-1001

    Histone Methyltransferase CD44 Cancer
    Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM .Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .
    Gintemetostat
  • HY-112445
    SGC3027
    5+ Cited Publications

    Histone Methyltransferase Cancer
    SGC3027 is a histone methyltransferase inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .
    SGC3027
  • HY-N2019
    Chaetocin
    5+ Cited Publications

    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-12186
    3-Deazaneplanocin A hydrochloride
    Maximum Cited Publications
    35 Publications Verification

    DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride

    Histone Methyltransferase S-adenosylhomocysteine hydrolase (SAHH) Orthopoxvirus Infection Inflammation/Immunology 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-100201
    A-196
    10+ Cited Publications

    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-12583
    A-366
    5+ Cited Publications

    Histone Methyltransferase Epigenetic Reader Domain Cancer
    A-366, a chemical probe, is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
    A-366
  • HY-15273
    UNC0638
    10+ Cited Publications

    VSV Histone Methyltransferase Autophagy Influenza Virus Infection Cancer
    UNC0638, a chemical probe, selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets .
    UNC0638
  • HY-12220
    MM-102
    4 Publications Verification

    HMTase Inhibitor IX

    WDR5 Apoptosis NF-κB TNF Receptor Interleukin Related Inflammation/Immunology Cancer
    MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
    MM-102
  • HY-13808
    UNC 0631
    5 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-16705
    BRD4770
    5 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-10929
    UNC0224
    2 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-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-141429A
    AS-99 TFA
    2 Publications Verification

    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-141539
    SETDB1-TTD-IN-1
    5 Publications Verification

    Histone Methyltransferase Akt Cancer
    SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .
    SETDB1-TTD-IN-1
  • HY-148458

    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-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-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
  • HY-122182

    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 (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-A0298

    Histone Methyltransferase Cancer
    EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .
    EZH2-IN-2
  • HY-135127
    Dot1L-IN-4
    1 Publications Verification

    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-13808R

    Reference Standards Histone Methyltransferase Cancer
    UNC 0631 (Standard) is the analytical standard of UNC 0631. This product is intended for research and analytical applications. 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 (Standard)
  • HY-121093

    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-12310

    DNA Methyltransferase HDAC MDM-2/p53 Others Inflammation/Immunology
    RSC133 is a dual inhibitor of DNA methyltransferase 1 and histone deacetylase 1 inhibitor. RSC133 promotes cell proliferation, up-regulates H3K9 histone acetylation, down-regulates p53, p21, p16/INK4A, and ablates pro-senescence phenotypes .
    RSC133
  • HY-12991A

    Histone Methyltransferase Cancer
    BIX-01338 hydrate is a histone lysine methyltransferase inhibitor.
    BIX-01338 hydrate
  • HY-114209
    MRK-740
    2 Publications Verification

    Histone Methyltransferase Cancer
    MRK-740, a chemical probe, 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-100757

    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-135128
    Dot1L-IN-5
    2 Publications Verification

    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-133121

    Apoptosis WDR5 Cancer
    WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .
    WDR5-IN-1
  • HY-19554A
    MM-401 TFA
    1 Publications Verification

    WDR5 Apoptosis Cancer
    MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
    MM-401 TFA
  • HY-168992

    Histone Methyltransferase Neurological Disease Cancer
    UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC50 of 3.4 μM and a Kd of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases .
    UNC6535
  • HY-141430

    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-44062

    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-P10948A

    WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia .
    CS-VIP 8 hydrochloride
  • HY-153331

    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

    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-P2254

    Histone Methyltransferase Cancer
    H3K27(Me3) (15-34), a histone peptide, is a repressive chromatin mark derived from human histone. Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me) .
    H3K27(Me3) (15-34)
  • HY-19554

    WDR5 Apoptosis Cancer
    MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
    MM-401
  • HY-141429
    AS-99 free base
    2 Publications Verification

    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-148817

    WDR5 Cancer
    WDR5-0102 is an inhibitor of WDR5. WDR5-0102 specifically targets the WIN site of WDR5, disrupts the WDR5-MLL1 interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer .
    WDR5-0102
  • HY-172614

    RK-552

    Histone Methyltransferase Apoptosis Cancer
    RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
    RK-0080552
  • HY-125244

    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-P10463

    Histone Methyltransferase Cancer
    ssK36 is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2), and ssK36 is designed for the SETD2 protein, a specific PKMT. ssK36 is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36
  • HY-W516880

    O-Demethylastemizole

    Drug Metabolite Parasite Histamine Receptor Potassium Channel Infection Cardiovascular Disease
    Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC50 of 0.12, 0.11 and 0.06  μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K + channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research .
    Desmethylastemizole
  • HY-122936

    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-P10948

    WDR5 Histone Methyltransferase Cardiovascular Disease
    CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .
    CS-VIP 8
  • HY-P10463A

    Histone Methyltransferase Cancer
    ssK36 TFA is a supersubstrate peptide of the histone methyltransferase (SET) domain protein 2 (SETD2) , and ssK36 TFA is designed for the SETD2 protein, a specific PKMT. ssK36 TFA is responsible in human cells for adding methyl groups to the 36th lysine residue of histone H3 (H3K36) to form H3K36me3. ssK36 TFA can be methylated by SETD2 at a rate more than 100 times faster than the natural substrate H3K36. ssK36 TFA can be used to study the catalytic mechanism of PKMTs, especially substrate specificity and catalytic efficiency .
    ssK36 TFA

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