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CARM1 inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114965
    TP-064
    5+ Cited Publications

    		 Histone Methyltransferase Inflammation/Immunology Cancer
    TP-064, a chemical probe, is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities .
    TP-064
  • HY-111109
    EZM 2302
    Maximum Cited Publications
    12 Publications Verification

    		 Histone Methyltransferase Cancer
    EZM 2302 is a potent and orally active CARM1 inhibitor with an IC50 value of 6 nM. EZM 2302 shows antiproliferative activity and anti-tumor activity. EZM 2302 inhibits PABP1 and SMB expression .
    EZM 2302
  • HY-110137
    Furamidine dihydrochloride
    3 Publications Verification

    DB75 dihydrochloride; NSC 305831 dihydrochloride

    		 Histone Methyltransferase Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology Cancer
    Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
    Furamidine dihydrochloride
  • HY-100565
    SGC2085
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
    SGC2085
  • HY-12759
    CARM1-IN-1
    4 Publications Verification

    		 Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1
  • HY-12759A
    CARM1-IN-1 hydrochloride
    4 Publications Verification

    		 Histone Methyltransferase Cancer
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
    CARM1-IN-1 hydrochloride
  • HY-156152A
    CARM1 degrader-1 hydrochloride

    		PROTACs Histone Methyltransferase Cancer
    CARM1 degrader-1 hydrochloride is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 hydrochloride degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 hydrochloride inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 hydrochloride can be used in breast cancer research .
    CARM1 degrader-1 hydrochloride
  • HY-163561
    CARM1-IN-6

    		Histone Methyltransferase Estrogen Receptor/ERR IFNAR Cancer
    CARM1-IN-6 is a potent CARM1 inhibitor that inhibits CARM1 enzymatic activity with an IC50 of 12.3 μM and a Kd of 0.6785 μM. CARM1-IN-6 suppresses oncogenic estrogen/ERα-target gene expression, activates type I interferon (IFN) and IFN-induced genes (ISGs), induces cell cycle arrest, and inhibits breast cancer cell proliferation both in vitro and in vivo. CARM1-IN-6 can be used for the research of breast cancer .
    CARM1-IN-6
  • HY-156152
    CARM1 degrader-1

    		PROTACs Histone Methyltransferase Cancer
    CARM1 degrader-1 is a CARM1 PROTAC degrader (DC50 = 8.1 nM) with high selectivity over other protein arginine methyltransferases. CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in cell-based assays. CARM1 degrader-1 inhibits cancer cell migration in cell-based assays. CARM1 degrader-1 can be used for the research of breast cancer .
    CARM1 degrader-1
  • HY-110137A
    Furamidine

    DB75; NSC 305831

    		 Histone Methyltransferase Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology Cancer
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
    Furamidine
  • HY-15214A
    CARM1-IN-3 dihydrochloride

    		Histone Methyltransferase Cancer
    CARM1-IN-3 dihydrochloride (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
    CARM1-IN-3 dihydrochloride
  • HY-157388
    CARM1/HDAC2-IN-1

    		Histone Methyltransferase HDAC Cancer
    CARM1/HDAC2-IN-1 (compound CH-1) is a dual inhibitor against CARM1 and HDAC2, with IC50 values of 3.71 nM and 4.07 nM, respectively. CARM1/HDAC2-IN-1 possesses antitumor activity .
    CARM1/HDAC2-IN-1
  • HY-100565A
    SGC2085 hydrochloride

    		Histone Methyltransferase Cancer
    SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
    SGC2085 hydrochloride
  • HY-136809
    PRMT6-IN-2

    		Histone Methyltransferase Cancer
    PRMT6-IN-2 (compound 2) is a dual inhibitor of protein arginine methyltransferase PRMT6 and CARM1 with an IC50 of 30 nM. PRMT6 is abnormally expressed in many cancer cells, and PRMT6-IN-2-based derivatives have potential anticancer activity.
    PRMT6-IN-2
  • HY-161334
    CARM1-IN-4

    		Histone Methyltransferase Apoptosis Cancer
    CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC50s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity .
    CARM1-IN-4
  • HY-156153
    CARM1 degrader-2

    		Histone Methyltransferase Cancer
    PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
    CARM1 degrader-2
  • HY-172368
    PROTAC CARM1/IKZF3 degrader-1

    		PROTACs Histone Methyltransferase IKZF Family Apoptosis Inflammation/Immunology Cancer
    PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research . (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
    PROTAC CARM1/IKZF3 degrader-1
  • HY-117927
    EPZ0025654

    GSK3536023

    		 Histone Methyltransferase Cancer
    EPZ0025654 (GSK3536023) is an inhibitor for protein arginine methyltransferases 4 (PRMT4) (which is also known as coactivator associated arginine methyltransferase 1 CARM1), with IC50 of 3 nM .
    EPZ0025654
  • HY-158157
    ZL-28-6

    		Histone Methyltransferase Cancer
    ZL-28-6 is a type I PRMT inhibitor (IC50: 18 nM). ZL-28-6 effectively targets CARM1 (a member of PRMT) within cells and can be used for cancer research .
    ZL-28-6
  • HY-158158
    CARM1-IN-5

    		Histone Methyltransferase Cancer
    CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines .
    CARM1-IN-5
  • HY-132885
    PARP/EZH2-IN-1

    		PARP Histone Methyltransferase Cancer
    PARP/EZH2-IN-1 is a first-in-class dual PARP-1/EZH2 inhibitor with IC50 values of 6.87 nM and 36.51 nM, respectively. PARP/EZH2-IN-1 induces autophagy in cancer cells and shows potent antiproliferative activity in BRCA wild-type triple-negative breast cancer cells .
    PARP/EZH2-IN-1
  • HY-172369
    CARM1/IKZF3 ligand 1

    		Histone Methyltransferase Ligands for Target Protein for PROTAC Cancer
    CARM1/IKZF3 ligand 1 is the inhibitor for CARM1 that can be used as the target protein ligand for synthesis of PROTAC CARM1/IKZF3 degrader-1 (HY-172368) .
    CARM1/IKZF3 ligand 1
  • HY-15214
    CARM1-IN-3

    		Histone Methyltransferase Cancer
    CARM1-IN-3 (compound 17b) is a potent and selective co-activator associated arginine methyltransferase (CARM1) inhibitor with IC50 values of 0.07, >25 µM for CARM1 and CARM3, respectively .
    CARM1-IN-3
  • HY-100855
    DC_C66

    		Histone Methyltransferase Cancer
    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5 .
    DC_C66
  • HY-114206
    SKI-73

    		Histone Methyltransferase Cancer
    SKI-73 is a chemical probe for CARM1 with prodrug properties. SKI-73 can rapidly penetrate cell membranes and be processed into active inhibitors. SKI-73 inhibits the invasion of breast cancer cells and can be used in the study of cancer .
    SKI-73
  • HY-W013500
    (1-Nitroethene-1,2-diyl)dibenzene

    alpha-Nitrostilbene; α-Nitrostilbene; NSC 385

    		 Histone Methyltransferase Others
    (1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
    (1-Nitroethene-1,2-diyl)dibenzene
  • HY-163561A
    CARM1-IN-6 dihydrochloride

    		Histone Methyltransferase Cancer
    CARM1-IN-6 (Compound iCARM1) dihydrochloride is an effective and selective inhibitor of CARM1 with an IC50 value of 12.3 μM. CARM1-IN-6 dihydrochloride exhibits cell growth inhibitory activity and can be used in cancer research .
    CARM1-IN-6 dihydrochloride
  • HY-110137R
    Furamidine dihydrochloride (Standard)

    DB75 dihydrochloride (Standard); NSC 305831 dihydrochloride (Standard)

    		 Histone Methyltransferase Phosphodiesterase (PDE) Parasite Reference Standards Infection Inflammation/Immunology Cancer
    Furamidine (dihydrochloride) (Standard) is the analytical standard of Furamidine (dihydrochloride). This product is intended for research and analytical applications. Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
    Furamidine dihydrochloride (Standard)
  • HY-183653
    AK442

    		Histone Methyltransferase Cancer
    AK442 is a selective PRMT4 (CARM1) inhibitor with an IC50 of 2.6 nM against human targets. AK442 is applicable to breast cancer-related research .
    AK442
  • HY-100565R
    SGC2085 (Standard)

    		Histone Methyltransferase Reference Standards Cancer
    SGC2085 (Standard) is the analytical standard of SGC2085 (HY-100565). This product is intended for research and analytical applications. SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins .
    SGC2085 (Standard)
  • HY-114510
    PRMT/HKMT-IN-1

    		Discoidin Domain Receptor Histone Acetyltransferase Sirtuin Fungal Apoptosis Infection Cancer
    PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .
    PRMT/HKMT-IN-1

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