Histone Methyltransferase
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB03941 | XY1 | 1624117-53-8 | XY1 is a negative control of SGC 707 which works as a potent and selective allosteric inhibitor of PRMT3, while XY1 shows almost no activity. |
| FB10073 | UNC3866 | 1872382-47-2 | UNC3866 is a high-affinity CBX4 and CBX7 inhibitor with Ki values of 94 and 97 nM, respectively. |
| FB03265 | UNC0642 | 1481677-78-4 | UNC0642 is a selective inhibitor of G9a/GLP with IC50 of < 15 nM. |
| FB12726 | UNC 0638 hydrate | 1255517-77-1 | UNC0638 is an inhibitor of protein lysine methyltransferases G9a and GLP with IC50 of < 15 nM, 19 nM, respectively. |
| FB03937 | UNC0379 Trifluoroacetate | 1620401-83-3 | UNC0379 trifluoroacetate is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 μM and is selective over 15 other methyltransferases. |
| FB12718 | TP 064 | 2080306-20-1 | TP-064 is a potent and selective PRMT4 inhibitor. The in vitro activity of TP-064 includes inhibition of PRMT4 with IC50 < 10nM for methylation of H3 (1-25) and greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In cellular assays, TP-064 inhibits the methylation of MED12 with IC50 = 43 nM. |
| FB12398 | TC-E 5003 | 17328-16-4 | TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor. |
| FB10263 | SGC2085 | 1821908-48-8 | SGC2085 is a selectivel and potent CARM1 inhibitor with IC50 value of 50 nM. |
| FB03299 | SGC0946 | 1561178-17-3 | SGC0946 is a selective inhibitor of DOT1L methyltransferase with IC50 of 0.3 nM and can kill mixed lineage leukaemia cells. |
| FB17710 | SAH-EZH2 | 1453222-26-8 | SAH-EZH2 is a EZH2-targeting stapled peptide that selectively inhibits H3 Lys27 trimethylation by dose-responsively disrupting the EZH2/EED complex and reducing EZH2 protein levels, a mechanism distinct from that reported for small molecule EZH2 inhibitors targeting the enzyme catalytic domain. |
| FB12678 | Ryuvidine | 265312-55-8 | Ryuvidine is an inhibitor of SETD8 with cellular activity. It also acts as a CDK4 inhibitor and inducer of the DNA damage response. |
| FB10823 | PRMT5 Inhibitor C17 | 330951-01-4 | PRMT5 inhibitor C17 is a potent, selective, and cell active protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50 = 0.33 μM) exhibited a broad selectivity against a panel of other methyltransferases. |
| FB03943 | PFI-2 | 1627676-59-8 | PFI-2 is an a first-in-class, potent, highly selective, and cell-active inhibitor of the methyltransferase activity of SETD7 with IC50 of 2 nM, 500 fold active than (S)-PFI-2. |
| FB18281 | NSD2-PWWP1 antagonist 3f | 1210906-48-1 | NSD2-PWWP1 antagonist 3f can bind to the NSD2-PWWP1 domain with Kd value of 3.4μM and abrogates histone H3K36me2 binding to the PWWP1 domain in cells. |
| FB17568 | ms1943 | 2225938-17-8 | MS1943 is a first-in-class EZH2 selective degrader that effectively reduces EZH2 levels in cells. |
| FB10220 | MS049 2HCl | 2095432-59-8 | MS049 2HCl is a potent and selective inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. |
| FB04025 | MS023 | 1831110-54-3 | MS023 is a potent and selective chemical probe for Type I PRMTs with IC50 values of 30, 119, 83, 8, and 8 nM for PRMTs 1,3,4,6,and 8, respectively. MS023 is active in cells. |
| FB10262 | MS049 | 1502816-23-0 | MS 049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC 50 of 34 nM and 43 nM respectively. |
| FB11203 | MM-589 Trifluoroacetate | 2253167-09-6 | MM-589 trifluoroacetate is a potent inhibitor of the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) interaction, and may yield a therapy for acute leukemia. |
| FB11202 | MM-589 | 2097887-20-0 | MM-589 is a potent inhibitor of the WD repeat domain 5 protein (WDR5)–mixed lineage leukemia (MLL) interaction, and may yield a therapy for acute leukemia. |
| FB10264 | MM-102 Trifluoroacetate | 1883545-52-5 | MM-102 trifluoroacetate 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. |
| FB04009 | LLY-507 | 1793053-37-8 | LLY-507 is a potent and selective protein-lysine methyltransferase SMYD2 inhibitor with IC50 <15 nM, which can inhibit p53K370 monomethylation in cells with an IC50 ~600 nM. |
| FB12043 | LLY-283 | 2040291-27-6 | LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity. |
| FB12277 | JQEZ5 | 1913252-04-6 | JQEZ5 is a potent and selective SAM-competitive EZH2 lysine methyltransferase inhibitor with IC50 of 11 nM. |
| FB20372 | JNJ-64619178 | 2086772-26-9 | JNJ-64619178 is a selective, orally active, and pseudo-irreversible inhibitor of protein arginine methyltransferase 5 (IC50: 0.14 nM). It has effective activity In lung cancer. |
| FB03934 | GSK591 | 1616391-87-7 | GSK591 is a potent and selective inhibitor of H4 histone methylation by PRMT5/MEP50 complex. |
| FB12823 | GSK3326595 | 1616392-22-3 | GSK3326595 is a potent, specific and reversible PRMT5 inhibitor which can decrease the levels of both monomethylated and dimethylated arginine residues in histones H2A, H3 and H4. |
| FB12166 | GSK2807 Trifluoroacetate | 2245255-66-5 | GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM. |
| FB10003 | GNA002 | 1385035-79-9 | GNA002 binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination. |
| FB10002 | Gambogenic Acid | 173932-75-7 | Gambogenic acid binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination. |
| FB12583 | Furamidine 2HCl | 55368-40-6 | Furamidine 2HCl is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 μM. |
| FB11833 | EZM 2302 | 1628830-21-6 | EZM 2302 is the first potent and selective inhibitor of CARM1 enzymatic activity with IC50 value of 6 nM. |
| FB10272 | EPZ031686 | 2095161-11-6 | EPZ031686 is a noncompetitive inhibitor for SMYD3 and MEKK2 with a Ki=1.2 nM and 1.1 nM respectively. |
| FB03980 | EPZ020411 | 1700663-41-7 | EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. |
| FB09983 | EPZ020411 HCl | 2070015-25-5 | EPZ020411 HCl is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has > 10 fold selectivity for PRMT6 over PRMT1 and PRMT8. |
| FB10200 | EPZ020411 2HCl | 2095432-47-4 | EPZ020411 2HCl is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM. |
| FB03311 | EPZ011989 Trifluoroacetate | 1598383-41-5 | EPZ011989 trifluoroacetate is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646, exhibiting 15-fold selectivity over EZH1 and > 3000-fold selectivity over other HMTase. |
| FB10787 | EPZ011989 HCl | 2095432-26-9 | EPZ011989 HCl is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of < 3 nM. |
| FB03192 | EI1 | 1418308-27-6 | EI1 is a selective inhibitor of wild type EZH2 and EZH2 Y641F mutant with IC50 values of 15 nM and 13 nM, respectively. |
| FB11541 | EBI-2511 | 2098546-05-3 | EBI-2511 is a Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma. EBI-2511 showed enzymatic activity and cellular activity of 4.0 and 6.0nM, respectively. EBI-2511 demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations. |
| FB10216 | Chaetocin | 28097-03-2 | Chaetocin, a natural product from Chaetomium species, is a histone methyltransferase inhibitor with IC50 of 0.8 μM, 2.5 μM and 3 μM for dSU (VAR)3-9, mouse G9a and Neurospora crassa DIM5, respectively. It also inhibits thioredoxin reductase (TrxR) with an IC50 of 4 μM. |
| FB10266 | CARM1-IN-1 HCl | 2070018-31-2 | CARM1-IN-1 HCl is a potent and specific CARM1 (Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 μM and shows very low activity against PRMT1 and SET7 (IC50 > 600 μM). |
| FB12237 | C 21 | 1229236-78-5 | C 21 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 1.8 μM. |
| FB15352 | BCI-121 | 432529-82-3 | BCI-121 (BCI121) is a substrate-competitive inhibitor of SMYD3 that inhibits SMYD3-substrate interaction and chromatin recruitment It can significantly reduce the proliferation of various cancer cells. |
| FB11931 | BAY-598 | 1906919-67-2 | BAY-598 is an inhibitor of SMYD2. It can inhibit in vitro methylation of p53 at lysine 370 with IC50 value of 27 nM. |
| FB17774 | AMI-1 free acid | 134-47-4 | AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding. |
| FB11171 | A-893 | 1868232-32-9 | A-893 is a potent and selective SMYD2 inhibitor (IC50: 2.8 nM). |
| FB11751 | A-395 | 2089148-72-9 | A-395 is a antagonist of Polycomb repressive complex 2 (PRC2) protein–protein interactions that potently inhibits the trimeric PRC2 complex (EZH2–EED–SUZ12) with an IC50 of 18 nM. |
| FB03279 | A-366 | 1527503-11-2 | A-366 is a peptide-competitive inhibitor of G9a/GLP with IC50 of ~3 nM. |
| FB10389 | A-196 | 1982372-88-2 | A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50s of 25 and 144 nM respectively. |