Search Result
Results for "
PRMTs
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-139611
-
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MRTX-1719; BMS-986504
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Histone Methyltransferase
|
Cancer
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Navlimetostat is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
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-
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- HY-19615
-
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Histone Methyltransferase
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Cancer
|
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MS023, a chemical probe, is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively .
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- HY-128717A
-
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EPZ019997 dihydrochloride
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Histone Methyltransferase
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Cancer
|
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GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
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-
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- HY-12970A
-
|
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Histone Methyltransferase
Apoptosis
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Cancer
|
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EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer .
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-
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- HY-128717
-
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EPZ019997
|
Histone Methyltransferase
|
Cancer
|
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GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
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-
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- HY-107777
-
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Histone Methyltransferase
|
Cancer
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LLY-283, a chemical probe, 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 .
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-
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- HY-18962
-
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Histone Methyltransferase
|
Cancer
|
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AMI-1 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 exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
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-
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- HY-12970
-
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Histone Methyltransferase
Apoptosis
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Cancer
|
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EPZ020411 is a selective inhibitor of PRMT6 with an IC50 of 10 nM, has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 can be used for the research of cancer .
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-
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- HY-19615B
-
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Histone Methyltransferase
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Cancer
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MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively .
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- HY-173561
-
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PROTACs
Histone Methyltransferase
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Cancer
|
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MS115 is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 promotes PRMT5/MEP50 ubiquitination and degradation. MS115 shows anticancer activity against breast cancer .
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- HY-151576
-
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Histone Methyltransferase
|
Cancer
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PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells .
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- HY-139611C
-
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MRTX-1719 hydrochloride; BMS-986504 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
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Navlimetostat hydrochloride is a potent, orally active, selective PRMT5-MTA complex inhibitor, with IC50s of 3.6 and 20.5 nM for PRMT5-MTA and PRMT5. Navlimetostat hydrochloride binds to the PRMT5-MTA complex, with KD value of 0.14 pM. Navlimetostat shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
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- HY-173557
-
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Histone Methyltransferase
Apoptosis
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Cancer
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PRMT7-IN-2 (A33) is a selective PRMT7 inhibitor with an IC50 of 0.50 μM. PRMT7-IN-2 arrests cell cycle at G0/G1 phase, induces cell apoptosis, and inhibits cell growth in vivo and in vitro. PRMT7-IN-2 decreases the monomethylarginine level of PRMT7, increases expression of epithelial marker (E-cadherin, and reduces expression of mesenchymal markers such as N-cadherin, Vimentin, and ZEB2 .
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-
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- HY-111213
-
-
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- HY-132309
-
BRD0639
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
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BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities .
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- HY-112165
-
-
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- HY-124131
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DS-437
1 Publications Verification
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
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DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3 .
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- HY-18962A
-
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Histone Methyltransferase
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Cancer
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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 .
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- HY-W280124
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-
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- HY-Q36691
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-30 (compound 17) is a potent and selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.33 μM and a Kd of 0.987 μM. PRMT5-IN-30 exhibits a broad selectivity against a panel of other methyltransferases. PRMT5-IN-30 inhibits PRMT5 mediated SmD3 methylation .
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- HY-147185
-
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Histone Methyltransferase
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Cancer
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PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells .
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- HY-160865
-
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Histone Methyltransferase
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Cancer
|
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PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC50 value of 1 nM. PRMT5-IN-35 can be used in cancer research .
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- HY-126256A
-
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Histone Methyltransferase
|
Cancer
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PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
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- HY-159728
-
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PROTACs
Histone Methyltransferase
Apoptosis
Early 2 Factor (E2F)
c-Myc
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Cancer
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PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia .
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- HY-152236
-
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Histone Methyltransferase
Apoptosis
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Cancer
|
PRMT6-IN-3 (compound 25) is a selective PRMT6 inhibitor with an IC50 value of 192 nM. PRMT6-IN-3 can induce apoptosis in cancer cells and has anticancer activity .
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- HY-172769
-
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Histone Methyltransferase
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Cancer
|
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CM112 is a selective protein arginine methyltransferase 1 (PRMT1) degrader by tethering hydrophobic tag, adamantane, to MS023 with a 5-PEG linker. CM112 induces the degradation of PRMT1 in various solid cancer cell lines. CM112 can also target the nonenzymatic function of PRMT1 by downregulating the stability of the orphan receptor TR3. CM112 is promising for research of cancers .
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- HY-134883
-
-
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- HY-155050
-
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Apoptosis
Histone Methyltransferase
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Cancer
|
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PRMT5-IN-31 (Compound 3m) is a selective PRMT5 inhibitor (IC50: 0.31 μM). PRMT5-IN-31 up-regulates hnRNP E1 protein level. PRMT5-IN-31 occupies the substrate site of PRMT5 and forms essential interactions with amino acid residues. PRMT5-IN-31 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. PRMT5-IN-31 has high metabolic stability on human liver microsomes (T1/2: 132.4 min) .
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- HY-136809
-
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Histone Methyltransferase
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Cancer
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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.
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- HY-158143
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-
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- HY-126256
-
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Histone Methyltransferase
|
Cancer
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PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
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- HY-174983
-
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Histone Methyltransferase
|
Cancer
|
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PRMT5-MTA-IN-6 (Compound 31) is a selective MTA-cooperative PRMT5 inhibitor. PRMT5-MTA-IN-6 exhibits potent inhibitory activity against PRMT5・MTA (IC50: 6.6 nM). PRMT5-MTA-IN-6 selectively inhibits the growth of MTAP-deleted HCT-116 cells (IC50: 319 nM). PRMT5-MTA-IN-6 can be used in the research of MTAP-deleted tumors .
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- HY-175821
-
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Histone Methyltransferase
Apoptosis
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Cancer
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PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC50s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC .
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- HY-176231
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- HY-178028
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
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- HY-176702
-
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Histone Methyltransferase
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Cancer
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PRMT5-MTA-IN-5 (Compound 7) is an orally active, irreversible PRMT5-MTA complex (PRMT5•MTA) inhibitor (IC50=1.15 nM). PRMT5-MTA-IN-5 blocks arginine methylation and inhibits ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-5 potently inhibits proliferation in MTAP-deficient tumor cells. PRMT5-MTA-IN-5 is promising for research of MTAP-deficient solid tumors, such as liver, breast, and pancreatic cancers .
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- HY-168263
-
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Histone Methyltransferase
Apoptosis
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Cancer
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PRMT5-IN-45 (compound 36) is a potent and selective PRMT5 inhibitor with an IC50 of 3 nM. PRMT5-IN-45 potently reduces the level of symmetric dimethylarginines (sDMA) and inhibits the proliferation of MOLM-13 cell lines by inducing apoptosis and cell cycle arrest .
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- HY-176534
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma .
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- HY-176701
-
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Histone Methyltransferase
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Cancer
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PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma .
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- HY-111030
-
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Histone Methyltransferase
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Cancer
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PRMT1-IN-2 (RM65) is a potent PRMT1 inhibitor with an IC50 of 55.4 μM. PRMT1-IN-2 shows histone hypomethylation in HepG2 cells .
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- HY-162003A
-
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Histone Methyltransferase
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Cancer
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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 .
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- HY-155154
-
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Histone Methyltransferase
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Cancer
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PRMT4-IN-2 (compound 55) is a pan-inhibitor of protein arginine methyltransferase (PRMT) with IC50s of 92 nM (PRMT4), 436 nM (PRMT6), 460 nM (PRMT1), 823 nM ( PRMT8), 1.386 μM (PRMT3) .
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- HY-155154A
-
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Histone Methyltransferase
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Cancer
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PRMT4-IN-3 (compound 56) is a potent inhibitor of class I protein arginine methyltransferase (PRMT), targeting PRMT4 (IC50: 37 nM) and PRMT4 (IC50: 253 nM) .
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- HY-178274
-
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Histone Methyltransferase
Apoptosis
|
Cancer
|
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SKLB06329 is a potent selective Type I PRMTs inhibitor. SKLB06329 shows good selectivity for PRMT6 (IC50 = 3.86 nM) over Type II/III PRMTs (PRMT5/7) and shows no significant inhibition against various lysine methyltransferases (PKMTs). SKLB06329 significantly inhibits the proliferation of triple-negative breast cancer (TNBC) cells, induces apoptosis, and suppresses the expression of asymmetric dimethylarginine (ADMA) within cells. SKLB06329 can be used for triple-negative breast cancer research .
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- HY-18962R
-
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Histone Methyltransferase
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Cancer
|
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AMI-1 (Standard) is the analytical standard of AMI-1. This product is intended for research and analytical applications. AMI-1 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 exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
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- HY-18962AR
-
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Histone Methyltransferase
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Cancer
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AMI-1 (free acid) (Standard) is the analytical standard of AMI-1 (free acid). This product is intended for research and analytical applications. 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 .
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- HY-159732
-
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Histone Methyltransferase
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Cancer
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PRMT3-IN-4 (intermediate 15) is a protein arginine methyltransferase 3 (PRMT3) inhibitor. PRMT3-IN-4 is an active control for HY-19715. PRMT3-IN-4 can be used to synthesize PROTACs targeting PRMT3. PRMT3-IN-4 can be used in leukemia-related research .
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- HY-171132
-
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Histone Methyltransferase
|
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PRMT3-IN-5 (Compound 14) is an allosteric PRMT3 inhibitor (IC50: 291 nM). PRMT3-IN-5 can be used for investigating PRMT3's biological functions and disease associations .
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- HY-163592
-
-
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- HY-163593
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- HY-163587
-
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Histone Methyltransferase
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Cancer
|
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PRMT5-IN-39-d3 is the deuterated form of PRMT5-IN-39. PRMT5-IN-39-d3 is an orally active PRMT5 inhibitor and can be used for study of cancer .
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- HY-163591
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research .
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- HY-168842
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity .
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- HY-162003
-
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Histone Methyltransferase
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Cancer
|
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DCPT1061 potently inhibits PRMT1, PRMT6 and PRMT8 in vitro with less inhibitory effect on PRMT3, PRMT4, and PRMT5 or other epigenetic enzymes. DCPT1061 has antitumor effect .
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- HY-115758
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-
- HY-160029
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- HY-146810
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- HY-162230
-
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Apoptosis
Histone Methyltransferase
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Cancer
|
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PRMT5-IN-33 (compound A8) is a selective, SAM-competitve PRMT5 inhibitors with IC50 of 10.9 nM. PRMT5-IN-33 induces apoptosis and inhibits proliferation of cells Z-138 and MOLM-13. PRMT5-IN-33 exhibits an antitumor activity .
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- HY-153422
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-29 is a potent and orally active PRMT5 Inhibitor with an IC50 of 1.5 μΜ. PRMT5-IN-29 has the potential for advanced cancers research .
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- HY-170603
-
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Fluorescent Dye
Histone Methyltransferase
Apoptosis
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Cancer
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PRMT5-targeted fluorescent ligand-1 (Compound 7) is a PRMT5-targeted fluorescent ligand, that inhibits PRMT5 with an IC50 of 29.39 nM. PRMT5-targeted fluorescent ligand-1 exhibits cell imaging activity, that exhibits good fluorescence signal in MCF-7 with an IC50 of 29 nM. PRMT5-targeted fluorescent ligand-1 induces apoptosis. PRMT5-targeted fluorescent ligand-1 exhibits a maximal excitation wavelength of 438 nm and a maximal emission wavelength of 550 nm .
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- HY-19615A
-
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Histone Methyltransferase
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Cancer
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MS023 trihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively .
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- HY-141874
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- HY-163590
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- HY-144189
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-18 (Compound 002) is a potent PRMT5 inhibitor that can be used for the research of a disease mediated by PRMT5, such as cancer .
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- HY-139823
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- HY-163799
-
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Histone Methyltransferase
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Cancer
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PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
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- HY-149005
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
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- HY-142211
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- HY-163589
-
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- HY-153057
-
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Histone Methyltransferase
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Metabolic Disease
Cancer
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PRMT5-IN-46 (compound 278) inhibits PRMT5 with IC50s of 1-10 μM. PRMT5 is a methyltransferase which is associated with specific genetic alterations. PRMT5-IN-46 can be used for research of proliferative diseases, metabolic disorders, and blood diseases .
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- HY-139823A
-
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Histone Methyltransferase
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Others
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PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
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- HY-141875
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- HY-169708
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- HY-150081
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- HY-172732
-
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Histone Methyltransferase
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Cancer
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PRMT5-IN-50 is an orally active and selective inhibitor of PRMT5. PRMT5-IN-50 has good metabolic stability and low clearance rate in human liver microsomes. PRMT5-IN-50 inhibits SDMA/HCT116-MTAPdel and SDMA/HCT116-MTAPwt with IC50s value of 1.0, 536 nM for arginine symmetric methylation, 19, 1620 nM for anti-proliferation, respectively. PRMT5-IN-50 inhibits tumor growth in mice .
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- HY-163434
-
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EGFR
Histone Methyltransferase
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Cancer
|
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PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
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- HY-168142
-
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Histone Methyltransferase
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Cancer
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YD1130 is a PRMT4 inhibitor (0.5 nM, 75% inhibition rate), and its inhibitory potency against other PRMTs is not significant (PRMT5 IC50> 1 μM, PRMT1/3/6/7/8 IC50 > 10 μM). .
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- HY-132937
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- HY-172733S
-
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Isotope-Labeled Compounds
Histone Methyltransferase
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Cancer
|
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
|
-
- HY-170792
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-48 (compound D3) is an orally effective PRMT5 inhibitor (IC50=20.7 nM) with anticancer activity. PRMT5-IN-48 can inhibit the growth of various cancer cells, induce apoptosis (apoptosis), and arrest the cell cycle at the G0/G1 phase. PRMT5-IN-48 can be used for non-Hodgkin lymphoma (NHL) research .
|
-
- HY-172197
-
-
- HY-144188
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-17 (Compound 6) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
|
-
- HY-144187
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-16 (Compound 20) is a PRMT5 inhibitor with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
|
-
- HY-163585
-
-
- HY-163586
-
-
- HY-128717C
-
|
EPZ019997 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC50 values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity .
|
-
- HY-172733
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective protein arginine methyltransferase 5 (PRMT5) inhibitor. PRMT5-MTA-IN-3 inhibits cell proliferation in the MTAP-deficient colorectal cancer HCT - 116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 is promising for research of cancers, especially for MTAP-deficient tumors, such as colorectal cancer, non-small cell lung cancer, pancreatic cancer .
|
-
- HY-P3822
-
|
|
Histone Methyltransferase
|
Cancer
|
PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
|
-
- HY-162989
-
-
- HY-128717B
-
|
EPZ019997 trihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
|
-
- HY-113846A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 dihydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 dihydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 dihydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected .
|
-
- HY-180816
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-7 (Compound 14) is a selective PRMT5-MTA inhibitor. PRMT5-MTA-IN-7 exhibits KD values of PRMT5-MTA-IN-7 for PRMT5-MTA and PRMT5-SAM of 236 nM and 2.84 μM respectively, and the IC50 values of 4.08 and 13.6 μM respectively. PRMT5-MTA-IN-7 can selectively inhibit the proliferation of MTAP-deficient cancer cells. PRMT5-MTA-IN-7 can be used for the study of colon cancer .
|
-
- HY-180356
-
-
- HY-181260
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PRMT5-MTA-IN-8 is an orally active PRMT5-MTA complex inhibitor (IC50 = 4.4 nM). PRMT5-MTA-IN-8 inhibits the intracellular production of symmetric dimethylarginine (SDMA) as well as the proliferation of MTAP-deficient cells. PRMT5-MTA-IN-8 exerts antitumor efficacy by inhibiting PRMT5, reducing SDMA levels and inducing tumor cell apoptosis in mouse models of triple-negative breast cancer. PRMT5-MTA-IN-8 can be used in research related to cancers such as triple-negative breast cancer .
|
-
- HY-182297
-
-
- HY-181294
-
-
- HY-173561A
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 TFA promotes PRMT5/MEP50 ubiquitination and degradation. MS115 TFA shows anticancer activity against breast cancer .
|
-
- HY-182275
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
|
-
- HY-182298
-
-
- HY-183061
-
|
|
LYTACs
Epigenetic Reader Domain
|
Neurological Disease
Cancer
|
|
MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC50 values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma .
|
-
- HY-120137
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected .
|
-
- HY-113846
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected .
|
-
- HY-122096
-
DCLX069
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects .
|
-
- HY-155814
-
-
- HY-138684
-
-
- HY-138684A
-
-
- HY-131493
-
|
PRMT5-IN-3
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect .
|
-
- HY-114510
-
|
|
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 .
|
-
- HY-182892
-
|
|
Histone Demethylase
Histone Methyltransferase
|
Cancer
|
|
MC4491 is a selective LSD1/PRMT5 inhibitor, with an IC50 of 0.152 μM against the LSD1/CoREST complex and an IC50 of 0.043 μM against the PRMT5/MEP50 complex. MC4491 induces transcriptomic changes and splicing alterations in AML cells. MC4491 is applicable for the research of acute myeloid leukemia .
|
-
- HY-139611B
-
|
(S)-MRTX-1719; (S)-BMS-986504
|
Histone Methyltransferase
|
Cancer
|
|
(S)-Navlimetostat (example 16-7) is the S-enantiomer of Navlimetostat. (S)-Navlimetostat is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM .
|
-
- HY-153421
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-28 (compound 36) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme. Protein arginine methylation is a common post-translational modification involved in gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape .
|
-
- HY-181522
-
-
- HY-110137A
-
|
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 .
|
-
- HY-178114
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
SKLB-0124 is a selective PRMT6 degrader with DC50s of 15.4 μM and a 16.4 μM in HCC827 and MDA-MB-435 cells. SKLB-0124 does not degrade PRMT1 or PRMT8. SKLB-0124 exhibits an IC50 on PRMT6 of 1.6 μM. SKLB-0124 induces proteasome dependent degradation of PRMT6 and significantly inhibits the proliferation. SKLB-0124 effectively induces apoptosis and cell cycle arrest. SKLB-0124 can be used for the studies of lung cancer and breast cancer .
|
-
- HY-110137
-
|
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 .
|
-
- HY-19714
-
XY1
1 Publications Verification
|
Drug Derivative
|
Cancer
|
|
XY1 is an analog of SGC707 (HY-19715), a potent and selective PRMT3 inhibitor with an IC50 of 31 nM. XY1 is completely inactive against PRMT3. XY1 and SGC707 represent an excellent pair of tools for further elucidating the biological functions and disease relevance of PRMT3 .
|
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-110137R
-
|
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 .
|
-
- HY-RS11177
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT6 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT6 Human Pre-designed siRNA Set A
PRMT6 Human Pre-designed siRNA Set A
- HY-RS11186
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT9 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT9 Human Pre-designed siRNA Set A
PRMT9 Human Pre-designed siRNA Set A
- HY-RS11170
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT2 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT2 Human Pre-designed siRNA Set A
PRMT2 Human Pre-designed siRNA Set A
- HY-RS11173
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt3 Rat Pre-designed siRNA Set A
Prmt3 Rat Pre-designed siRNA Set A
- HY-RS11171
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT3 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT3 Human Pre-designed siRNA Set A
PRMT3 Human Pre-designed siRNA Set A
- HY-RS11185
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt8 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt8 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt8 Rat Pre-designed siRNA Set A
Prmt8 Rat Pre-designed siRNA Set A
- HY-RS19732
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt2 Mouse Pre-designed siRNA Set A
Prmt2 Mouse Pre-designed siRNA Set A
- HY-RS11181
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt7 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt7 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt7 Mouse Pre-designed siRNA Set A
Prmt7 Mouse Pre-designed siRNA Set A
- HY-RS11172
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt3 Mouse Pre-designed siRNA Set A
Prmt3 Mouse Pre-designed siRNA Set A
- HY-RS11183
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT8 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT8 Human Pre-designed siRNA Set A
PRMT8 Human Pre-designed siRNA Set A
- HY-RS20467
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt9 Mouse Pre-designed siRNA Set A
Prmt9 Mouse Pre-designed siRNA Set A
- HY-RS11169
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt1 Rat Pre-designed siRNA Set A
Prmt1 Rat Pre-designed siRNA Set A
- HY-RS11174
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT5 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT5 Human Pre-designed siRNA Set A
PRMT5 Human Pre-designed siRNA Set A
- HY-RS11168
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt1 Mouse Pre-designed siRNA Set A
Prmt1 Mouse Pre-designed siRNA Set A
- HY-RS26976
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt9 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt9 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt9 Rat Pre-designed siRNA Set A
Prmt9 Rat Pre-designed siRNA Set A
- HY-RS11184
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt8 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt8 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt8 Mouse Pre-designed siRNA Set A
Prmt8 Mouse Pre-designed siRNA Set A
- HY-RS11175
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt5 Mouse Pre-designed siRNA Set A
Prmt5 Mouse Pre-designed siRNA Set A
- HY-RS26228
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt2 Rat Pre-designed siRNA Set A
Prmt2 Rat Pre-designed siRNA Set A
- HY-RS11179
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT6 Rat Pre-designed siRNA Set A contains three designed siRNAs for PRMT6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT6 Rat Pre-designed siRNA Set A
PRMT6 Rat Pre-designed siRNA Set A
- HY-RS11180
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT7 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT7 Human Pre-designed siRNA Set A
PRMT7 Human Pre-designed siRNA Set A
- HY-RS11176
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt5 Rat Pre-designed siRNA Set A
Prmt5 Rat Pre-designed siRNA Set A
- HY-RS11178
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt6 Mouse Pre-designed siRNA Set A
Prmt6 Mouse Pre-designed siRNA Set A
- HY-RS11167
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
PRMT1 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
PRMT1 Human Pre-designed siRNA Set A
PRMT1 Human Pre-designed siRNA Set A
- HY-RS11182
-
|
|
Small Interfering RNA (siRNA)
|
Others
|
|
Prmt7 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt7 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
|
-
Prmt7 Rat Pre-designed siRNA Set A
Prmt7 Rat Pre-designed siRNA Set A
- HY-173092
-
-
- HY-100855
-
|
|
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 .
|
-
- HY-162783
-
|
|
Histone Methyltransferase
|
Cancer
|
|
AZ-PRMT5i-1 (Compound 28) is an effective and orally active MTAP-selective PRMT5 inhibitor. AZ-PRMT5i-1 also demonstrates MTA cooperativity and exhibits both in vitro and in vivo antitumor activities, and can be used to study MTAP-deficient cancers .
|
-
- HY-107777R
-
|
|
Reference Standards
Histone Methyltransferase
|
Cancer
|
|
LLY-283 (Standard) is the analytical standard of LLY-283 (HY-107777). This product is intended for research and analytical applications. LLY-283, a chemical probe, 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 .
|
-
- HY-141877B
-
|
YS43-22 (isomer)
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-173562
-
-
- HY-158157
-
|
|
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 .
|
-
- HY-12970B
-
|
|
Histone Methyltransferase
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Cancer
|
|
EPZ020411 dihydrochloride is a selective, blood-brain barrier-permeable PRMT6 inhibitor with an IC50 of 0.010 μM. EPZ020411 dihydrochloride blocks PRMT6-mediated histone H3R2 methylation, reduces ROS production, and inhibits Apoptosis. EPZ020411 dihydrochloride is applicable to research related to neuropathic pain, colorectal cancer, ototoxicity, hearing loss and glioblastoma .
|
-
- 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 .
|
-
- HY-178102
-
|
|
Drug Derivative
|
Cancer
|
|
SKLB-0266 is the negative control of SKLB-0124 (HY-178114) (a PRMT6 inhibitor). SKLB-0266 after undergoing methylation modification completely loses its inhibitory activity against PRMT6 .
|
-
- HY-100565A
-
|
|
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 .
|
-
- HY-168143
-
|
|
Histone Methyltransferase
|
Cancer
|
|
YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
|
-
- HY-181521
-
-
- HY-114211
-
|
|
Histone Methyltransferase
HSP
|
Cancer
|
|
SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity .
|
-
- HY-182891
-
|
|
Histone Demethylase
|
Cancer
|
|
MC4455 is a LSD1/PRMT5 dual inhibitor. MC4455 inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC50 values of 0.104 μM and 0.014 μM. MC4455 covalently binds to LSD1’s FAD cofactor, stabilizes the LSD1/CoREST complex. MC4455 induces myeloid differentiation, alters transcriptomic profiles, drives alternative splicing changes, and impairs leukemic cell viability in AML cells. MC4455 can be used for the research of acute myeloid leukemia .
|
-
- HY-110158
-
-
- HY-W072962
-
|
|
Histone Methyltransferase
PAK
Bcl-2 Family
KLF
|
Cancer
|
|
WX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer .
|
-
- HY-128579
-
|
|
Histone Methyltransferase
|
Cancer
|
|
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity .
|
-
- HY-12727
-
-
- HY-186045
-
|
|
Histone Methyltransferase
Apoptosis
DNA/RNA Synthesis
ATP-binding cassette (ABC) transporters
|
Cancer
|
|
SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-100025A
-
-
- 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 .
|
-
- HY-163588
-
-
- HY-100025
-
-
- HY-126300
-
-
- HY-100565R
-
|
|
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 .
|
-
- HY-100360A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-100235A
-
|
EPZ015866 hydrochloride; GSK3203591 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
GSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM .
|
-
- HY-141876
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRT543 is a PRMT5 inhibitor to research cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
|
-
- HY-100360
-
MS049
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-100235
-
|
EPZ015866; GSK3203591
|
Histone Methyltransferase
|
Cancer
|
|
GSK591 (EPZ015866), a chemical probe, is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM .
|
-
- HY-15890
-
-
- HY-153390A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
(R)-AMG-193 is an isomer of AMG 193 (HY-153390). 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 .
|
-
- HY-148674
-
-
- HY-133740
-
|
|
Histone Methyltransferase
|
Cancer
|
|
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM .
|
-
- HY-112445
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SGC3027 is a histone methyltransferase inhibitor . SGC3027 is the first potent, selective and cell active chemical probe for PRMT7 .
|
-
- HY-174445
-
|
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker) .
|
-
- HY-114965
-
|
|
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 .
|
-
- HY-W013500
-
|
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.
|
-
- HY-126300A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SGC6870N is inactive against PRMT6 and can be utilized as a negative control. SGC6870N is an inactive enantiomer of SGC6870 (HY-126300) .
|
-
- HY-183653
-
|
|
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 .
|
-
- HY-148419
-
|
TNG908
|
Histone Methyltransferase
|
Cancer
|
|
TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research .
|
-
- HY-19715
-
-
- HY-100360R
-
|
|
Histone Methyltransferase
Reference Standards
|
Cancer
|
|
MS049 (Standard) is the analytical standard of MS049 (HY-100360). This product is intended for research and analytical applications. MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
|
-
- HY-159733
-
-
- HY-117927
-
|
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 .
|
-
- HY-109963
-
-
- HY-156680
-
|
TNG-462
|
Histone Methyltransferase
|
Cancer
|
|
TNG-462 is an orally active and selective PRMT5 inhibitor with anti-tumor activity against methylthioadenosine phosphorylase (MTAP) deficiency and/or methylthioadenosine (MTA) accumulation cancers .
|
-
- HY-164456
-
-
- HY-107777A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases .
|
-
- HY-101564
-
|
JNJ-64619178
|
Histone Methyltransferase
|
Cancer
|
|
Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer .
|
-
- HY-164497
-
|
|
DNA/RNA Synthesis
Histone Methyltransferase
|
Cancer
|
|
NSC 641396 is a ribonucleotide reductase (RNR) inhibitor with an IC50 value of 1.2 μM. NSC 641396 is also a protein arginine N-methyltransferase 9 (PRMT9) inhibitor. NSC 641396 has antitumor activity .
|
-
- HY-174908
-
|
|
Histone Methyltransferase
11β-HSD
Androgen Receptor
|
Cancer
|
|
SJL2-1 is a PRMT5 inhibitor, with an IC50 of 1.56 μM. SJL2-1 suppresses proliferation, migration, and invasion in prostate cancer cells. SJL2-1 promotes apoptosis and blocks the cell cycle at the G0/G1 phase. SJL2-1 can target the binding of PRMT5 in cells and inhibit the methylation and expression of the androgen receptor. SJL2-1 can be used for the study of early androgen-sensitive prostate cancer and advanced castration-resistant prostate cancer (CRPC) .
|
-
- HY-100025AR
-
|
|
Histone Methyltransferase
Reference Standards
Apoptosis
|
Cancer
|
|
HLCL-61 (hydrochloride) (Standard) is the analytical standard of HLCL-61 (hydrochloride) (HY-100025A). This product is intended for research and analytical applications. HLCL-61 hydrochloride is a first-in-class inhibitor of protein arginine methyltransferase 5 (PRMT5).
|
-
- HY-157388
-
|
|
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 .
|
-
- HY-169218
-
|
|
BCL6
|
Cancer
|
|
WK692 is a BCL6 inhibitor that inhibits the BCL6 BTB/SMRT interaction. WK692 can effectively inhibit the growth of diffuse large B-cell lymphoma cells and synergize with EZH2 and PRMT5 inhibitors. .
|
-
- HY-155051
-
|
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
|
Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
|
-
- HY-100235R
-
|
EPZ015866 (Standard); GSK3203591 (Standard)
|
Histone Methyltransferase
Reference Standards
|
Cancer
|
|
GSK591 (Standard) is the analytical standard of GSK591 (HY-100235). This product is intended for research and analytical applications. GSK591 (EPZ015866), a chemical probe, is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM .
|
-
- HY-157151
-
|
|
Histone Methyltransferase
|
Cancer
|
|
iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively .
|
-
- HY-N2420R
-
-
- HY-N2420
-
-
- HY-101564R
-
|
JNJ-64619178 (Standard)
|
Histone Methyltransferase
Reference Standards
|
Cancer
|
|
Onametostat (Standard) is the analytical standard of Onametostat (HY-101564). This product is intended for research and analytical applications. Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. Onametostat has potent activity in lung cancer .
|
-
- HY-107777AR
-
|
|
Histone Methyltransferase
Reference Standards
|
Cancer
|
|
LLY-284 (Standard) is the analytical standard of LLY-284 (HY-107777A). This product is intended for research and analytical applications. LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases .
|
-
- HY-138993
-
|
|
Amine N-methyltransferase
|
Cancer
|
|
NNMT-IN-6 is a selective nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 can be used for the research of oral cancer .
|
-
- HY-101563
-
GSK3326595
Maximum Cited Publications
31 Publications Verification
EPZ015938
|
Histone Methyltransferase
SARS-CoV
MDM-2/p53
CDK
Apoptosis
|
Infection
Cancer
|
|
GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma .
|
-
- HY-138993A
-
|
|
Amine N-methyltransferase
|
Cancer
|
|
NNMT-IN-6 hydrochloride is a selective nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 hydrochloride inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 hydrochloride can be used for the research of oral cancer .
|
-
- 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 .
|
-
- HY-182820
-
|
|
Histone Methyltransferase
PROTACs
KLF
|
Cancer
|
|
YZ-836P is a Protein arginine methyltransferase 5 (PRMT5) targeting agent. YZ-836P promotes ubiquitination and proteasomal degradation of PRMT5 in a cereblon (CRBN)-dependent manner, which in turn reduces levels of its downstream target KLF5. YZ-836P induces G1 phase cell cycle arrest in triple-negative breast cancer cells. YZ-836P induces Apoptosis in triple-negative breast cancer cells. YZ-836P exerts cytotoxic effects on triple-negative breast cancer cells. YZ-836P inhibits the growth of triple-negative breast cancer patient-derived organoids. YZ-836P inhibits the growth of triple-negative breast cancer xenografts in nude mice. YZ-836P can be used for the research of triple-negative breast cancer .
|
-
- 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 .
|
-
- HY-101563R
-
|
EPZ015938 (Standard)
|
Histone Methyltransferase
Reference Standards
SARS-CoV
MDM-2/p53
CDK
Apoptosis
|
Infection
Cancer
|
|
GSK3326595 (Standard) is the analytical standard of GSK3326595 (HY-101563). This product is intended for research and analytical applications. GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma .
|
-
- HY-161334
-
|
|
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 .
|
-
- HY-168497
-
|
|
Histone Methyltransferase
|
Cancer
|
|
C-MS023 is a photo-activatable MS023 (HY-19615) prodrug, achieving spatiotemporal inhibition of Histone Arginine Asymmetric Dimethylation. C-MS023 inhibits PRMT6 mediated asymmetric dimethylation of H3 arginine 2 (H3R2me2a), with an estimate IC50 of 0.2224 μM. The photolysis of C-MS023 could be triggered by visible light irradiation at 420 nm, thereby liberating MS023 for effective downregulation of histone arginine asymmetric dimethylation and DNA replication-related transcriptomic activities .
|
-
- HY-12759
-
|
|
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 .
|
-
- HY-12759A
-
|
|
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 .
|
-
- HY-107574
-
|
|
Histone Methyltransferase
AP-1
NF-κB
PKA
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers .
|
-
- HY-147081
-
AS 1411
2 Publications Verification
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
-
- HY-178446
-
|
|
METTL3
c-Myc
Bcl-2 Family
|
Cancer
|
|
METTL3-IN-11 is an excellent, selective METTL3 inhibitor (IC50 = 45.31 nM). METTL3-IN-11 exhibits high selectivity towards METTL3 compared to DNMT1, EZH1, MLL1, and PRMT1. METTL3-IN-11 reduces the m6A level of total RNA in MOLM-13 and SKOV3 cells, induces cell apoptosis, and inhibits cell migration. METTL3-IN-11 can reduce the expression of m6A downstream target genes (c-MYC and BCL2). METTL3-IN-11 can be used for the study of ovarian cancer and acute myeloid leukemia .
|
-
- HY-147081A
-
|
AGRO-100 sodium
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
|
-
- HY-107574R
-
|
|
Reference Standards
Histone Methyltransferase
AP-1
NF-κB
PKA
|
Metabolic Disease
Inflammation/Immunology
Cancer
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TC-E 5003 (Standard) is the analytical standard of TC-E 5003 (HY-107574). This product is intended for research and analytical applications. TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein Kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers .
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- HY-172159
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HDAC
Apoptosis
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Cancer
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FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3822
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Histone Methyltransferase
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Cancer
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PRMT5-IN-23 (compound 50) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) with anti-tumor activity. PRMT5 is a type of protein arginine methyltransferase, and is a new anti-tumor target related to epigenetic modification .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-163587
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PRMT5-IN-39-d3 is the deuterated form of PRMT5-IN-39. PRMT5-IN-39-d3 is an orally active PRMT5 inhibitor and can be used for study of cancer .
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- HY-163591
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PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research .
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- HY-172733S
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PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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| Cat. No. |
Product Name |
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Classification |
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- HY-147081
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AS 1411
2 Publications Verification
AGRO-100
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Aptamers
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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- HY-147081A
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AGRO-100 sodium
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Aptamers
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AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
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- HY-RS11173
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11174
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siRNAs
Human Pre-designed siRNA Sets
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PRMT5 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11180
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siRNAs
Human Pre-designed siRNA Sets
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PRMT7 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11167
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siRNAs
Human Pre-designed siRNA Sets
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PRMT1 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11177
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siRNAs
Human Pre-designed siRNA Sets
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PRMT6 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11186
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siRNAs
Human Pre-designed siRNA Sets
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PRMT9 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11170
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siRNAs
Human Pre-designed siRNA Sets
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PRMT2 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11171
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siRNAs
Human Pre-designed siRNA Sets
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PRMT3 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11185
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt8 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt8 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS19732
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11181
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt7 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt7 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11172
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11183
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siRNAs
Human Pre-designed siRNA Sets
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PRMT8 Human Pre-designed siRNA Set A contains three designed siRNAs for PRMT8 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS20467
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11169
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11168
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11184
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt8 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt8 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11175
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11176
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11178
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siRNAs
Mouse Pre-designed siRNA Sets
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Prmt6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Prmt6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11182
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt7 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt7 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS26976
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt9 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt9 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS26228
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siRNAs
Rat Pre-designed siRNA Sets
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Prmt2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Prmt2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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- HY-RS11179
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siRNAs
Rat Pre-designed siRNA Sets
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PRMT6 Rat Pre-designed siRNA Set A contains three designed siRNAs for PRMT6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
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