Search Result
Results for "
PRMT5 Inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-153390
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Histone Methyltransferase
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Cancer
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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 .
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- HY-148674
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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-160029
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- HY-144187
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Histone Methyltransferase
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Cancer
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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 .
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- HY-144188
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Histone Methyltransferase
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Cancer
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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 .
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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-163593
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- HY-163592
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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-142211
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- HY-163589
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- HY-163590
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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-134883
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- HY-141875
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- HY-150081
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- HY-169708
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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-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 IC50 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-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-156680
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Histone Methyltransferase
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Cancer
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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 .
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- HY-132937
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- HY-158143
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- HY-111213
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- HY-163585
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- HY-163586
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- HY-163588
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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-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-132309
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BRD0639
1 Publications Verification
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Histone Methyltransferase
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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-141876
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Histone Methyltransferase
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Cancer
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PRMT5-IN-14 is a PRMT5 inhibitor to research cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
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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-126256
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Histone Methyltransferase
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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-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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- HY-126256A
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Histone Methyltransferase
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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-151576
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Histone Methyltransferase
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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-162989
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- HY-139611
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Histone Methyltransferase
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Cancer
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MRTX-1719 is a potent, orally active, selective PRMT5•MTA complex inhibitor, with IC50 of 3.6 and 20.5 nM for PRMT5•MTA and PRMT5. MRTX-1719 binds to the PRMT5•MTA complex, with KD value of 0.14 pM. MRTX-1719 shows antineoplastic activity in vitro and in vivo, and can be used for cancer study .
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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-112165
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- HY-139611C
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Histone Methyltransferase
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Cancer
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MRTX-1719 hydrochloride is a potent first-in-class selective inhibitor of the PRMT5/MTA complex, with an IC50 of less than 10 nM in PRMT5/MTA MTAP DEL SDMA cells .
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- HY-131493
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PRMT5-IN-3
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Histone Methyltransferase
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Cancer
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PF-06939999 (PRMT5-IN-3) is a PRMT5 inhibitor that exhibits synthetic lethality to tumor cells but produce few side effects combined with DNA damaging agents.
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- HY-107777
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LLY-283
3 Publications Verification
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Histone Methyltransferase
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Cancer
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LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
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- HY-124131
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DS-437
1 Publications Verification
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Histone Methyltransferase
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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-141877
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MS4322
1 Publications Verification
YS43-22
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PROTACs
Histone Methyltransferase
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Cancer
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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 )) .
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- HY-153421
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Histone Methyltransferase
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Cancer
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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 .
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- HY-141877B
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YS43-22 (isomer)
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PROTACs
Histone Methyltransferase
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Cancer
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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 )) .
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- HY-138684
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- HY-138684A
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- HY-12727
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- HY-100025A
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- HY-128579
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Histone Methyltransferase
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Cancer
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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 .
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- HY-100025
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- HY-100235
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EPZ015866; GSK3203591
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Histone Methyltransferase
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Cancer
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GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM .
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- HY-100235A
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EPZ015866 hydrochloride; GSK3203591 hydrochloride
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Histone Methyltransferase
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Cancer
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GSK591 (EPZ015866) hydrochloride is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM .
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- HY-139611B
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Histone Methyltransferase
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Cancer
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(S)-MRTX-1719 (example 16-7) is the S-enantiomer of MRTX-1719. (S)-MRTX-1719 is a PRMT5/MTA complex inhibitor, with an IC50 of 7070 nM .
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- HY-153390A
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Histone Methyltransferase
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Cancer
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(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 .
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- HY-148419
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TNG908
1 Publications Verification
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Histone Methyltransferase
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Cancer
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TNG908 is a MTAP synergistic PRMT5 inhibitor. TNG908 crosses the blood-brain barrier and is orally active. TNG908 could be used in cancer research .
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- HY-120137
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Histone Methyltransferase
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Cancer
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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 .
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- HY-113846
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Histone Methyltransferase
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Cancer
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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 .
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- HY-113846A
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Histone Methyltransferase
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Cancer
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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 .
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- HY-109963
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- HY-162783
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Histone Methyltransferase
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Cancer
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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 .
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- HY-107777A
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Histone Methyltransferase
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Cancer
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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 .
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- HY-101564
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JNJ-64619178
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Histone Methyltransferase
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Cancer
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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 .
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- HY-169218
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BCL6
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Cancer
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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. .
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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-155051
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Apoptosis
Histone Methyltransferase
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Cancer
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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 .
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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-100855
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Histone Methyltransferase
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Cancer
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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 .
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- HY-101563
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GSK3326595
Maximum Cited Publications
20 Publications Verification
EPZ015938
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Histone Methyltransferase
SARS-CoV
MDM-2/p53
CDK
Apoptosis
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Infection
Cancer
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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 .
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- HY-148817
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WDR5
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Cancer
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WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5 .
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- HY-110137A
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DB75; NSC 305831
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Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-110137
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DB75 dihydrochloride; NSC 305831 dihydrochloride
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Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
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Infection
Inflammation/Immunology
Cancer
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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 .
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- HY-147081
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AGRO-100
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Histone Methyltransferase
Bcl-2 Family
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Cancer
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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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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 |
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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Cat. No. |
Product Name |
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Classification |
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- HY-147081
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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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