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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
16 Results for "
PRMT5-MTA
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "PRMT5-MTA" in MCE Product Catalog:
3
3 Cited Publications
Synonyms: MRTX-1719; BMS-986504
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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 .
3
3 Cited Publications
Cat. No.: HY-139611C
Purity: 99.22%
Synonyms: MRTX-1719 hydrochloride; BMS-986504 hydrochloride
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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 .
1
1 Cited Publications
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MRTX9768 is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .
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1 Cited Publications
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MRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor .
Synonyms: (S)-MRTX-1719; (S)-BMS-986504
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(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 .
Cat. No.: HY-176702
CAS No.: 3078322-88-7
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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 .
Cat. No.: HY-174983
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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 .
Cat. No.: HY-176701
CAS No.: 3025838-18-7
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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 .
Cat. No.: HY-163799
CAS No.: 3048425-88-0
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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 .
Cat. No.: HY-172733S
CAS No.: 3052146-54-7
Cat. No.: HY-181260
CAS No.: 3105952-57-3
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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 .
Cat. No.: HY-172733
CAS No.: 3028674-29-2
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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 .
Cat. No.: HY-180816
CAS No.: 303969-88-2
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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 .
Cat. No.: HY-162989
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PRMT5-MTA-IN-2 (compund 1) is a MTA co-inhibitor of PRMT5 with IC50 less than 1.5 nM .
Cat. No.: HY-184434
CAS No.: 3064280-41-4
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PRMT5-IN-57 is an orally active andselective MTA-cooperative PRMT5 inhibitor, with an IC50 of 8.39 nM against PRMT5/MTA complex. PRMT5-IN-57 exhibits potent and selective antiproliferative activity against MTAP-null cancer cells. PRMT5-IN-57 demonstrates significant in vivo antitumor efficacy in an HCT116 MTAP-/- CDX model. PRMT5-IN-57 can be used for the research of MTAP-deleted cancers .
Cat. No.: HY-184290
CAS No.: 3062852-59-6
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PRMT5-IN-56 is a PRMT5⋅MTA complex inhibitor with an IC50 of 0.2 nM, oral activity, and blood-brain barrier penetration. PRMT5-IN-56 inhibits PRMT5 methyltransferase activity in an MTA-cooperative manner, suppresses symmetrical dimethylarginine levels in MTAP-deficient cells. PRMT5-IN-56 suppresses proliferation of MTAP-deleted cancer cells with high selectivity over MTAP-wild type cells. PRMT5-IN-56 induces dose-dependent tumor growth inhibition in subcutaneous xenograft models, inhibits intracranial tumor progression, and prolongs survival in orthotopic brain xenograft models. PRMT5-IN-56 exhibits high intrinsic permeability, good oral bioavailability, and a high brain-to-plasma ratio. PRMT5-IN-56 can be used for the research of MTAP-deleted cancers and glioblastoma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
