mta

MRTX-1719 is a potent and selective inhibitor of the PRMT5/MTA complex with an IC50 value of <10 nM against PRMT5/MTAMTAPDELSDMA cell lines.

4-Methyl-2-oxopentanoic acid is an abnormal metabolite, a neurotoxin and a metabolic toxin.

PRMT5-MTA-IN-2 (compound 1) is a synergistic inhibitor of PRMT5 with an IC50 of less than 1.5 nM.

PRMT5-MTA-IN-3 (Compound P2A) is an orally active and selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It inhibits the proliferation of MTAP-deficient colorectal cancer HCT-116 cell line with an IC50 value of 5 nM. PRMT5-MTA-IN-3 holds potential for research in cancers, particularly in MTAP-deficient tumors such as colorectal cancer, non-small cell lung cancer, and pancreatic cancer.

PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor of the protein arginine methyltransferase PRMT5-MTA. It suppresses the proliferation of colorectal cancer cells HCT116, both wild-type and MTAP del mutants, with IC50 values of 16 nM and 2.47 μM, respectively. Additionally, PRMT5-MTA-IN-1 demonstrates favorable hepatic microsomal stability, membrane permeability, and pharmacokinetic properties in CD-1 mice.

PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible inhibitor of protein arginine methyltransferase 5 (PRMT5) with an IC50 of 8 nM. It obstructs arginine methylation, hinders ribosomal RNA processing, and suppresses cell cycle-related protein expression. This compound shows antiproliferative activity in various tumor cell lines, exemplified by an IC50 of 0.3 μM in DLD-1 cells. PRMT5-MTA-IN-4 holds potential for research into hematological malignancies such as acute myeloid leukemia and diffuse large B-cell lymphoma.

PRMT5-MTA-IN-5 (Compound 7) is an orally active, irreversible inhibitor of the PRMT5-MTA complex (PRMT5•MTA) with an IC50 value of 1.15 nM. It effectively blocks arginine methylation, impedes the processing of ribosomal RNA, and suppresses the expression of proteins related to the cell cycle. PRMT5-MTA-IN-5 significantly inhibits the proliferation of tumor cells lacking MTAP and shows potential for research into MTAP-deficient solid tumors, such as liver, breast, and pancreatic cancers.

PRMT5-MTA-IN-6 (Compound 31) is a selective inhibitor of PRMT5 in conjunction with MTA, exhibiting potent inhibitory activity against PRMT5・MTA with an IC50 of 6.6 nM. It selectively inhibits the growth of MTAP-deficient HCT-116 cells with an IC50 of 319 nM and is useful for studying MTAP-deficient tumors.

Umtatin is a useful organic compound for research related to life sciences and the catalog number is T125576.

TrimTAC1 is a PROTAC degrader that selectively targets the polyprotein Nucleoporin for degradation.

212Pb-DOTAMTATE is a bifunctional ligand used to prepare Pb212-complex and serves as a targeted alpha radiation therapy for metastatic neuroendocrine tumors that express SSTR. It may have significant clinical implications when used alone or in combination with chemotherapeutic compounds.

LYMTAC-2 is a lysosome-targeting chimera (LYMTAC) developed to degrade membrane-associated proteins through lysosomal membrane proteins (LMP) such as RNF152, LAPTM4a, and LAPTM5. It forms a ternary complex with target proteins like KRASG12D, facilitating their relocation to lysosomes and resulting in ubiquitin-dependent degradation. This compound has potential for studying membrane protein regulation and devising strategies to counter resistance in KRAS-driven signaling pathways.

HEMTACWEE1degrader-1 is a WEE1-targeting heterobifunctional chimeric degrader (HEMTAC) facilitated by HSP90, exhibiting an HSP90 enzyme inhibitory activity with an IC50 of 16.76 nM. It enhances the ubiquitination and subsequent degradation of WEE1, effectively blocking the G2/M cell cycle transition. This compound shows anticancer properties in patient-derived xenograft (PDX) models of acute myeloid leukemia (AML). HEMTACWEE1degrader-1 is utilized in AML research.

RNA MTase-IN-1 (Compound 47) is an inhibitor of RNA methyltransferase (RNA MTase), exhibiting an IC50 of 68 μM against 16S rRNA (m1A1408) methyltransferase (NpmA). It demonstrates significant inhibitory activity against aminoglycoside resistance linked to pathogens and is applicable in research on antibiotic-resistant bacterial infections.

Cinnamtannin B-1 (LDN 0022358) is an A-type proanthocyanidin contained in several plant species such as Vaccinium vitis-idaea, Laurus nobilis L., Cinnamomum zeylanicum, and Lindera umbellata. It is a potent antioxidant and protective agent against oxidative stress and apoptosis in human platelets. It is a Cox-2 inhibitor.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that combines the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of DM1, a microtubule-inhibitory derivative of maytansine, and is utilized in the investigation of advanced breast cancer[1][2].

Cinnamtannin A2 is a natural product and procyanidin tetramer that enhances GLP-1 and insulin secretion in mice. It protects against renal injury by reducing KIM-1 and NGAL expression and exhibits antioxidant activity.

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a \( K_d \) value of 35.7 μM. It induces CDK4/6 degradation in B16F10 melanoma cells, arrests the cell cycle at the G0/G1 phase, and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in cancer research [1].

Petosemtamab (MCLA 158) is a highly potent monoclonal antibody against EGFR (Kd: 0.22 nM) and LGR5 (Kd: 0.86 nM). Petosemtamab promotes EGFR signaling disruption and receptor breakdown in LGR5+ cancer cells. Petosemtamab can be used in the study of solid tumors such as head and neck squamous cell carcinoma (HNSCC) and metastatic colorectal cancer (CRC).

Fidasimtamab is a recombinant human IgG1 bispecific antibody designed to target and inhibit both HER2 and PD-1 signaling pathways. Fidasimtamab bridges PD-1 expressing T cells with HER2 expressing tumor cells, thereby modulating immune responses while exhibiting potential immunosuppressive and antitumor effects. This mechanism provides an unique therapeutic approach for cancer research.

MTase-IN-1 (compound 26), a potent and selective inhibitor of coronavirus nsp14 N7-methyltransferases, exhibits an IC50 of 0.72 nM. It disrupts viral RNA translation and hinders immune evasion [1].

Cinnamtannin D2 (compound 13), a tannin derived from Vaccinium vitis-idaea L., boasts isolation from the aforementioned source [1].

Cinnamtannin B2 (compound 12), a tannin derivative found in cinnamon, has been isolated from the plant Vaccinium vitis-idaea L. [1].

DMTAP, a cationic lipid, facilitates the delivery of DNA, RNAi, and drugs [1] [2] [3].