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.

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.

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, a tetrameric procyanidin, enhances GLP-1 and insulin secretion in mice, upregulates the expression of corticotrophin releasing hormone (CRH), and exhibits antioxidant, anti-diabetic, and nephroprotective effects.

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 (IBI-315; BH2950), a recombinant human IgG1 bispecific antibody, specifically targets, binds to, and inhibits HER2 and PD-1 along with their downstream signaling pathways. Additionally, it bridges PD-1 expressing T cells with HER2 expressing tumor cells, demonstrating potential immunosuppressive and antitumor activities [1].

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].

Laprituximab emtansine (IMGN-289), an immunotoxin targeting HER1, is an EGFR antibody-drug conjugate (ADC) composed of J2898A antibody, DM1 (anti-microtubule agent), and the SMCC thioether linker, utilized in cancer research [1] [2] [3].

Naratuximab emtansine (IMGN529) is a CD37-targeted antibody-drug conjugate (ADC) composed of a humanized IgG1 monoclonal antibody linked to the microtubule-disrupting agent DM1. This compound demonstrates high affinity and specificity to CD37, facilitating the internalization, processing, and intracellular release of DM1. The functional activity of DM1 enables it to induce cell cycle arrest and apoptosis by disrupting microtubule assembly.

Precemtabart is a humanized IgG1κ antibody targeting CEACAM5, with HumanIgG1kappa, Isotype Control serving as its corresponding isotype control.

Bulumtatug is a humanized IgG1κ monoclonal antibody that targets Nectin-4, with the corresponding isotype control being Human IgG1 kappa, Isotype Control.

Amtabafusp alfa is a humanized IgG1λ1 antibody targeting CD3E CD4. Its isotype control corresponds to HumanIgG1lambda1, Isotype Control.