(S,R,S)-AHPC-C4-NH2 dihydrochloride is a chemically derived E3 ligase ligand-linker conjugate, consisting of the (S,R,S)-AHPC VHL ligand and a linker specifically designed for EED-Targeted PROTAC[1].
Lenalidomide-C4-NH2 hydrochloride is a Cereblon ligand derived from Lenalidomide. It serves as a recruiting agent for the CRBN protein. The compound, known as PROTAC (Compound 24), can be formed by linking Lenalidomide-C4-NH2 hydrochloride to the ligand for the protein. It exhibits inhibitory effects with IC50s of 0.98 nM and 13.7 nM against the growth of RS4;11 and MOLM-13 acute leukemia cell lines, respectively[1].
Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate consisting of an E3 ligase ligand-linker, incorporating the Thalidomide-based cereblon ligand and a linker moiety. This compound, Thalidomide-NH-C4-NH2 TFA, is utilized as a component in PROTAC BRD2 BRD4 degrader-1, which is a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].
Produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets, leukotriene C4 (LTC4) is the parent cysteinyl leukotriene formed by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4, however, is rapidly metabolized to LTD4 and LTE4, which makes the characterization of LTC4 pharmacology difficult. N-methyl Leukotriene C4 (N-methyl LTC4) is a synthetic analog of LTC4 that is not readily metabolized to LTD4 and LTE4.It acts as a potent and selective CysLT2 receptor agonist exhibiting EC50 values of 122 and > 2,000 nM at the human CysLT2 and CysLT1 receptors, respectively. It has essentially the same potency as LTC4 at both the human and murine receptors CysLT2 receptors. N-methyl LTC4 is potent and active in vivo, causing vascular leak in mice overexpressing the human CysLT2 receptor but not in CysLT2 receptor knockout mice.
Mal-C4-NH-Boc is a alkyl ether-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
The chemical compound Mal-Phe-C4-Val-Cit-PAB-DMEA is a cleavable antibody-drug conjugate (ADC) linker that incorporates a Maleimide group. It is commonly employed in the synthesis of ADCs.
Pomalidomide-amido-C4-amido-C6-NH-Boc, a synthesized conjugate, is a ligand-linker incorporating the cereblon ligand based on Pomalidomide and a PROTAC technology linker.
Mal-Phe-C4-VC-PAB-MMAE is a chemical compound resulting from the conjugation of monomethyl auristatin E (MMAE), a potent tubulin inhibitor serving as a toxin payload in antibody-drug conjugates, with a Mal-Phe-C4-VC-PAB linker.
C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7 Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation, enhances cAMP-activated chloride secretion, and suppresses secretion of IL-8 in primary epithelial cells isolated from patients with cystic fibrosis.[3]
Boc-NH-C4-Br is a alkyl chain-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
Pomalidomide-amido-C4-amido-PEG2-C2-NH-Boc is a novel synthesized conjugate compound functioning as an E3 ligase ligand-linker in PROTAC technology. This compound incorporates a Pomalidomide-derived cereblon ligand, which binds selectively to the E3 ligase cereblon, and a 2-unit PEG linker, which provides stability and flexibility to the conjugate.
Mal-Phe-C4-Val-Cit-PAB is a cleavable antibody-drug conjugate (ADC) linker featuring a Maleimide functional group. It is employed in the synthesis of ADCs.
11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum as a cysteinyl leukotriene receptor preparation, the pKis for LTC4 and 11-trans LTC4 were determined to be 6.42 and 6.58, respectively.
Pomalidomide-C4-NH2 is a chemically synthesized conjugate, consisting of a ligand for E3 ligase (cereblon) derived from Pomalidomide and a linker employed in PROTAC technology.
Mal-Phe-C4-VC-PAB-DMEA-PNU-159682 is a drug-linker conjugate utilized in antibody-drug conjugate (ADC) therapy. It comprises the ADC linker Mal-Phe-C4-VC-PAB and the potent ADC cytotoxin DMEA-PNU-159682. DMEA-PNU-159682 encompasses metabolites of nemorubicin (MMDX) derived from liver microsomes, as well as the ADC cytotoxin PNU-159682[1].