homologue

(S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

H-HoArg-OH (a homologue of arginine) is a potent inhibitor of human liver and bone alkaline phosphatase.

3-Pyridylacetic acid hydrochloride (3-PAA-HCl) is a high homologue of niacin. It is a decomposition product of nicotine (and other tobacco alkaloids). It can also react with amines, alcohols and carboxylic acids, and can also act as an acid in the reaction. catalyst.

Ethaverine hydrochloride is a homologue of papaverine and is used as a vasodilator and antispasmodic.[2]

ALLO-1 is a crucial autophagy receptor responsible for facilitating the formation of autophagosomes around paternal organelles. It directly interacts with the worm LC3 homologue, LGG-1, through its LC3-interacting region (LIR) motif.

Compound BPP (HDGFRP2/PSIP1-IN-1) is a dual inhibitor targeting the PWWP domains of Hepatoma-derived Growth Factor Related Protein 2 (HDGFRP2) and its homologue PSIP1. This compound effectively hinders the occurrence and progression of Diffuse Intrinsic Pontine Glioma (DIPG). It demonstrates binding affinity with a Kd value of 7 μM for HDGFRP2, indicative of its efficient ligand efficacy at 0.47. Additionally, Compound BPP exhibits a Kd value of 27 μM when binding to the PSIP1 PWWP domain, and a Kd value of 14 μM against HDGFRP3, confirming its potency as an inhibitor within the HDGFRP2 PWWP subfamily.

1,2,3,7,8,9-Hexachlorodibenzofuran is a polychlorinated dibenzofuran homologue. It can interact with the aryl hydrocarbon receptor (AhR) and is known for its high toxicity, teratogenicity, carcinogenicity, and mutagenicity.

E3 ligase Ligand 53 serves as a FEM1B ligand to recruit Fem-1 homologue B (FEM1B) proteins. It can be linked to target protein ligands, such as HDAC1, through a linker to create mPROTAC molecules, like FF2049.

EZH2-IN-200 (compound 30) is an effective EZH2 (Enhancer of Zeste homologue 2) inhibitor with an IC50 of 11 nM against EZH2, suitable for studying hematologic malignancies and solid tumors.

(S)-(+)-Docosahexaenyl-2'-hydroxy-1'-propylamide (N-Docosahexacnoylethanolamide(22:6)) is a homologue of dehydroepiandrosterone (DHEA). This compound can block Shaker-related voltage-gated potassium channels and inhibits Kv1.2 K+ currents with an IC50 value of 1.5 μM.

SOS1-IN-22 is an inhibitor of the non-heptakinase homologue (SOS1). It effectively prevents the formation of the KRAS-G12C/SOS1 complex with an IC50 value of 40.28 nM. Additionally, SOS1-IN-22 reduces the phosphorylation levels of ERK. This compound is applicable in cancer research, including studies on pancreatic and appendiceal cancers.

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3) and inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1].

SW2_110A acetate is a selective, cell-permeable chromobox inhibitor of homologue CBX8 (Kd = 800 nM) bound to CBX8 N-terminal color gamut (ChD). SW2_110A acetate has a high affinity for CBX8N, inhibits the association between CBX8 and cell chromatin, and inhibits the proliferation of ML-AF9-induced THP1 leukemia cells.

Linoleoyl glycine, a modified polyunsaturated fatty acid, is an endogenous homologue of linoleoyl glycine. Linoleoyl glycine activates human KCNQ1/KCNE1 (hKCNQ1/hKCNE1) channels expressed in xenopus oocytes from mammalian skin, spinal cord and brain, and has shown analgesic activity in animal studies.

Viriditoxin is a secondary metabolite isolated from Aspergillus viridinutans that has been shown to inhibit FtsZ, the bacterial homologue of eukaryotic tubulin.

Bizine dihydrochloride is a potent LSD1 inhibitor in vitro, being selective versus monoamine oxidases A/B and the LSD1 homologue, LSD2.

LB244 is a homologue of BB-Cl-amidine and functions as an orally effective STING inhibitor with an EC50 value of 0.8 μM, capable of suppressing STING-dependent inflammatory signaling, although pharmacokinetic studies indicate limited oral activity in mice, making it a useful tool for mechanistic investigations of innate immunity and inflammatory disease models.

Azetidine-2-carboxylic acid, a non-proteinogenic amino acid homologue of proline found in common [beets], can be misincorporated into proteins in place of proline in various species, including humans, and is both toxic and teratogenic.

Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).

(Rac)-Juvenile hormone III, derived from farnesoic acid, represents the most prevalent homologue of juvenile hormones [1].

SOS1 agonist-1 (compound 79) serves as an agonist for the Son of sevenless homologue 1 (SOS1), a crucial guanine nucleotide exchange factor involved in catalyzing the GDP to GTP exchange on RAS proteins, thus regulating RAS activation. By increasing nucleotide exchange on RAS, SOS1 agonists enhance cellular RAS-GTP levels and induce biphasic signaling alterations in ERK1/2 phosphorylation, playing a pivotal role in anti-cancer activity [1].

EZH2-IN-18 (compound 9e) serves as a potent inhibitor of enhancer of zeste homologue 2 (EZH2 WT), exhibiting an IC50 of 1.01 nM. It effectively inhibits proliferation and induces apoptosis in tumor cells [1].

Bid BH3-Gly-r8 is a variant of Bid BH3 linked with eight arginines. It shows no difference in apoptotic effects compared to the unmodified peptide homologue, Bid BH3. Both Bid BH3-Gly-r8 and Bid BH3 exhibit high affinity for Bax and Bcl-2. This compound is applicable in tumor research.

(S)-(-)-Linoleyl-1'-Hydroxy-2'-Propylamide is a homologue of linoleyl ethanolamide (LOEA), characterized by the addition of an (S)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.