MM 22

biotinylated anandamide analog acts as a probe for visualizing the accumulation and intracellular trafficking of anandamide

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Chenodeoxycholic acid (CDCA) is a bile acid that inhibits 11β-HSD2 with an IC50 value of 22 mM. Chenodeoxycholic acid acts as a detergent to dissolve fat for intestinal absorption and is reabsorbed by the small intestine. Chenodeoxycholic acid is used as a choledocholithiasis, choledocholithiasis and laxative, as well as to prevent or dissolve gallstones.

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.

Antitumor agent-176 (Compound 22) is an antitumor agent that binds effectively to FGF2, inhibits the activation of fibroblast growth factor receptor (FGFR) in multiple myeloma (MM) cells, and demonstrates significant antitumor activity against MM both in vivo and in vitro.

TFM is a piscicide.1It is toxic to sea lamprey (P. marinus) with LC50values ranging from 1.97 to 2.11 and 2.05 to 2.21 mg/L for sac and swim-up fry, respectively, 1.6 to 2.45 mg/L for juveniles, and 1.6 to 1.63 mg/L for adults. It is also toxic to juvenile lake sturgeon (A. fulvescens) less than 100 mm in size but not to a variety of other fish species. TFM (50 μM) uncouples oxidative phosphorylation by 22 and 28% in isolated sea lamprey and rainbow trout (O. mykiss) liver, respectively.2Formulations containing TFM have been used as lampricides in the control of larval sea lamprey populations. 1.Boogaard, M.A., Bills, T.D., and Johnson, D.A.Acute toxicity of TFM and a TFM/niclosamide mixture to selected species of fish, including lake sturgeon (Acipenser fulvescens) and mudpuppies (Necturus maculosus), in laboratory and field exposuresJ. Great Lakes Res.29(Suppl 1)529-541(2003) 2.Birceanu, O., McClelland, G.B., Wang, Y.S., et al.The lampricide 3-trifluoromethyl-4-nitrophenol (TFM) uncouples mitochondrial oxidative phosphorylation in both sea lamprey (Petromyzon marinus) and TFM-tolerant rainbow trout (Oncorhynchus mykiss)Comp. Biochem. Physiol. C. Toxicol. Pharmacol.153(3)342-349(2011)

CAY10761 is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1; IC50s = 467 and 429 μM for the human and snake venom enzymes, respectively).1,2 It also inhibits mushroom tyrosinase (Ki = 1.9 μM) and urease from jack bean, P. mirabilis, and B. pasteurii (IC50s = 0.093, <0.125, and 0.089 mM, respectively, at pH 8.2).3,4 |1. Khan, K.M., Fatima, N., Rasheed, M., et al. 1,3,4-Oxadiazole-2(3H)-thione and its analogues: A new class of non-competitive nucleotide pyrophosphatases/phosphodiesterases 1 inhibitors. Bioorg. Med. Chem. 17(22), 7816-7822 (2009).|2. Onyedibe, K.I., Wang, M., and Sintim, H.O. ENPP1, an old enzyme with new functions, and small molecule inhibitors - A STING in the tale of ENPP1. Molecules 24(22), E4192 (2019).|3. Ghani, U., and Ullah, N. New potent inhibitors of tyrosinase: Novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg. Med. Chem. 18(11), 4042-4048 (2010).|4. Amtul, Z., Rasheed, M., Choudhary, M.I., et al. Kinetics of novel competitive inhibitors of urease enzymes by a focused library of oxadiazoles/thiadiazoles and triazoles. Biochem. Biophys. Res. Commun. 319(3), 1053-1063 (2004).

HIV-1 inhibitor-16 (compound 7a) is a potent HIV-1 inhibitor with an EC50 of 1.3 nM against wild-type HIV-1, and exhibits inhibitory activity against HIV-1 K103N, E138K, Y181C, and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM, and 35 nM, respectively. It demonstrates good solubility, hepatic microsomal stability, and lacks significant CYP enzyme inhibitory activity or acute toxicity.

CDK4/6-IN-10 is a selective, potent, orally active inhibitor of CDK4 (IC50: 22 nM) and CDK6 (IC50: 10 nM) with antitumour effects, showing potential for studies in multiple myeloma (MM).