mt 4

MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.

Mt KARI-IN-4 (compound 5c) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki of 5.48 μM. It also inhibits Mtb H37Rv, displaying a minimum inhibitory concentration (MIC) of 0.78 μM, and exhibits low cytotoxicity, with an IC50 over 72 μg/mL against human embryonic kidney cells (HEK) [1].

Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]

GSK3368715 is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50s: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). It has strong anti-cancer activity.

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

Trolox is a vitamin E analogue, used in reducing oxidative stress or damage.

Spermine (Neuridine) is a biogenic polyamine formed from spermidine. It is found in a wide variety of organisms and tissues and is an essential growth factor in some bacteria.

IT1t dihydrochloride inhibits CXCL12/CXCR4 interaction with IC50 of 2.1 nM. IT1t dihydrochloride is an antagonist of CXCR4.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).

IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

Heparin (Adomiparin) is a mucopolysaccharide sulfate often used as an anticoagulant in clinical medicine.Heparin has shown partial anti-inflammatory activity in in vivo experiments.

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

TC14012 TFA is a peptide-mimetic CXCR4 antagonist (IC50 = 19.3 nM) and CXCR7 agonist (EC50 = 350 nM) that promotes the recruitment of β-arrestin by CXCR7 and shares a ligand-binding surface for the CXCR4 and CXCR7 cores.

Mavorixafor (AMD-070) is an effective and selective antagonist of CXCR4, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells (IC50 = 1 nM) and PBMCs (IC50 = 9 nM).

Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active and potent inhibitor of type I protein arginine methyltransferases (PRMTs), including PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8. It exhibits anticancer and antitumor activity and can be used to study advanced solid tumors.

Edotreotide (SMT-487) is an Indicator and Reagent. It also is used in the Diagnosis and Staging of Tumors Expressing Somatostatin Receptors.

GSK3368715, a potent inhibitor of type I protein arginine methyltransferases (PRMT), could inhibit PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.

Furamidine dihydrochloride (DB75 dihydrochloride) is a cell-permeable, selective small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1) that also binds preferentially to strings of AT base pair sequences within the minor groove of DNA; it targets the PRMT1 enzyme active site primarily through a competitive mechanism with the protein substrate and is noncompetitive toward the cofactor, ultimately leading to the blockade of cell proliferation in various leukemia cell lines irrespective of their genetic lesions.

TP-064 is a potent and selective PRMT4 inhibitor, featuring an IC50 < 10nM for methylation of H3 (1-25) and over 100-fold selectivity compared to other histone methyltransferases and non-epigenetic targets. It inhibits the methylation of MED12 in cells with an IC50 of 43 nM.

MS049 dihydrochloride is a selective and cell-active dual inhibitor of PRMT4 and PRMT6 (IC50=34/43 nM), capable of reducing Med12me2a and H3R2me2a levels in HEK293 cells.