Trypanosoma brucei

DDD85646 is an inhibitor of T. brucei N-myristoyltransferase with a Ki of 1.44 nM, an IC50 of 2 nM and an EC50 of 2 nM. The IC50 of hNMT is 4 nM.

CRK12-IN-1 is a potent CRK12 inhibitor with insecticidal activity and exhibits inhibitory effects on Trypanosoma brucei (T.b. brucei) and Trypanosoma congolense (T. congolense) with EC50s of 1.3 and 18 nM, respectively, rapidly killing the pathogenic cells.

Tuberculosis inhibitor 1 is a potent, non-cytotoxic inhibitor of Trypanosoma brucei growth [EC50: 5 nM].

1. Columbin has anti-inflammatory activity. 2. Columbin has chemopreventive ability against human colon cancer. 3. Columbin inhibits PLA2 hydrolysis of ghost RBC in a dose-dependent fashion.

6'-hydroxydihydrocinchonidine is a metabolite of quinine, with antimicrobial and antitumor activity, and inhibitory effect on Trypanosoma brucei and Streptococcus pneumoniae.

Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα but exhibits anti-parasite activity and is a potent activator of PKA, binding to the R site (PKAR) with an EC50 of 6.5 nM and a Kd of 8 nM in Trypanosoma brucei.

3',4',5,5',6,7-Hexamethoxyflavone is a flavonoid with notable antiprotozoal activity, and 3',4',5,5',6,7-Hexamethoxyflavone exhibits inhibitory effects against Trypanosoma brucei rhodesiense with an IC50 value of 21.3 μM, corresponding to 8.58 μg/mL, thereby demonstrating its potential as a bioactive compound in the investigation of natural product-derived therapeutics for protozoan parasitic infections.

Antitrypanosomal agent 2 shows potent and specific antiparasite activities against Trypanosoma brucei.

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC50 of 2.5 μM.

DDD100097 is a potent N-myristoyltransferase inhibitor with potential inhibitory effects on Trypanosoma brucei, which can be used to study neurological disorders.

Glycodeoxycholic Acid is an endogenous metabolite, a natural product found in Streptomyces niger, Trypanosoma brucei, and Cryptomonas, which induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis.

NPD1335, a potent inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1), exhibits submicromolar activity against T. brucei parasites and an improved cytotoxicity profile. By elevating intracellular cAMP levels, NPD1335 disrupts the cell cycle, leading to cell death [1].

Obtusifoliol is a specific inhibitor of CYP51(Trypanosoma brucei (TB) and human CYP51 with Kd values of 1.2 µM and 1.4 µM, respectively).

Compound C-1 (Antitrypanosomal agent 21) serves as an inhibitor of Trypanosoma brucei. It effectively reduces the levels of D6XM23 in the parasite lysate.

MCG-02 is an inhibitor of cruzain (CRZ) and cathepsin L-like protease (CATL), capable of inhibiting CRZ in Trypanosoma cruzi and CATL in Trypanosoma brucei, with IC50 values of 0.2 μM and 0.02 μM, respectively.

Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, effectively blocking T. b. brucei, T. b. gambiense, and T. b. rhodesiense with EC50 values of 157 nM, 220 nM, and 156 nM, respectively. Additionally, Proteasome-IN-6 has demonstrated antitrypanosomal activity in a mouse model.

Pyrazole N-Desmethyl sildenafil (Compound 10) is an analogue of Sildenafil. At a concentration of 100 µM, it inhibits the activity of the Trypanosoma brucei phosphodiesterase TbrPDEB1 by 16%.

Antitrypanosomal agent 19 (compound 10) is an orally active antitrypanosomal drug. It effectively inhibits the growth of Trypanosoma brucei brucei, T. b. gambiense, and T. b. rhodesiense, alleviating the acute infection induced in mice by African human trypanosomiasis (HAT).

HGPRT/TBrHGPRT1-IN-1 (Compound 5) is a selective inhibitor of human hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and Trypanosoma brucei TBrHGPRT1, with a Ki of 3 nM. By inhibiting HGPRT/TBrHGPRT1, it ultimately reduces cell growth. HGPRT/TBrHGPRT1-IN-1 is primarily used in research on infectious diseases and cancer.

Ebsulfur is a benzisothiazolone parasitic inhibitor targeting the trypanothione reductase (TryR) of Trypanosoma brucei, with an IC50 value ranging from 61 to 293 nM for this parasite. Ebsulfur is utilized in the study of African trypanosomiasis.

Antitrypanosomal agent 26 (Compound 1) is an allosteric inhibitor of trypanosome alternative oxidase (TAO). It exhibits potent activity against African trypanosomes, such as Trypanosoma brucei, with an IC50 value of 1.3 nM for recombinant TAO. The compound disrupts the mitochondrial electron transport chain of trypanosomes and inhibits glucose-dependent respiration. Antitrypanosomal agent 26 shows potential for research in treating African animal trypanosomiasis, including bovine trypanosomiasis.

Fexinidazole (HOE 239) is an antiparasitic agent with activity against Trypanosoma cruzi, Tritrichomonas foetus, Trichomonas vaginalis, Entamoeba histolytica, Trypanosoma brucei, and Leishmania donovani. The biologically relevant active metabolites in vivo are the sulfoxide and sulfone.

DMU759 is a lysyl-tRNA synthetase 1 (KRS1) inhibitor. It exhibits potent anti-kinetoplastid activity against Trypanosoma cruzi, Trypanosoma brucei, and Leishmania donovani. In mouse models of acute Chagas disease, DMU759 significantly reduces parasitemia. DMU759 is applicable for research on parasitic infections, including Chagas disease.

PEX5-PEX14 PPI-IN-3 (Compound 7) is an inhibitor of the PEX5-PEX14 protein-protein interaction, with an EC50 of 95 μM. It demonstrates an EC50 of 7.2 μM against Trypanosoma brucei and exhibits low cytotoxicity in HepG2 cells. PEX5-PEX14 PPI-IN-3 also possesses antiparasitic activity.