Search Result
Results for "
Trypanosoma+brucei
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-125731
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- HY-12054
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Hesperadin
Maximum Cited Publications
12 Publications Verification
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Aurora Kinase
Autophagy
Influenza Virus
Parasite
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Cancer
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Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral .
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- HY-103056
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IMP-366
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DNA/RNA Synthesis
Parasite
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Infection
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DDD85646 (IMP-366) is an orally active of trypanosoma brucei N-myristoyltransferase (TbNMT IC50=2 nM; hNMT IC50=4 nM). The enzyme N-myristoyltransferase (NMT) is a potential agent target for human African trypanosomiasis .
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- HY-128170
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Parasite
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Infection
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Ebsulfur is a benzisothiazolone cytocidal inhibitor targeting the trypanothione reductase (TryR) of Trypanosoma brucei, with IC50 values of 61-293 nM for Trypanosoma brucei. Ebsulfur can be used for the research of African trypanosomiasis .
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- HY-N7266
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Cytochrome P450
Parasite
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Infection
Cancer
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Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 μM and 1.4 μM for Trypanosoma brucei (TB) and human CYP51, respectively .
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- HY-153021
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Parasite
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Infection
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NMT-IN-1 is a Trypanosoma brucei N-myristoyltransferase (TbNMT) inhibitor, with an IC50 of 31 μM against TbNMT and an IC50 of 66 μM against hNMT. As a thiazolidinone hit compound identified via virtual screening, NMT-IN-1 exerts enzymatic inhibitory effects by binding to the active site of TbNMT. NMT-IN-1 adopts a binding mode distinct from that of pyrazole sulfonamide inhibitors and can inhibit the myristoyl transfer reaction catalyzed by TbNMT. NMT-IN-1 is mainly used in the research of anti-parasitic lead compounds for human African trypanosomiasis (African sleeping sickness). It provides a structural basis for the subsequent optimization of TbNMT inhibitors with high activity, high selectivity and blood-brain barrier permeability .
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- HY-101015A
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- HY-136637
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Phosphodiesterase (PDE)
Parasite
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Infection
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NPD-001 is a potent Trypanosoma brucei phosphodiesterases 1/2 (TbrPDEB1/2) inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits hPDE4. NPD-001 can increase cAMP levels in parasites, prevent cytokinesis, and cause the parasites to form multinucleated, multi-flagellated cells that eventually lyse. NPD-001 can be used for the research of infection .
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- HY-125731R
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Reference Standards
Endogenous Metabolite
STAT
Autophagy
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Inflammation/Immunology
Cancer
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Glycodeoxycholic Acid (Standard) is the analytical standard of Glycodeoxycholic Acid. This product is intended for research and analytical applications. Glycodeoxycholic Acid is a natural product found in Streptomyces nigricans, Trypanosoma brucei and C. elegans. Glycodeoxycholic Acid induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis .
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- HY-111759
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7-CN-7-C-Ino
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PKA
Parasite
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Infection
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Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity .
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- HY-108938
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Cytochrome P450
Fungal
Parasite
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Infection
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SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h) .
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- HY-N6674
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ECO-4601; TLN-4601; BU 4664L
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Apoptosis
Bacterial
Cathepsin
Parasite
Endogenous Metabolite
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Infection
Inflammation/Immunology
Cancer
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Diazepinomicin (ECO-4601) is an anticancer and antibacterial agent. Diazepinomicin can be produced by a Micromonospora strain. Diazepinomicin induces Apoptosis. Diazepinomicin inhibits the proteases Rhodesain and Cathepsin L at an IC50 of 70-90 μM. Diazepinomicin possesses anti-inflammatory and anti-tumor activity. Diazepinomicin has demonstrated activity against hepatocellular carcinoma. Diazepinomicin shows antiparasitic activity against trypomastigote forms of Trypanosoma brucei with an IC50 of 13.5 μM. Diazepinomicin exhibits moderate antibacterial activity against specific Gram-positive bacteria, with an MIC of approximately 32 μg/mL .
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- HY-162066
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Parasite
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Infection
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DNDI-6174 is an orally active Leishmania cytochrome b (Qi site of cytochrome bc1 complex/complex III) inhibitor. DNDI-6174 binds to the Qi site of Leishmania cytochrome b, inhibits cytochrome bc1 complex activity in the parasite's electron transport chain across promastigote and axenic amastigote stages. DNDI-6174 reduces parasite burden in rodent models, inhibits growth of various Leishmania species, drug-resistant clinical isolates, and Trypanosoma cruzi, with marginal activity against Trypanosoma brucei. DNDI-6174 can be used for the research of visceral leishmaniasis, cutaneous leishmaniasis .
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- HY-155655
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Parasite
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Infection
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JC-229 is a TbRPA1 inhibitor. JC-229 targets RPA1 in Trypanosoma brucei. JC-229 can be used for the research of Human African Trypanosomiasis (HAT) .
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- HY-135562
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Parasite
Antibiotic
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Infection
Cancer
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Ascofuranone is an orally active inhibitor of Trypanosoma brucei brucei (TAO) with a Ki value of 2.38 nM. Ascofuranone inhibits IGF-1-induced cancer cell migration, invasion, motility and actin cytoskeleton formation, and exerts anti-tumor effects. Ascofuranone can be used in research related to tumor metastasis, African trypanosomiasis, bacterial infections, lung cancer and hepatocellular carcinoma .
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- HY-179690
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Parasite
Adenosine Kinase
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Infection
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Antiparasitic agent-30 is a potent adenosine kinase TbrAK modulator and antitrypanosomal agent. Antiparasitic agent-30 exhibits significant inhibitory activity against Trypanosoma brucei rhodesiense, while enhancing the activity of recombinant TbrAK(EC50=38 nM, Ka=75 nM-497 nM). Antiparasitic agent-30 exerts its pharmacological effects by eliminating intrinsic substrate inhibition and hyperactivating TbrAK in Trypanosoma brucei rhodesiense. Antiparasitic agent-30 serves as a valuable tool molecule for studying acute African human trypanosomiasis (sleeping sickness) .
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- HY-W973644
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Mitochondrial Metabolism
Parasite
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Infection
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LY-266500 is a succinyl CoA synthetase (SCS) specific inhibitor. LY-266500 has inhibitory effects on various parasites, such as Trypanosoma brucei brucei (IC50 =0.6 μM) and Leishmania donovani (IC50 =2.86 μM). LY-266500 can be used for research on parasitic infections .
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- HY-W391625
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(Rac)-Epiligulyl oxide
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Fungal
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Cancer
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(Rac)-Dehydrocostus Lactone ((Rac)-Epiligulyl oxide) is a natural product with antiparasitic activity. (Rac)-Dehydrocostus Lactone can significantly inhibit the growth of Trypanosoma brucei rhodesiense. (Rac)-Dehydrocostus Lactone exhibits a broad spectrum of biological effects, including anti-inflammatory, anticancer, antiviral and antimicrobial activities. (Rac)-Dehydrocostus Lactone also has antifungal, antioxidant, antidiabetic, antiulcer and antihelminthic effects. (Rac)-Dehydrocostus Lactone exhibits different IC(50) values in cytotoxicity tests and has a high selectivity index .
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- HY-101015
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Phospholipase
Apoptosis
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Inflammation/Immunology
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(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM .
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- HY-16121
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Cathepsin
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Others
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CAA-0225 is a tissue protease L inhibitor that inhibits rat liver tissue protease L with a IC50 value of 1.9 nM. CAA-0225 can participate in the degradation of autophagosome membrane markers LC3-II and GABARAP (HY-P72639), improve cardiac function in mice with reperfusion injury, and kill and eliminate Trypanosoma brucei parasites [1][2][3].
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- HY-136200
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Parasite
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Infection
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Antitrypanosomal agent 2 is a potent and selective trypanosoma brucei inhibitor .
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- HY-119938
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Bacterial
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Infection
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Tuberculosis inhibitor 1 is a potent and non-cytotoxic trypanosoma brucei growth inhibitor with an EC50 of 5 nM .
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- HY-N3247
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Parasite
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Others
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Monomethyl kolavate is a Trypanosoma brucei GAPDH enzyme (TbGAPDH) inhibitor with theIC50 value of 2 µM .
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- HY-118580
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Fungal
Parasite
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Infection
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RO-09-4609 exhibits antimicrobial activity, that inhibits Candida albicans, Trypanosoma brucei and Plasmodium vivax through inhibition of N-myristoyl transferase .
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- HY-168538
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Paraptosis
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Infection
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Antitrypanosomal agent 21 (Compound C-1) is a trypanosoma brucei inhibitor. Antitrypanosomal agent 21 decreases the level of D6XM23 in parasite lysates .
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- HY-125632
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Parasite
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Infection
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Ro 19-9638 is the major metabolite of Ro 15-0216. Ro 19-9638 exhibits antiparasitic efficacy against Trypanosoma brucei rhodesiense with an IC50 of 0.0341 µg/mL .
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- HY-162656
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Dihydrofolate reductase (DHFR)
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Infection
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DHFR-IN-19 (Compound 2g) is a selective inhibitor for TbDHFR with Ki of 9 nM. DHFR-IN-19 exhibits antiparasitic activity against Trypanosoma brucei with an EC50 of 14.5 μM .
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- HY-144296
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Parasite
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Infection
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Purine phosphoribosyltransferase-IN-2 is a potent inhibitor of the Plasmodium falciparum ((Pf)), Plasmodium vivax ((Pv)) and Trypanosoma brucei ((Tbr)) 6-oxopurine phosphoribosyltransferase (PRT), with Kis of 30, 20 and 2 nM, respectively .
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- HY-157028
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Others
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Infection
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Antiparasitic agent-19 (compound 40) is a compound with broad-spectrum antiparasitic activity. Antiparasitic agent-19 has minimal toxicity against Trypanosoma brucei, Leishmania Infantum, and Trypanosoma cruzi .
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- HY-172297
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- HY-W653999
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- HY-125084
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Parasite
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Infection
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NEU617 is an anti-parasite agent. NEU617 inhibits the proliferation for the HAT (human African trypanosomiasis) pathogen (EC50: 42 nM for Trypanosoma brucei, 1.8 μM for T. cruzi). NEU617 is a derivative of Lapatinib (HY-50898) .
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- HY-147933
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Parasite
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Infection
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Antitrypanosomal agent 8 (compound 3b) has potent antitrypanosomal activity against Trypanosoma brucei with an IC50 value of 0.79 μM and exhibits certain cytotoxicity in L6 cells (IC50=80.95 μM) .
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- HY-155207
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Parasite
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Infection
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Antileishmanial agent-23 (compound G1/9) is a potent and selective trypanothione reductase (TR) inhibitor, with an IC50 of 2.24 ± 0.52 μM. Antileishmanial agent-23 inhibits the growth of Leishmania, Trypanosoma cruzi, and Trypanosoma brucei .
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- HY-144294
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Parasite
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Infection
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Purine phosphoribosyltransferase-IN-1 (Compound (S,R)-48) is a potent inhibitor of the Plasmodium falciparum (Pf), P. vivax (Pv) and Trypanosoma brucei (Tbr) 6-oxopurine purine phosphoribosyltransferases (PRTs), with Ki values of 50, 20, and 2 nM, respectively .
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- HY-W540326
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Drug Intermediate
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Infection
Cancer
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Norbornane is a component of the essential oil extracted from the rhizomes of Cyperus rotundus from Morocco. Active derivatives of Norbornane are fused heterocyclic compounds with in vitro anti-tumor and anti-Trypanosoma brucei activities. Norbornane and its derivatives can be used in research related to cancers such as leukemia and African trypanosomiasis .
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- HY-116045
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Parasite
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Cancer
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PDEB1-IN-1 (Compound 12b) is the derivative of Cilomilast (HY-10790), and serves as an inhibitor for TryPanosoma Brucei PDEB1 (TbrPDEB1) with an IC50 of 0.95 μM. PDEB1-IN-1 inhibits the proliferation of T. Brucei with an EC50 of 26 μM .
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- HY-147940
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Parasite
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Infection
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TbPTR1 inhibitor 1 (compound 5d) is a potent kinetoplastid pteridine reductase 1 (PTR1) inhibitor with an IC50<0.1 nM for TbPTR1. TbPTR1 inhibitor 1 has inhibitory activity against Trypanosoma brucei (EC50=0.66 μM) .
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- HY-170363
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Proteasome
Parasite
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Infection
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Proteasome-IN-6 (Compound J-80) inhibits the β5 catalytic subunit of the Trypanosoma brucei 20S proteasome, inibits T. b. brucei, T. b. gambiense and T. b. rhodesiense with EC50s of 157 nM, 220 nM and 156 nM, respectively. Proteasome-IN-6 exhibits antitrypanosomal activity in mouse model .
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- HY-175305
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Parasite
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Infection
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DMU759 is a Lysyl-tRNA synthetase 1 (KRS1) inhibitor. DMU759 has potent anti-kinetoplastid activity against Trypanosoma cruzi , Trypanosoma brucei and Leishmania donovani. DMU759 significantly reduces parasitemia in acute Chagas disease mice model. DMU759 can be used for parasitic infection like Chagas disease research .
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- HY-147549
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Parasite
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Infection
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Antitrypanosomal agent 6 (compound 18a) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 6 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC50 value of 0.47 μM. Antitrypanosomal agent 6 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA .
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- HY-147550
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Parasite
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Infection
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Antitrypanosomal agent 7 (compound 18c) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 7 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC50 value of 0.71 μM. Antitrypanosomal agent 7 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA .
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- HY-N16437
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Parasite
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Infection
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Panowamycin A is an isochroman compound that can be produced by Streptomyces sp. K07-0010. Panowamycin A exhibits antitrypanosomal activity against the Trypanosoma brucei brucei GUTat 3.1 strain (IC50: 0.40 μg/mL). Panowamycin A shows weak cytotoxicity towards human fetal lung fibroblast MRC-5 cells (IC50: 2.95 μg/mL). Panowamycin A can be used for research in the field of antitrypanosomal studies .
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- HY-126250
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Phosphodiesterase (PDE)
Parasite
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Infection
Inflammation/Immunology
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NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death . NPD-1335 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-146049
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Parasite
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Infection
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Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively . Antitrypanosomal agent 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-176253
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Parasite
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Infection
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Antitrypanosomal agent 26 (Compound 1) is an allosteric trypanosome alternative oxidase (TAO) inhibitor. Antitrypanosomal agent 26 exhibits potent activity against African animal trypanosomes (e.g., Trypanosoma brucei, etc.) with an IC50 value of 1.3 nM for recombinant TAO. Antitrypanosomal agent 26 blocks the mitochondrial electron transport chain of trypanosomes and inhibits glucose-dependent respiration. Antitrypanosomal agent 26 is promising for research of African animal trypanosomiasis, such as bovine trypanosomiasis .
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- HY-175517
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Parasite
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Infection
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PEX5-PEX14 PPI-IN-3 (Compound 7) is an inhibitor of the PEX5-PEX14 protein-protein interaction (PPI) with an EC50 of 95 μM. PEX5-PEX14 PPI-IN-3 has an EC50 of 7.2 μM against Trypanosoma brucei (T. brucei). PEX5-PEX14 PPI-IN-3 exhibits low cytotoxicity towards HepG2 cells and possesses antiparasitic activity .
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- HY-178064
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Parasite
Mitochondrial Metabolism
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Infection
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Antiparasitic agent-29 (Compound 5) is a Trypanosome alternative oxidase (TAO) inhibitor with an IC50 of 1.3 nM in Trypanosoma brucei. Antiparasitic agent-29 has a broad-spectrum antiparasitic activity against Trypanosoma and Leishmania spp. Antiparasitic agent-29 accumulates in parasite mitochondria, selectively disrupting its energy metabolism and has potent membrane-perturbing activity with no cross-resistance. Antiparasitic agent-29 shows low ecotoxicity in zebrafish and Daphnia magna models. Antiparasitic agent-29 can be used for parasitic diseases like surra and dourine research .
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- HY-175979
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Parasite
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Infection
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HAT-IN-9 (Compound 3F) is a selective proliferation inhibitor targeting Trypanosoma brucei. HAT-IN-9 inhibits the proliferation and division of Trypanosoma brucei. HAT-IN-9 is promising for research of African trypanosomiasis (HAT, i.e., sleeping sickness) .
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- HY-118606
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PAK
Parasite
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Infection
Cancer
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LDN-0044878 is a PAK3 inhibitor. LDN-0044878 inhibits the proliferation or induces the death of p53-deficient cells. LDN-0044878 exhibits moderate trypanocidal activity against Trypanosoma brucei, but does not directly inhibit the core target Rhodesain. LDN-0044878 can be used in studies related to cervical adenocarcinoma and Trypanosoma brucei infection.
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- HY-168732
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Parasite
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Infection
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MCG-02 is the inhibitor for cruzain (CRZ) and cathepsin L-like protease (CATL), that inhibits the CRZ in Trypanosoma cruzi and CATL in Trypanosoma brucei with the IC50 0.2 μM and 0.02 μM .
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- HY-N19754
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Parasite
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Infection
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Cladospirone B is a secondary metabolite of the endophytic fungus Lasiodiplodia theobromae. Cladospirone B exhibits trypanocidal activity, with a MIC of 17.8 µM against Trypanosoma brucei. Cladospirone B can be used in the research of African human trypanosomiasis (sleeping sickness) .
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- HY-P11367
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Fluorescent Dye
Ser/Thr Protease
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Infection
Metabolic Disease
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Boc-Ala-Gly-Pro-Arg-AMC is a synthetic fluorescent substrate, widely used for the detection of protease activity. Boc-Ala-Gly-Pro-Arg-AMC can be used to detect the activity of serine proteases and the oligopeptide enzyme B of Trypanosoma brucei .
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- HY-125188
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Parasite
DNA/RNA Synthesis
AMPK
Clathrin
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Infection
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NEU-4438 is an antimalarial agent. NEU-4438 inhibits DNA synthesis, reduces AMPK-γ, and increases Clathrin heavy chain. NEU-4438 exhibits antiparasitic activity against Trypanosoma brucei. NEU-4438 reduces trypanosome tissue burden in a chronic HAT mouse model .
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- HY-103056R
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IMP-366 (Standard)
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Reference Standards
DNA/RNA Synthesis
Parasite
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Infection
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DDD85646 (Standard) is the analytical standard of DDD85646 (HY-103056). This product is intended for research and analytical applications. DDD85646 (IMP-366) is an orally active of trypanosoma brucei N-myristoyltransferase (TbNMT IC50=2 nM; hNMT IC50=4 nM). The enzyme N-myristoyltransferase (NMT) is a potential agent target for human African trypanosomiasis .
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- HY-W743767
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MZR-P
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IMPDH
Parasite
Drug Metabolite
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Infection
Inflammation/Immunology
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Mizoribine 5'-monophosphate (MZR-P) is the active metabolite of Mizoribine (HY-17470). Mizoribine 5'-monophosphate is an inhibitor of inosine-5'-monophosphate dehydrogenase (IMPDH), and its Ki values for IMPDH of Trypanosoma brucei, Bacillus subtilis and Oceanobacillus iheyensis are 3.3, 72 and 157 nM respectively. Mizoribine 5'-monophosphate can be used in anti-trypanosomiasis and immunosuppression research .
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- HY-N16437A
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Parasite
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Infection
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Panowamycin B is an isochroman compound that can be produced by Streptomyces sp. K07-0010. Panowamycin B exhibits antitrypanosomal activity against the Trypanosoma brucei brucei GUTat 3.1 strain (IC50: 3.30 μg/mL). Panowamycin B shows weak cytotoxicity towards human fetal lung fibroblast MRC-5 cells (IC50: 13 μg/mL). Panowamycin B can be used for research in the field of antitrypanosomal studies .
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- HY-182443
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Parasite
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Infection
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PEX5-PEX14 PPI-IN-4 is a potent PEX14-PEX5 PPI inhibitor, with EC50 values of 7.78 μM, 27.5 μM and 9.31 μM against the protein-protein interactions of TbPEX14-PEX5, TcPEX14-PEX5 and HsPEX14-PEX5, respectively. PEX5-PEX14 PPI-IN-4 exhibits trypanocidal activity against Trypanosoma brucei rhodesiense and Trypanosoma cruzi. PEX5-PEX14 PPI-IN-4 shows cytotoxic activity against mammalian cells. PEX5-PEX14 PPI-IN-4 can be used in the research of human African trypanosomiasis and Chagas disease .
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Product Name |
Target |
Research Area |
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-W653999
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Glycodeoxycholic acid-d5 is deuterium labeled Glycodeoxycholic Acid. Glycodeoxycholic Acid is a natural product found in Streptomyces nigricans, Trypanosoma brucei and C. elegans. Glycodeoxycholic Acid induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis .
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