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T.brucei

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bacterial (3) Cholinesterase (ChE) (2) Farnesyl Transferase (1) GSK-3 (1) Parasite (24) Phosphodiesterase (PDE) (1)
By Research Areas:	Cancer (2) Infection (23) Inflammation/Immunology (1) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13801

Fexinidazole 1 Publications Verification HOE 239	Parasite	Infection
Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei .

HY-W052512

Antitrypanosomal agent 1	Parasite	Infection
Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC₅₀ of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) (IC₅₀=64.8 μM) and T. brucei (EC₅₀=1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity .

HY-12607

ML251	Parasite	Infection
ML251, a potent nanomolar T. brucei and T. cruzi phosphofructokinase (PFK) inhibitor, inhibits T. brucei PFK (IC₅₀=0.37 μM) and T. cruzi PFK (IC₅₀=0.13 μM). ML251 can be used for the research of parasite .

HY-N2230

N-p-trans-Coumaroyltyramine	Cholinesterase (ChE) Parasite	Infection Neurological Disease
N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC₅₀ of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC₅₀ of 13.3 µM for T. brucei rhodesiense .

HY-13801R

Fexinidazole (Standard)	Parasite	Infection
Fexinidazole (Standard) is the analytical standard of Fexinidazole. This product is intended for research and analytical applications. Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei .

HY-155024

HAT-IN-8	Parasite	Infection
HAT-IN-8 (Compound 38) is a BBB-penetrable T. brucei inhibitor (EC₅₀: 0.18 μM). HAT-IN-8 can be used for the research of Human African trypanosomiasis .

HY-146071

Antitrypanosomal agent 5	Parasite	Infection
Antitrypanosomal agent 5 (Compound 25)is a selective anti-trypanosomal agent with IC₅₀s of 1 nM and 483.3 µM against T. brucei cell growth and HEK293 cells growth , respectively .

HY-155025

Antitrypanosomal agent 14	Parasite GSK-3	Infection
Antitrypanosomal agent 14 (Compound 1) is a T. brucei inhibitor (EC₅₀: 0.47 μM). Antitrypanosomal agent 14 inhibits TbGSK3 with an IC₅₀ of 12 μM. Antitrypanosomal agent 14 can be used for the research of Human African trypanosomiasis .

HY-149986

Antitrypanosomal agent 13	Parasite	Infection
Antitrypanosomal agent 13 (compound 4b) is a potent antitrypanosomal agent. Antitrypanosomal agent 13 has trypanocidal and cytotoxic activity with GI₅₀ values of 0.18 and 8.4 μM for T. brucei and HL-60, respectively .

HY-149722

Antiparasitic agent-20	Parasite	Infection
Antiparasitic agent-20 (Compound 1p) is a parasite inhibitor with broad antiparasitic activity. Antiparasitic agent-20 has inhibitory effects on T. brucei and T. cruzi with EC₅₀ values of 0.09 μM and 14.1 μM respectively .

HY-146489

Anti-infective agent 3	Bacterial Parasite	Infection
Anti-infective agent 3 (compound 3l) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC₅₀ values of 0.47 and 0.13 μM, respectively. Anti-infective agent 3 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 4 μg/mL .

HY-W009689

TbPTR1 inhibitor 2	Parasite	Infection
TbPTR1 inhibitor 2 (Compound 3a) is a PTR1 enzyme inhibitor, with IC₅₀s of 34.2 and 32.9 μM for TbPTR1 and LmPTR1. TbPTR1 inhibitor 2 has anti-parasitic activity against T. brucei (IC₅₀: 34.2 μM) .

HY-146488

Anti-infective agent 2	Parasite Bacterial	Infection
Anti-infective agent 2 (compound 3k) shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC₅₀ values of 0.07 and 2.20 μM, respectively. Anti-infective agent 2 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 32 μg/mL .

HY-116045

PDEB1-IN-1	Parasite	Cancer
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 .

HY-N1985

Acetylastragaloside I	Parasite	Infection
Acetylastragaloside I is a glycoside that can be isolated from the roots of Astragalus baibutensis. Acetylastragaloside I is the first cycloartane-type triterpene with remarkable trypanocidal activity with IC₅₀ values of 9.5 and 5.0 μg/mL for T. brucei rhodesiense and *T. cruzi*, respectively. Acetylastragaloside I can be used for the research of trypanosome infection .

HY-155281

Antiparasitic agent-18	Parasite	Infection
Antiparasitic agent-18 (compound 3a) is active and selective against the T. brucei (EC₅₀=0.4 μM), T. cruzi (EC₅₀=0.21 μM), and L. donovani (EC₅₀=0.26 μM). Antiparasitic agent-18 has potent antiprotozoal activity .

HY-146487

Anti-infective agent 1	Bacterial Parasite	Infection
Anti-infective agent 1 (compound 3a) is a potent and selective antiprotozoal and antimycobacterial agent. Anti-infective agent 1 shows antiparasitic activity against P. falciparum and T. brucei rhodesiense, with IC₅₀ values of 10.95 and 0.06 μM, respectively. Anti-infective agent 1 shows antimycobacterial activity against Mycobacterium smegmatis with a MIC of 8 μg/mL .

HY-147550

Antitrypanosomal agent 7	Parasite	Infection
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 .

HY-147549

Antitrypanosomal agent 6	Parasite	Infection
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 .

HY-N7634

Tectol	Farnesyl Transferase Parasite	Infection Cancer
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC₅₀s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC₅₀ of 3.44 μM .

HY-N2230R

N-p-trans-Coumaroyltyramine (Standard)	Cholinesterase (ChE) Parasite	Infection Neurological Disease
N-p-trans-Coumaroyltyramine (Standard) is the analytical standard of N-p-trans-Coumaroyltyramine. This product is intended for research and analytical applications. N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC₅₀ of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC₅₀ of 13.3 μM for T. brucei rhodesiense .

HY-158379

Antiparasitic agent-22	Parasite	Infection
Antiparasitic agent-22 (Compound 24) is a pan antiparasitic agent, that inhibits T. Brucei, L. infantum, L. tropica promastigotes (IC₅₀ of 2.41, 5.95, 8.98 μM), L. infantum amastigotes (IC₅₀ of 8.18 μM) and P. falciparum W2 strain (IC₅₀ of 0.155 μM). Antiparasitic agent-22 exhibits low cytotoxicity against THP1, with CC₅₀ of 64.16 μM .

HY-126250

NPD-1335	Phosphodiesterase (PDE) Parasite	Infection Inflammation/Immunology
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.

HY-126489

Tetromycin B	Parasite	Infection
Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsin B, respectively. It inhibits the growth of T. brucei in vitro (IC₅₀=30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC₅₀s=71.77 and 20.2 μM, respectively).

N-p-trans-Coumaroyltyramine	Ophiopogon japonicus (L. f.) Ker-Gawl. Structural Classification Liliaceae Simple Phenylpropanols Source classification Phenols Polyphenols Phenylpropanoids Plants	Cholinesterase (ChE) Parasite
N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC₅₀ of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC₅₀ of 13.3 µM for T. brucei rhodesiense .

Tectol	Infection Structural Classification other families Classification of Application Fields Source classification Phenols Polyphenols Plants Disease Research Fields	Farnesyl Transferase Parasite
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC₅₀s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC₅₀ of 3.44 μM .

Acetylastragaloside I	Structural Classification Natural Products Leguminosae Astragalus membranaceus var. mongholicus (Bunge)P.K.Hsiao Plants	Parasite
Acetylastragaloside I is a glycoside that can be isolated from the roots of Astragalus baibutensis. Acetylastragaloside I is the first cycloartane-type triterpene with remarkable trypanocidal activity with IC₅₀ values of 9.5 and 5.0 μg/mL for T. brucei rhodesiense and *T. cruzi*, respectively. Acetylastragaloside I can be used for the research of trypanosome infection .

N-p-trans-Coumaroyltyramine (Standard)	Ophiopogon japonicus (L. f.) Ker-Gawl. Structural Classification Liliaceae Simple Phenylpropanols Source classification Phenols Polyphenols Phenylpropanoids Plants	Cholinesterase (ChE) Parasite
N-p-trans-Coumaroyltyramine (Standard) is the analytical standard of N-p-trans-Coumaroyltyramine. This product is intended for research and analytical applications. N-p-trans-Coumaroyltyramine is a cinnamoylphenethyl amide isolated from polygonum hyrcanicum, acts as an acetylcholinesterase (AChE) inhibitor with an an IC₅₀ of 122 μM. N-p-trans-Coumaroyltyramine exhibits anti-trypanosomal activity with an IC₅₀ of 13.3 μM for T. brucei rhodesiense .

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T.brucei

Inhibitors & Agonists

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