mpc

MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.

UK-5099 (PF-1005023) is a specific and potent inhibitor of MPC carrier activity, effectively inhibiting pyruvate-dependent oxygen consumption in rat heart mitochondria with an IC50 of 50 nM [1].

GW604714X (2,4-Thiazolidinedione, 5-[[5-[6-(4-acetyl-1-piperazinyl)-3-nitro-2-pyridinyl]-2-fluorophenyl]methylene]-) were found to be potent inhibitors of mitochondrial respiration supported by pyruvate

MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of Hsp90 with significant antitumor activity [1].

MPC-0767, a potent, selective, and orally active hsp90 inhibitor, is the L-alanine ester prodrug of MPC-3100, exhibiting enhanced chemical stability.

MPC-IN-1 (compound 4i), a derivative of UK-5099, is a cyanocinnamate-based inhibitor of the mitochondrial pyruvate transporter (MPC). This compound selectively fosters the development of hair follicle stem cells while not impacting normal cells. It enhances cellular lactate production and has shown significant hair growth promotion in mice, suggesting its potential use in combating hair loss.

MPCI is a selective melanocortin-4 receptor antagonist.

AMPC is a TFF3 inhibitor with antitumor activity and inhibits tumor growth in vivo. AMPC inhibits cell proliferation and survival in TFF3-positive CMS4 colorectal cancer cells and can be used to study colorectal cancer.

Cyclic HPMPC is a potent antiviral agent that increases arterial oxygen saturation in mice infected with the lethal vaccinia virus (IHD strain) and reduces viral replication in guinea pigs, thereby improving outcomes in congenital guinea pig cytomegalovirus (GPCMV) infection [1] [2].

AMPCP is an Ecto-5'-nucleotidase (CD73) inhibitor.

EDMPC, a cationic lipid, exhibits an enhanced capability for DNA delivery to pulmonary tissues. It facilitates intralobar DNA transfer in rodents [1].

PIMPC, a compound endowed with antioxidant and metal-chelating properties, acts as a novel inhibitor of glycogen synthase kinase 3 (GSK-3), and exhibits potential therapeutic effects for Alzheimer's disease [1].

MSDC-0602K (Azemiglitazone potassium) (Azemiglitazone potassium) is a PPARγ-sparing thiazolidinedione (Ps-TZD) compound that binds to PPARγ with an IC50 of 18.25 μM. It also modulates the mitochondrial pyruvate carrier (MPC). This compound, MSDC-0602K, has potential applications in researching fatty liver conditions, including dysfunctional lipid metabolism, inflammation, and insulin resistance. MSDC-0602K acts as an insulin sensitizer, improving insulinemia and fatty liver disease in mice both individually and in combination with Liraglutide.

Aranidipine (MPC1304) (MPC1304) is a calcium channel antagonist with potent and long-lasting antihypertensive effects.

Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood-brain barrier permeable microtubule-disrupting agent with potent and broad-spectrum cytotoxic activities and significant anticancer efficacy in human MX-1 breast cancer and various mouse xenograft cancer models.

Verubulin (MPC 6827) is a potent microtubule blocker with cytotoxic and potentially anticancer activity that disrupts newly formed blood vessels in xenografts, and can be used to image microtubules (MTs) using positron emission tomography (PET).

BE2647 is a selective inhibitor of the mitochondrial pyruvate carrier (MPC), with an EC50 of 70 nM. It exhibits good metabolic stability in mouse liver microsomes. BE2647 can be utilized in research related to metabolic diseases, metabolic-associated steatotic liver disease (MASLD), or metabolic-associated steatohepatitis (MASH).

TAK1-IN-5 (Compound 26) is an inhibitor of transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. It effectively suppresses the growth of MPC-11 and H929 cells, with a GI50 below 30 nM. TAK1-IN-5 is a useful tool for research in multiple myeloma.

Azemiglitazone (MSDC 0602) is an insulin sensitizer potentially for the treatment of diabetes.

Bevirimat (PA-457) is a first-in-class inhibitor of HIV-1 maturation, blocking the cleavage of the Gag capsid (CA) precursor, CA-SPI, to mature CA protein during virion maturation.

Tarenflurbil ((R)-Flurbiprofen) is the non-cyclooxygenase inhibiting R-enantiomer of the NSAID flurbiprofen, evaluated as a treatment for Alzheimer's disease.