Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) with IC50s between 5μM and 50μM for differing isoforms. Paxilline possesses significant anticonvulsant activity[1][2][3].
Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity[1].
(S)-2-((S)-2-Amino-5-guanidinopentanamido)-3-phenylpropanoic acid compound with acetic acid (1:1) is a phenylalanine derivative[1].
YM-53601, a squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in vivo[1]. YM-53601 inhibits squalene synthase derived from human hepatoma cells with an IC50 of 79 nM. Lipid-lowering agent[2]. YM-53601 also is an inhibitor of farnesyl-diphosphate farnesyltransferase 1 (FDFT1) enzyme activity and abrogates HCV propagation[3].
3,4-Dehydro-DL-proline is a proline derivative[1].
AKT-IN-7 (compound 1-P1) is a potent AKT inhibitor. AKT-IN-7 has the potential for cancer research[1].
Morantel tartrate is a broad spectrum anthelmintic, effective and low toxicity.
URAT1&XO inhibitor 2 (Compound BDEO) is a dual inhibitor of xanthine oxidase and URAT1, with IC50 of 3.3 μM for xanthine oxidase. URAT1&XO inhibitor 2 blocks uptake of uric acid in HEK293 cells expressing URAT1, with a Ki value of 0.145 μM. URAT1&XO inhibitor 2 decreases serum urate level and uric acid excretion in hyperuricemic mice. URAT1&XO inhibitor 2 can be used for research of hyperuricemia[1].
RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor. RIPK3-IN-4 inhibits HK-2 cell damage, necroptosis and inflammatory responses. RIPK3-IN-4 reduces Cisplatin (HY-17394)- and I/R-induced kidney damage, inflammatory response and necroptosis in acute kidney injury[1].
Sanggenon A (Sanggenone A) exerts anti-inflammatory effects by regulating NF-κB and HO-1/Nrf2 signaling pathways in BV2 and RAW264.7 cells. Sanggenon A markedly inhibits the Lipopolysaccharide (LPS; HY-D1056)-induced production of nitric oxide[1].
MRT-81 is a potent antagonist of human and rodent smoothened Smo receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer[1].
Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor[1][2][3].
N-Chloroacetyl-DL-isoleucine is an isoleucine derivative[1].
Mifamurtide(CGP19835; MTP-PE) is a drug against osteosarcoma.Target: OthersMifamurtide is an immunomodulator with antitumor effects that appear to be mediated via activation of monocytes and macrophages. Mifamurtide is generally well tolerated; adverse events attributed to administration of the drug include chills, fever, headache, nausea, and myalgias. Based on the available data, mifamurtide can be considered for inclusion in treatment protocols for localized osteosarcoma [1]. Mifamurtide has orphan drug status for the treatment of osteosarcoma in the US and EU [2].
Ceralifimod is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.
Biotin-PEG3-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.
Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.
3-Morpholinosydnonimine (SIN-1; Linsidomine) is a spontaneous ROS/RNS generator and a peroxynitrite donor. 3-Morpholinosydnonimine inhibits hypertrophic chondrocytes activity and induces necrosis. 3-Morpholinosydnonimine induces p53-dependent apoptosis, induces p53 accumulation and activates MAPK phosphorylation[1][2].
SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
GHRF, bovine (bGRF(1-44)-NH2) is the bovine growth hormone (GH)-releasing factor (GHRF). GHRF, bovine increases the release of bovine GH, and shows a synergistic effect with Hydrocortisone (HY-N0583)[1][2].
Roxyl-9 is a IDO1 (Indoleamine 2,3-dioxygenase 1) inhibitor[1].
α-Lipoic acid-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Coibamide A, an N-methyl-stabilized cytotoxic depsipeptide, shows potent antiproliferative activity. Coibamide A induces autophagosome accumulation via an mTOR-independent mechanism. Coibamide A induces apoptosis. Coibamide A inhibits VEGFA/VEGFR2 expression and suppresses tumor growth in glioblastoma xenografts[1][2].
nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research[1].
(E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic[1].
N-Methylcalycinine is a nature product with AChE inhibitory activity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on[1].
Procaspase-3/6 activator 1 (compound 1541) is a highly specific and robust activator of executioner procaspases-3 and -6, with EC50 values of 2.4 ± 0.2 and 2.8 ± 0.3 μM, respectively. Procaspase-3/6 activator 1 does not activate procaspases-1 or -7[1].
Cellobiohydrolase I (Cbh1) belongs to glycoside hydrolase family 7 (GH7) that catalyzes the processive hydrolysis of cellulose into cellobiose[1].
3',5'-TIPS-N-Ac-Adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].