Fasnall is a selective fatty acid synthase (FASN) inhibitor with an IC50 of 3.71 μM. Fasnall induces apoptosis in HER2+ breast cancer cell lines. Fasnall shows potent anti-tumor activities[1].
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment[1][2].
Azathioprine(Azasan, Imuran; BW 57-322) is a drug that suppresses the immune system and is used in organ transplantation and autoimmune disease. Target: Azathioprine is an immunosuppressive antimetabolite pro-drug. It is an imidazolyl derivative of 6-mercaptopurine and many of its biological effects are similar to those of the parent compound. Azathioprine is converted into 6-mercaptopurine in the body where it blocks purine metabolism and DNA synthesis. Thus it most strongly affects proliferating cells, such as the T cells and B cells of the immune system. The main adverse effect of azathioprine is bone marrow suppression, which can be life-threatening, especially in people with a genetic deficiency of the enzyme thiopurine S-methyltransferase. It is also listed by the International Agency for Research on Cancer as a Group 1 carcinogen (carcinogenic to humans) [1-3].
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD)[1][2].
Phenoxypropazine is a potent monoamine oxidase (MAO) inhibitor. Phenoxypropazine can be used in research of depression[1].
Urechistachykinin II (Uru-TK II), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect[1][2].
Zeylenone, isolated from ethanol extract of the leaves of Uvaria grandiflora Roxb. Zeylenone, a naturally occurring cyclohexene oxide, inhibits proliferation and induces apoptosis in cervical carcinoma cells via PI3K/AKT/mTOR and MAPK/ERK pathways[1].
UCM-1336 is a potent ICMT inhibitor, with an IC50 of 2 μM. UCM-1336 induces mislocalization of endogenous Ras, decreases Ras activation and induces cell death by autophagy and apoptosis[1].
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modifies the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium[1][2].
Propan-1-amine-dd5 hydrochloride is the deuterium labeled Propan-1-amine hydrochloride[1].
Pyraclostrobin is a strobilurin fungicide that inhibits mitochondrial complex III of fungal and mammalian cells. Pyraclostrobin induces triglyceride accumulation and triglyceride accumulation in 3T3-L1 cells.
17α-Hydroxyprogesterone acetate possesses progestational activity. 17α-Hydroxyprogesterone acetate has antiinflammatory effects at the murine maternal-fetal interface[1][2].
Antioxidant agent-7 (SD-7) is a benzodiazepine derivative with antioxidant activity with an IC50 value of 470 nM to scavenge DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical[1].
PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src.
Stylopine hydrochloride (Tetrahydrocoptisine hydrochloride) is an alkaloid compound originally isolated from Corydalis tubers that exhibits anti-inflammatory and anti-parasitic activities[1][2].
Calcium Green 1AM is a cell-permeant fluorescent calcium indicator (Excitation 506 nm; Emission 531 nm). Calcium Green 1AM is converted to the fluorescent calcium indicator by intracellular esterases[1].
DL001, a FKBP12-dependent rapamycin analog, is a selective mechanistic Target Of Rapamycin Complex 1 (mTORC1) inhibitor with an IC50 of 74.9 pM. In cells, DL001 efficiently represses elevated mTORC1 activity and restores normal gene expression to cells lacking a functional tuberous sclerosis complex. DL001 inhibits mTORC1 signaling without impairing glucose homeostasis and with substantially reduced and no side effects on lipid metabolism and the immune system in vivo in C57BL/6J mice[1].
Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis[1].
Disomotide (G209-2M) is a melanoma antigen that enhances the generation of cytotoxic T lymphocytes (CTL) recognizing native G209 as well as melanoma[1][2].
AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects[1].
EP2 receptor antagonist-2 (CID891729) is an antagonist of EP2 receptor. EP2 receptor antagonist-2 inhibits the EP2 receptor activation induced by PGE2. EP2 receptor antagonist-2 also suppresses lactate dehydrogenase (LDH) release induced by N-methyl-D-aspartate (NMDA)[1].
Hulupinic acid is a prominent oxidation product of hop acids[1].
Z-VRPR-FMK is an irreversible MALT1 protein inhibitor. Z-VRPR-FMK inhibits the growth and invasion of diffuse large B-cell lymphoma by inhibiting MALT1-induced NF-κB activation and MMP expression[1].
Glenzocimab (ACT017) is a Fab fragment of humanized anti-GPVI monoclonal antibody. Glenzocimab inhibits collagen-induced platelet aggregation. Glenzocimab has the potential for the research of acute ischemic stroke[1][2].
Sulfamonomethoxine sodium is a long acting sulfonamide?antibacterial?agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate[1].
Fmoc-Glu-O-2-PhiPr is a glutamic acid derivative[1].
Desglymidodrine (ST 1059), the active metabolite of midodrine, is a selective α1-adrenoceptor agonist. Desglymidodrine is an effective arterial and venous vasoconstrictor and can be used to regulate blood pressure[1][2].
6PPD-quinone-d5 is the deuterium labeled 6PPD-quinone[1].
(S)-IDO1-IN-5 is the S-isomer of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1[1].
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo[1][2].