Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
4’-C-Methyl-4-deoxyuridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Thiocystine is a relatively stable trisulfide analog of Cystine. Thiocystine functions as a persullide in transferring its sulfane sulfur to thiophilic acceptors[1][2].
Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 11 can bind to BTK[1].
Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer[1].
AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
PHD2-IN-1 is a potent and orally active inhibitor of HIF prolyl hydroxylase 2 (PHD2) with an IC50 of 22.53 nM. PHD2-IN-1 can be used for anemia research[1].
Ceftobiprole medocaril (BAL5788) sodium is the parenteral prodrug of Ceftobiprole (HY-112579). Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens[1][2].
TIM-063 (TIM063) is a potent, selective, ATP-competitive CaMKK inhibitor with Ki of 0.35/0.2 uM for CaMKKα and CaMKKβ, respectively.TIM-063 directly targets the catalytic domain of CaMKK, similar to STO-609.TIM-063 suppressed the ionomycin-induced phosphorylation of exogenously expressed CaMKI, CaMKIV, and endogenous AMPKα in HeLa cells with an IC50 of 0.3 uM.TIM-063 suppressed CaMKK isoform-mediated CaMKIV phosphorylation in transfected COS-7 cells.TIM-063 displayed cell permeability and the ability to inhibit CaMKK activity in cells. TIM-063 is a useful chemical probe for the precise analysis of CaMKK-mediated signaling pathways.
D-(-)-Quinic acid is a cyclohexanecarboxylic acid and is implicated in the perceived acidity of coffee.
Anticancer agent 72 (compound 8c) is a potent inhibitor of K+ channel. Anticancer agent 72 induces apoptosis[1].
Lacutamab (IPH4102) is a humanized monoclonal antibody (mAb) directed against the immune receptor molecule KIR3DL2, produced by recombinant technology in CHO cells. Lacutamab can be used in research of cutaneous T-cell lymphoma[1].
Deoxycalyciphylline B is a hepatotoxic alkaloid that can be isolated from Daphniphyllum calycinum[1].
STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 STX-478 shows robust and durable tumor regression and can be used in cancer research[1].
A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO).
Diethylglycine is a Glycine (HY-Y0966) derivative[1].
Alpha-ketoisocaproic acid-13C5 (sodium) is the 13C labeled Alpha-ketoisocaproic acid sodium[1].
Galanin-B2 (NAX-5055) has activity in the epilepsy model. Galanin-B2 can penetrate the blood-brain-barrier[1].
Deltorphin I is a δ-opioid receptor agonist with high affinity and selectivity.
FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 nM and 0.5 nM for Plasmodium falciparum and human, respectively[1].
mTOR Inhibitor 1 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR Inhibitor 1 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates[1].
N-Boc-N-bis(PEG3-acid) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).IC50 value: 50 nM [1]Target: Pim-1TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism. Preliminary data further suggested that 1 lacked in vitro inhibitory activity toward related serine/threonine kinases Pim-2 and MEK1/2 (IC50 > 20 lM). Hence, small molecules similar to TCS PIM-1 1 may serve as useful starting scaffolds for the development of other improved yet selective Pim-1 inhibitors.
Chitin synthase inhibitor 14 (compound 4n) is chitin synthase (CHS) inhibitor. Chitin synthase inhibitor 14 has antifungal activity while possessed the potency against drug-resistant fungal variants[1].
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM[1].
Yuanhuadin, extracted from Genkwa Flos Daphne genkwa, has antitumor activity through inhibiting Akt/mTOR and EGFR pathways, induce cell-cycle arrest and abortion[1].
Crenatine is an antibacterial agent. Crenatine is more effective against Gram-positive than Gram-negative bacteria[1].
PDE10-IN-2 is a PDE10 inhibitor with an IC50≦0.01 μM[1].
Nimbolide is a triterpene derived from the leaves and flowers of neem (Azadirachta indica L). Nimbolide induces apoptosis through inactivation of NF-κB. Nimbolide inhibits CDK4/CDK6 kinase activity. Nimbolide suppresses the NF-κB, Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways[1].
Epoxomicin is a cell-permeable and irreversible proteasome inhibitor, primarily the chymotrypsin-like activity.