activity

Zoledronic acid monohydrate (CGP 42446) is a synthetic imidazole bisphosphonate analog with anti-bone-resorption activity.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

inactive analog of the 3-phosphoglycerate dehydrogenase (PHGDH) inhibitors NCT-502 and NCT-503

Leptomerine (IC50 = 2.5 mM) shows potent anticholinesterasic activity.

Hexamethonium Bromide (Hexamethonium Dibromide), a specific antagonist of neuronal-type nicotinic AChR in ganglia, is poorly absorbed from the gastrointestinal tract and does not cross the blood-brain barrier.

Iriflophenone 3-C-glucoside (Iriflophenone 3-C-β-D-glucopyranoside),has antioxidant activity,isolated from Cyclopia genistoides.

Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively).

Puerarin-4'-O-β-D-glucopyranoside (Puerarin4'-O-glucoside) is a natural product isolated from Pueraria lobata root, exhibiting estrogenic activity and anti-proliferative effects in MCF-7 human breast carcinoma cells.

9-ING-41 is a glycogen synthase kinase-3 inhibitor.

CLK-IN-T3 is an inhibitor of CLK1, CLK2, and CLK3 with IC50s of 0.67, 15, and 110 nM. CLK-IN-T3 exhibits anti-cancer activity.

Fervenulin is isolated from a nematicidal actinomycete Streptomyces sp. CMU-MH021 with nematicidal activity. It also inhibits egg hatch and J2 mortality of M. incognita (MICs: 30 μg/mL and 120 μg/mL, respectively).

Mifobate (SR-202) is a potent and specific antagonist of PPARγ, exhibiting antiobesity, antidiabetic, and antiatherosclerotic effects[1].

trans-AUCB (t-AUCB) is an effective and selective soluble epoxide hydrolase inhibitor, with IC50 values of 1.3 nM for hsEH, 8 nM for mouse sEH, and 8 nM for rat sEH.

D-64131 is a tubulin polymerization inhibitor with an IC50 value of 0.53 μM.

MDR-652 is a highly specific and efficacious agonist of nonpungent transient receptor potential vanilloid 1 (TRPV1), with Ki values of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively, and EC50s of 5.05 nM and 93 nM for hTRPV1 and rTRPV1, respectively. MDR-652 is a potent topical analgesic.

1. Kakuol has antifungal activity, it can completely inhibit the mycelial growth of Botrytis cinerea Pers ex Fr and Cladosporium cucumerinum Ellis & Arthur at 5 microg ml(-1) and 3 microg ml(-1), respectively. 2. kakuol and a derivative analogue are able

SB-334867 free base (SB334867A free base) is a selective orexin-1 (OX1) receptor antagonist. In CHO-OX1 cells, SB-334867 inhibits calcium responses mediated by the human OX1 receptor in a concentration-dependent manner, with a binding pKi value of 7.17 for the human OX1 receptor.

(S)-crizotinib (ent-crizotinib) （IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

Reboxetine mesylate (FCE20124 mesylate) is a norepinephrine reuptake inhibitor with a Ki of 8.2 nM.

Datelliptium chloride hydrochloride is a DNA-intercalating agent derived from ellipticine, exhibiting anti-tumor activities.

AUDA is an inhibitor of sEH(IC50 values of 18 and 69 nM for the mouse and human enzymes, respectively)

THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).

BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV) with an EC50 of 1.8 μM, directly binding to a hydrophobic pocket of the BVDV RdRp, and demonstrating antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC).

Vomicine is a natural product from Strychnos nux-vomica, the S. nux-vomica extracts show antihyperglycemic activity in experimental animals.