Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), .6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation[1][3][5].
Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell[1].
Oleoside can be isolated from olive pomace[1].
Dihydralazine sulfate is an antihypertensive agent.
Thalidomide-5-PEG2-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-PEG2-Cl can be connected to the ligand for protein by a linker to form PROTACs[1].
Isobutylparaben (Isobutyl 4-hydroxybenzoate) is a constitutive androstane receptor (CAR) activator. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics[1].
Isoprothiolane is a systemic fungicide. Isoprothiolane is a rice blast controlling agent against the fungal disease of rice planty Pyvioutavia oryzae Cav[1].
MethylCBI-azaindole-benzamide-MOM-Boc-ethylenediamine-D is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
5-Furan-2-yl-2’-O-methyl uridine 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].
Caprochlorone has antiviral activity against orthopoxvirus. Caprochlorone can inhibit cell penetration by virus, also delays release of newly formed virus from the cell. Caprochlorone decreases the titers of influenza virus in infected-mice lungs[1][2][3].
Mirococept (APT070) is an antibody targeting to complement system C3b/C4b, as well as a membrane-localizing C3 convertase inhibitor. Mirococept reduces the release of C-peptide and pro-inflammatory cytokines, and reduces the infiltration of inflammatory cells. Mirococept reduces intraislet inflammation, which is beneficial to islet transplantation. Mirococept also inhibits increased intestinal and pulmonary vascular permeability to reduce neutrophil influx[1][2].
Trimethoprim propanoic acid is a hapten.
D-Tyrosine-d7 is the deuterium labeled D-Tyrosine. D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth[1][2].
Hederacoside C is a principal bioactive pharmaceutical ingredient of Hedera helix leaf that can treat respiratory disorders, because of its expectorant, bronchodilator, antibacterial, and bronchospasmolytic effects.
EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis[1].
Imidazole is a planar 5-membered ring. Imidazole is a highly polar compound. Imidazole has been used extensively as a corrosion inhibitor.Imidazole is incorporated into many important biological molecules. The most pervasive is the amino acid histidine, which has an imidazole side-chain. Imidazole is useful as a buffer in the pH range of 6.2-7.8 One of the applications of imidazole is in the purification of His-tagged proteins in immobilised metal affinity chromatography(IMAC). Imidazole is used to elute tagged proteins bound to Ni ions attached to the surface of beads in the chromatography column. An excess of imidazole is passed through the column, which displaces the His-tag from nickel co-ordination, freeing the His-tagged proteins. Imidazole has become an important part of many pharmaceuticals. Synthetic imidazoles are present in many fungicides and antifungal, antiprotozoal, and antihypertensive medications. Imidazole is part of the theophylline molecule, found in tea leaves and coffee beans, which stimulates the central nervous system. It is present in the anticancer medication mercaptopurine, which combats leukemia by interfering with DNA activities.
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
Met-Enkephalin-Arg-Phe is a naturally occurring heptapeptide with analgesic activity[1].
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae[1].
(3β,20E)-24-Norchola-5,20(22)-diene-3,23-diol is a steroid-based allylic alcohol.
PS-432 is an allosteric inhibitor of PKCι and PKCζ with IC50 of 16.9 and 18.5 uM, respectively; has no inhibitory activity against PKCα, PKCβ, PKCδ and PKCθ nor the activity of related kinases such as PDK1, PKB/Akt, RSK1, MSK1 and Aurora A; inhibits the proliferation of the lung cancer cell lines A549 (IC50=14.8 ± 4.2 uM) and A427 (IC50=10.4± 0.3 uM) as well as androgen-independent prostate cancer cell line DU145 (IC50 = 20.8 ± 9.0 uM); well tolerated in vivo.
VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain[1].
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme[1].
Sodium Nitroprusside is a potent vasodilator working through releasing NO spontaneously in blood.Target: OthersSodium Nitroprusside is a potent vasodilator. Sodium nitroprusside has potent vasodilating effects in arterioles and venules. Sodium Nitroprusside breaks down in circulation to release nitric oxide (NO). NO activates guanylate cyclase in vascular smooth muscle and increases intracellular production of cGMP. The end result is vascular smooth muscle relaxation, which allow vessels to dilate [1]. Sodium nitroprusside decreases the proliferation of vascular smooth muscle cells [2]. Sodium nitroprusside (5 mg/kg) significantly reduces the intestinal ischemiareperfusion injury as a nitric oxide donor in rats [3].
Doxycycline calcium, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor[1]. Doxycycline calcium shows antibacterial activity and anti-cancer cell proliferation activity[1][2][3][4][5].
Maprotiline HCl is a selective noradrenalin re-uptake inhibitor and a tetracyclic antidepressant.Target: OthersMaprotiline (sold as Deprilept, Ludiomil, Psymion) is a tetracyclic antidepressant (TeCA). However, Maprotiline's fourth ring is spurious, as formed by a bridge across the central tricyclic ring. It is a strong norepinephrine reuptake inhibitor with only weak effects on serotonin and dopamine reuptake. It exerts strong blocking effect at H1 receptors, moderate at 5-HT2 and alpha1 and weak blocking effect at D2 and mACh postsynaptic receptors [1, 2].
LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines[1].
Isopimpinellin, an orally active compound isolated from the roots of Pimpinella saxifrage. Isopimpinellin blocks DNA adduct formation and skin tumor initiation by 7,12-dimethylbenz[a]anthracene. Isopimpinellin possesses anti-leishmania effect[1].
M62812 is a toll-like receptor 4 (TLR4) signaling inhibitor. M62812 inhibits endothelial and leukocyte activation and prevents lethal septic shock in mice. M62812 can reduces LPS-induced coagulation and inflammatory responses. M62812 can be used for the research of sepsis[1].