Bremelanotide acetate is an analogue of the naturally occurring peptide alpha-MSH.

PLX5622 is a a potent, selective, orally active inhibitor of CSF1R tyrosine kinase (c-Fms) activity with Ki of 5.9 nM, 60-fold less potency against KIT.

Danazol is a derivative of the synthetic steroid ethisterone that suppresses the production of gonadotropins and has some weak androgenic effects. Before becoming available as a generic drug, danazol was marketed as Danocrine in the United States. It was approved by the US Food and Drug Administration (FDA) as the first drug to specifically treat endometriosis in the early 1970s. Although effective for endometriosis, its use is limited by its masculinizing side-effects. Its role as a treatment for endometriosis has been largely replaced by the GnRH agonists.

Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC50=69 nM) and constitutively active truncated AR splice variants (AR1-651 IC50=309 nM).

c-FMS-IN-8 is a potent, selective c-FMS kinase inhibitor with IC50 of 0.8 nM, shows activity in collagen-induced model of arthritis in mice..

D,L-Buthionine-(S,R)-sulfoximine is a potent inhibitor of glutamylcysteine synthetase biosynthesis.

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.

BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research.

M-110 is a potent, selective inhibitor of PIM kinase family with preference for PIM-3 with IC50 of 0.047, 2.5 and 2.5 uM for PIM3, PIM1 and PIM2, respectively.

CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity.

A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM).

Bentiamine is also known as Dibenzoyl Thiamine. Dibenzoyl Thiamine (Bentiamine), a derivative of thiamine, is rapidly absorbed into the body and converted to thiamine.

4,5-Dicaffeoylquinic acid ( Isochlorogenic acid C) possesses potent hepatoprotective and anti-HBV effects.IC50 value:Target: Anti-hepatitis natural produce.In vitro: To study anti-hepatitis effect of isochlorogenic acid C, anti-apoptotic and anti-injury properties of test compound were evaluated. The results showed that test compound at concentrations of 10 to 100 μg/ml significantly reduced the caspase-3 and transformed growth factor β1 (TGFβ1) levels of the D-GalN-challenged hepatocytes. Also, test compound improved markedly cell viability of the D-GalN-injured hepatocytes and produced a maximum protection rate of 47.28% at a concentration of 100 μg/ml. Furthermore, test compound significantly inhibited productions of HBsAg and HBeAg. Its maximum inhibitory rates on the HBsAg and HBeAg expressions were 86.93 and 59.79%, respectively. In addition, test compound significantly induced the HO-1 expression of HepG2.2.15 cells [1]. In vivo:

LKY-047 is a decursin derivative that potently and selectively inhibits CYP2J2, competitively inhibits CYP2J2-mediated astemizole O-demethylase and terfenadine hydroxylase activity with Ki of 0.96 and 2.61 uM, respectively.

VE-822 is a selective ATR inhibitor with an Ki value of 0.2 nM, >150 fold selectivity over ATM (Ki=34 nM), DNA-PK (Ki >4 uM) and mTOR (Ki >1 uM).

Isoniazid is an antibacterial agent used primarily as a tuberculostatic.Target: AntibacterialIsoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG [1]. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid, required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of isoniazid, including nitric oxide, which has also been shown to be important in the action of another antimycobacterial prodrug PA-824 [2, 3]. Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing [4].

Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. This agent may potentiate the anti-tumor activity of alkylating agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.

A potent, selective ubiquitin-specific protease USP8 inhibitor with IC50 of 0.28 uM.

ALLO-2 is a potent small molecule Smoothened (Smo) antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM.

JNK-IN-7 is a relatively selective JNKs inhibitor(IC50= 1.54/1.99/0.75 for JNK1/2/3); also bound to IRAK1, PIK3C3, PIP5K3 and PIP4K2C.

Cefotetan Sodium, also known as ICI-156834 and YM-09330, is a second-generation cephalosporin, cephamycin antibiotic that is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative bacteria. Cefotetan binds to penicillin-binding proteins and disrupts the cell wall synthesis.

JNJ-53718678 (JNJ53718678, JNJ-678) is a potent (Kd=7.4 nM), small-molecule inhibitor of the F-glycoprotein-mediated complex membrane fusion process of the RSV.

PF-06446846 (PF-6446846) is a potent, highly selective inhibitor of PCSK9 translation with IC50 of 0.3 uM for inhibition the secretion of PCSK9 by Huh7 cells.

SM-7368 inhibits TNF-alpha-induced MMP-9 upregulation in a concentration-dependent manner. SM-7368 strongly inhibits the TNF-alpha-induced invasion of HT1080 human fibrosarcoma cell line.

A cell-permeable, small-molecule c-Abl kinase activator with pEC50 of 6.1(EC50=794 nM).

ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958 is highly selective for B1 over B2 receptors, and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor.IC50 value: 0.26 nM (Ki)Target: B1 Receptorin vitro: ELN-441958 is a novel small molecule bradykinin B1 receptor antagonist, based on the inhibition of agonist-induced increases in intracellular calcium in native and recombinant cells. ELN-441958 does not inhibit the activation of the human bradykinin B2 receptor at concentrations up to 10 μM, showing that it is highly selective for B1 over B2 receptors. ELN-441958 also displays good selectivity for B1 over other receptors examined in a broad screening panel. It is >500-fold and >2000-fold selective for the B1 receptor over the human μ- and δ-opioid receptor, the most potent off-target activity identified. In IMR-90 cells expressing the native human B1 receptor, ELN-441958 produced a concentration-dependent antagonism of the DAKD-induced calcium mobilization with a KB of 0.12 nM. [1]in vivo: ELN-441958 is essentially completely absorbed and produces high plasma levels after oral administration in rhesus monkeys.ELN-441958 has a moderate clearance and volume of distribution in both species following i.v. administration, consistent with the high metabolic stability in rat, rhesus, and human microsomes. ELN-441958 has high oral exposure and moderate plasma half-lives in rats and rhesus monkeys. The oral availability of ELN441958 in rats was 57%. ELN-441958 dose-dependently reduced carrageenan-induced thermal hyperalgesia in a rhesus monkey tail-withdrawal model, with an ED50 3 mg/kg s.c. [1]

SMAD3 is a receptor-regulated intracellular protein that functions downstream of TGF-β and activin receptors and mediates their signaling, playing a role in cell proliferation, differentiation, apoptosis and formation of extracellular matrix. Smad3 Inhibitor, SIS3 is a cell-permeable pyrrolopyridine compound that selectively inhibits TGF-β1-dependent Smad3 phosphorylation and Smad3-mediated cellular signaling with no effect on Smad2, p38 MAPK, ERK, or PI 3-K signaling. It has been shown to reduce TGF-β1-induced type 1 procollagen expression and myofibroblast differentiation in normal dermal fibroblasts as well as scleroderma fibroblasts.

A novel potent, selective inhibitor of phosphorylation and transcriptional activity of STAT5, but not STAT3, AKT, or Erk1/2 phosphorylation.

A novel selective STAT3 inhibitor that inhibits JAK2-STAT3 activation but has no effects on other transcription factors such as NF-κB, and kinases such as AKT, ERK, and c-Src.