Elacridar Hcl (GF120918; GW0918) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.IC50 value:Target: P-glycoprotein In vitro, GF120918A demonstrated high plasma protein binding across species, although a definitive protein binding evaluation was precluded by poor recovery, particularly in buffer and in mouse, rat, and dog plasma. GF120918A did not demonstrate potent inhibition of several human cytochrome P450 enzymes evaluated in vitro, with IC(50) values well above concentrations anticipated to be achieved in vivo. Together, these data confirm the utility of GF120918A as a tool P-glycoprotein inhibitor in preclinical species and offer additional guidance on preclinical dose regimens likely to produce P-glycoprotein-mediated effects.

WL47 is a selective, high-affinity, disrupter of cavolin-1 oligomers (Kd=23 nM) than BSA, casein, and HEWL. WL47 is a caveolin-1 (CAV1) ligand and is 80% smaller in length than the original T20 parent sequence. WL47 can be used for the study of caveolin-1 function.

WL47 TFA is a selective, high-affinity, disrupter of cavolin-1 oligomers (Kd=23 nM) than BSA, casein, and HEWL. WL47 TFA is a caveolin-1 (CAV1) ligand and is 80% smaller in length than the original T20 parent sequence. WL47 TFA can be used for the study of caveolin-1 function.

Idalopirdine, also known as Lu AE58054 or Iladopirdine, is a potent and selective 5-HT6 receptor antagonist under development by Lundbeck as an augmentation therapy for the treatment of cognitive deficits associated with Alzheimer's disease and schizophrenia. It is in phase III clinical trials. Lu AE58054 displayed high affinity to the human 5-HT(6) receptor (5-HT(6)R) with a Ki of 0.83 nm. Lu AE58054 demonstrated >50-fold selectivity for more than 70 targets examined. Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia. Lu AE58054 may be useful for the pharmacotherapy of cognitive dysfunction in disease states such as schizophrenia and Alzheimer's disease.

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

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.

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.

ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.

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).

Cell permeable cAMP analog, acting as a cardiac stimulant and inhibiting phosphodiesterase

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.

IPN-60090 is an orally active and highly selective inhibitor of glutaminase 1 (GLS1; IC50=31 nM), with no activity observed against GLS-2. IPN-60090 exhibits excellent physicochemical and pharmacokinetic properties in vivo. IPN-60090 can be used for solid tumors research, such as lung and ovarian cancers.

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.

SMN2 splicing modulator TEC-1 is a novel specific, CNS penetrant small molecule SMN2 splicing modulator, increases the expression level of FL-SMN2 mRNA and decreases the expression level of Δ7 mRNA.TEC-1 showed higher selectively (>60-fold) on galactosylceramidase and huntingtin gene expression compared to previously reported compounds (e.g., SMN-C3) due to off-target effects on cryptic exon inclusion and nonsense-mediated mRNA decay.TEC-1 modulates SMN2 splicing and displays disease-modifying effects in motor neurons derived from SMA patient iPSCs (GM24468).|TEC-1 rescues the phenotype in a murine model of spinal muscular atrophy (SMA).

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.

AP 811 acetate is a selective atrial natriuretic peptide clearance receptor (ANP-CR, NPR3) antagonist with a Ki of 0.48 nM. AP 811 acetate displays >20000-fold selectivity for NPR3 over NPR1. AP 811 acetate abolishes ANP-induced pump stimulation.

JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research.

CYCA-117-70 is a DCAF1 ligand (KD: 70 μM). CYCA-117-70 is an ideal chemical handles for PROTACs recruiting DCAF1.

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].

S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC50 value of 3.04 nM. S19-1035 can be used for the research of tumor.

LOX-IN-3 Dihydrochloride is an orally active and selective lysyl oxidase (LOX) inhibitor.

Toluidine Blue is a basic thiazine metachromatic dye with high affinity for acidic tissue components. Toluidine Blue has wide applications in vital staining in living tissues and a special stain.