Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research[1][2][3].
N-(2,4-Dinitrophenyl)-L-phenylalanine is an alanine derivative[1].
Griseoluteic acid, a phenazine antibiotic, is originally isolated from S. griseoluteus. Griseoluteic acid is a breakdown product of griseolutein A and B[1].
Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.
Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal and anticancer activity.IC50 value:Target:in vitro: Dihydrosanguinarine showed much less cytotoxicity than sanguinarine: at the highest concentration tested (20 microM) and 24h exposure, dihydrosanguinarine decreased viability only to 52% [1]. Dihydrosanguinarine showed the highest antifungal activity against B. cinerea Pers, with 95.16% mycelial growth inhibition at 50 μg/ml [2]. dihydrosanguinarine showed the most potent leishmanicidal activities (IC(50) value: 0.014 microg/ml, respectively) [4].in vivo: Repeated dosing of DHSG for 90 days at up to 500 ppm in the diet (i.e. approximately 58 mg/kg/day) showed no evidence of toxicity in contrast to results published in the literature [3].
Urotensin II-related peptide is a human urotensin II anague. Urotensin II-related peptide has high affinity for the UT receptor[1][2].
Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC).
PCI-27483 is a FVIIa/tissue factor inhibitor, with antitumour effects.
Guanabenz (hydrochloride) is an oral α-2-adrenoceptor agonist, has antihypertensive effect and antiparasitic activity. Guanabenz (hydrochloride) interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz (hydrochloride) also is used for the research of high blood pressure(equivalent).
N4-Acetylsulfamethoxazole (Acetylsulfamethoxazole) is a metabolite of Sulfamethoxazole (HY-B0322). Sulfamethoxazole is a sulfonamide bacteriostatic antibiotic, used for bacterial infections[1].
Paraquat dichloride is an orally active, fast-acting, non-selective contact herbicide that is absorbed by leaves through some translocation of xylem. The adsorption of Paraquat dichloride is weakly dependent on PH value[1][2][3][4].
ETC-206 is a selective MNK1 and MNK2 inhibitor with IC50s of 64 nM and 86 nM, respectively.
BRD9539 inhibits G9a activity with an IC50 of 6.3 μM, inhibits PRC2 activity with a similar IC50.target: G9a, PRC2;IC50: 6.3 μM ( G9a ), 6.3 uM ( PRC2 ); BRD9539 is a more potent biochemical inhibitor than its methyl-ester analogue BRD4770, with 20% remaining G9a activity compared to 45% of BRD4770 at screening concentration.
Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
N-Boc-PEG10-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
RG7800 a small molecule SMN2 splicing modifier to enter human clinical trials to treat spinal muscular atrophy.
Isoanthricin ((Rac)-Deoxypodophyllotoxin) is the racemate of Deoxypodophyllotoxin. Deoxypodophyllotoxin is a potent antitumor and anti-inflammatory agent[1][2].
Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM.
Acetyl-(D-Arg2)-GRF (1-29) amide (human) is an antagonist of growth hormone releasing factor (GRF). Acetyl-(D-Arg2)-GRF (1-29) amide (human) inhibits the release of growth hormone (GH) and can be used for endocrine research[1].
Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers[1][2].
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H+/K+-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor[1][2].
BAPTA-APM is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer[1].
Aripiprazole lauroxil, an N-acyloxymethyl prodrug of aripiprazole, is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity[1].
Samelisant (SUVN-G3031) is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant has a similar binding affinity towards human (hH3R; Ki=8.7 nM) and rat (rH3R;Ki=9.8 nM) H3R indicating no inter-species differences. Samelisant can be used for the research of sleep-related disorders[1].
Methyl β-D-glucopyranoside is used to synthesize natural glycophenolics via enzymatic caffeoylation[1].
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
Gomisin L1 is a lignan, shows inhibitory effect on cell viability of A2780 and Ishikawa cells, with IC50s of 39.06 μM and 74.16 μM, respectively[1].
Ciprofloxacin hydrochloride is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity.