Chlorophenothane-d8 is the deuterium labeled Chlorophenothane. Chlorophenothane has stomach poisoning and contact killing effects. Chlorophenothane has been widely used as an insecticide[1][2].
Methyl (6-chloropyrimidin-4-yl)glycinate is a Glycine (HY-Y0966) derivative[1].
(S)-2-(Benzylamino)-3-(4-hydroxyphenyl)propanoic acid is a tyrosine derivative[1].
A-908292 is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 38 nM (hACC2), no activity against ACC1 (IC50>30 uM).
MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM. IC50 Value: 16 nM (Human Liver FBPase) [1]Target: Fructose 1, 6-bisphosphataseOral delivery of MB05032 was achieved by using the bisamidate prodrug MB06322 (CS-917), which is converted to MB05032 in two steps through the action of an esterase and a phosphoramidase.in vitro: MB05032 inhibits human liver FBPase with a potency (IC50 = 16 ± 1.5 nM) significantly greater than the natural inhibitor, AMP (IC50 = 1 μM), and the most well characterized AMP mimetic, ZMP (IC50 = 12 ± 1.4 μM). MB05032 inhibits rat FBPase 3-fold weaker (IC50 of 61 ± 4 nM) than human FBPase, whereas AMP is 20-fold weaker as an inhibitor [1]. Inhibition of FBPase activity in islet β-cells by its specific inhibitor MB05032 led to significant increase of their glucose utilization and cellular ATP to ADP ratios and consequently enhanced GSIS in vitro [2]. in vivo: Oral administration of MB06322 to young (8-9 weeks old) ZDF rats with mild diabetes (basal insulin levels of 7.7 ± 0.7 ng/ml) and aged (12-13 weeks) ZDF rats with overt diabetes (basal insulin levels of 0.65 ± 0.16 ng/ml) results in dose-dependent glucose lowering. The dose-response is relatively steep, with 6-10 mg/kg and 30-100 mg/kg being the approximate doses associated with minimal and maximal activity, respectively [1]. Pretreatment of mice with the MB05032 prodrug MB06322 could potentiate GSIS in vivo and improve their glucose tolerance [2].Toxicity: Neither lactate nor triglycerides increased in 8- to 9-week-old ZDF rats with mild diabetes treated with high doses of MB06322. In ZDF rats with more advanced disease, lactate and triglyceride levels were elevated but only modestly (<2-fold). These results suggest that, unlike inhibitors of other GNG enzymes, FBPase inhibitors may lower glucose with an adequate safety margin [1].Clinical trial: Evaluation of Glucose Lowering Effect, Safety and Tolerability of CS-917. Phase 2b
WAY-312491 is an active molecule.
Biotinyl-NH-PEG3-C3-amido-C3-COOH (DIPEA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(R)-mchm5U is a diastereomer of (S)-mchm5U (HY-153100A)[1].
Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.
D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.
H-Gly-Arg-Ala-Asp-Ser-Pro-OH (GRADSP) is a negative control peptide of GRGDdSP[1].
PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein hydrolysis. PROTAC KRAS G12C degrader-2 is a bifunctional compound, which contain on one end a cereblon inhibitor of apoptosis proteins (IAP) and on the other end a moiety which binds KRAS[1].
Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
E3 ligase Ligand-Linker Conjugates 34 Hydrochloride incorporates a cIAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. E3 ligase Ligand-Linker Conjugates 34 Hydrochloride can be used to design PROTAC degrader[1].
(R)-OP-1074 is the inactive isomer of OP-1074 (HY-125263), and can be used as an experimental control. OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2?nM, respectively[1].
XT-4 is an antimicrobial peptide derived from skin secretions of Xenopus tropicalis. XT-4 has strong activity against E.coli, the vaule of MIC is 18 μM[1].
Pomalidomide-6-OH is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-OH can be connected to the ligand for protein by a linker to form PROTAC[1].
RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). IC50 value: 7 nM (Ki, fot androgen receptor) [1]Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM). [1] RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.[2]in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys. [1] RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.[2]
Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin[1].
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at opioid-like NOP receptors. Naloxone benzoylhydrazone has potently analgesia effect[1][2][3].
N-Fmoc-N-methoxy-3-aminopropionic acid, a Weinreb amide linker, is a protein cross-linking agent[1].
Digeranyl bisphophonate is a potent geranylgeranylpyrophosphate (GGPP) synthase inhibitor, which inhibits geranylgeranylation of Rac1.
Green DND-26 is used to mark acidic lysosomes to determine the cellular distribution. Green DND-26 is a fluorescent dye that stains acidic compartments in live cells and has been shown to selectively accumulate in lamellar bodies in alveolar type II (AT2) cells in the lung[1][2].
m-PEG3-CH2COOH is a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.
2-(((Benzyloxy)carbonyl)amino)propanoic acid is an alanine derivative[1].
3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively[1].
Sorbitol dehydrogenase-IN-1 is a potent and orally active sorbitol dehydrogenase inhibitor with IC50 s of 4, 5 nM for rat and human, respectively[1].
Penicillin G benzathine (Benzathine benzylpenicillin) is an antibiotic against many bacterial infections[1].
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.