MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity[1][2].
5-Bromo-6-chloro-3-indolyl β-D-Galactopyranoside (contains ca. 10% Ethyl Acetate) (5-Bromo-6-chloro-3-indolyl-beta-D-galactoside) is a chromogenic substrate of β-galactosidase (β-gal)[1].
Eldocasiran is a micro-ARN-193a-3p analogue, Eldocasiran has anticancer activity. Eldocasiran can be used for cancer research[1].
Doravirine is a novel non-nucleoside inhibitor of HIV-1 reverse transcriptase with potent activity against wild-type virus (95% inhibitory concentration 19 nM, 50% human serum). target:HIV [1]In vitro: Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1] MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2]In vivo: Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3]
Glutaminase C-IN-1 (968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
Elastase LasB-IN-1 (Compound 4b) has antibacterial activity. Elastase LasB-IN-1 (Compound 4b) is a selective elastase LasB inhibitor with an IC50 value of 76 nM[1].
1-O-Gentiobiosyl-3,7-dimethoxy-8-hydroxyxanthone (Compound 18) is a natural product that can be isolated from Swertia mussotii[1].
Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation[1].
Biotin-TAT (47-57), biotin tagged TAT, is a transactivator of transcription. Biotin-TAT (47-57) is one of the most widely used PTDs into different primary cells is ATP- and temperature-dependent, indicating the involvement of endocytosis[1][2].
Lisinopril is angiotensin-converting enzyme inhibitor, used in treatment of hypertension, congestive heart failure, and heart attacks.Target: ACELisinopril is a potent, competitive inhibitor of angiotensin-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII). ATII regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS). Lisinopril may be used to treat hypertension and symptomatic congestive heart failure, to improve survival in certain individuals following myocardial infarction, and to prevent progression of renal disease in hypertensive patients with diabetes mellitus and microalbuminuria or overt nephropathy [1, 2].
3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae)[1].
PA452, retinoic X receptor (RXR) specific antagonist, inhibits the effect of Retinoic acid (RA) on Th1/Th2 development[1].
α-Helical Corticotropin Releasing Factor (9-41) is a corticotropin releasing factor (CRF) antagonist. α-Helical Corticotropin Releasing Factor (9-41) decreases plasma growth hormone (GH) values in vivo[1][2].
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant[1].
Odoratisol B is a natural product that can be isolated from Machilus odoratissima NEES[1].
GHRF, mouse, a mouse growth hormone-releasing factor, is a peptide containing 44 amino acids. GHRF, mouse stimulates the release and synthesis of growth hormone[1].
Ivangustin is a sesquiterpene isolated from the flower heads of the medicinal plant Inula britannica[1].
MC-AlkyMC-Alkyl-Hydrazine is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Boc-D-Tyr-OH is a tyrosine derivative[1].
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas[1][2].
Olmesartan ethyl ester (compound 11) is an Olmesartan impurity. Olmesartan (RNH-6270) is an angiotensin II receptor (AT1R) antagonist used to in the high blood pressure study[1].
Lu AF27139 is a novel rodent-active and CNS-penetrant P2X7 receptor antagonist. Lu AF27139 is highly selective and potent against rat, mouse, and human forms of the receptors. The rat pharmacokinetic profile is favorable with high oral bioavailability, modest clearance (0.79 L/(h kg)), and good CNS permeability. Importantly, Lu AF27139 was without effect in standard in vitro and in vivo toxicity studies. Lu AF27139 is a valuable tool for probing the role of the P2X7 receptor in rodent models of CNS diseases.
ABMA is a novel broad-spectrum inhibitor of intracellular toxins and pathogens, efficiently protects cells against various toxins and pathogens including viruses, intracellular bacteria and parasite; protects mice from nasal instillation of an LD90 of ricin; provokes Rab7-positive late endosomal compartment accumulation in mammalian cells without affecting other organelles.
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
Lamivudine (BCH-189) salicylate is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Lamivudine salicylate can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS[1][2].
BIBR 1087 SE is an intermediate metabolite of dabigatran etexilate.
MoTP is a specific platelet activating factor receptor antagonist and can induce melanocyte ablation. MoTP can be used for the research of cancer.
Sulfinalol is an orally active β-adrenoceptor antagonist with direct vasodilator activity[1].
Regaloside B is a phenylpropanoid isolated from Lilium longiflorum. Regaloside B can inhibit the expression of iNOS and COX-2, has anti-inflammatory activity[1][2].