m-PEG10-amine is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1]. m-PEG10-amine is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitory activity against α-glucosidase and PKCα (IC50 of 19.0 μM)[1][2][3].
Amino-PEG8-amine is a PEG-based (8 units) PROTAC linker can be used in the synthesis of PROTACs.
Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. IC50 Value: 0.25-1.2 nM(Ki for adrenergic receptor); 0.03-4.0 nM(Ki for 5-HT receptor)Target: 5-HT Receptor; Adrenergic ReceptorAsenapine maleate is a 5-HT receptor antagonist (5-HT1A,1B, 5-HT2A, 2B, 2C, 5-HT5A, 5-HT6 and 5-HT7), a D2 antagonist, and an antipsychotic. Asenapine has a broad receptor affinity profile for most serotonergic, dopaminergic, and adrenergic receptors, with no appreciable affinity for muscarinic receptors. Asenapine may be a helpful treatment option for patients with schizophrenia when weight gain, dyslipidemia, and endocrine abnormalities are a concern.
Clonidine-d4 is the deuterium labeled Clonidine. Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent[1][2][3][4][5].
OSu-PEG4-VC-PAB-MMAE involves in GDP-FAmP4MMAE (Monomethylauristatin E) synthesis, which is for GDP label via site-specific conjugation[1].
2,4,6-Triiodophenol is an orally active and potent leukotriene B4 (LTB4) synthesis inhibitor. 2,4,6-Triiodophenol can induce mouse blastocysts apoptosis[1][2].
Tubulin polymerization-IN-12 is a tubulin polymerization inhibitor (IC50=0.75 μM). Tubulin polymerization-IN-12 arrests cell cycle at G2/M phase, and exhibits cytotoxicity against cancer cells[1].
Angenomalin is a furanocoumarin from Angenlica anomala[1].
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
Shishijimicin A is a novel antitumor agent found from the Ascidian Didemnum proliferum. Shishijimicin A shows anti-tumor activity with highly potent cytotoxicities[1][2].
(R)-(-)-2-Butanol is released by the females of the white grub beetle, Dasylepida ishigakiensis, to attract males. (R)-(-)-2-Butanol is an intermediate of pharmaceutical synthesis by coupling[1][2].
Scaff10-8 is an inhibitor of AKAP-Lbc-RhoA interaction that acts by promoting the translocation of aquaporin-2 to the plasma membrane of renal collecting duct principal cells.
GSTO1-IN-1 is a potent glutathione S-transferase omega 1 (GSTO1) inhibitor with an IC50 of 31 nM.
DBCO-NH-(CH2)4COOH is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Alendronate sodium is an orally active nitrogen-containing bisphosphonate. Alendronate sodium potently inhibits bone resorption. Alendronate sodium is used for the research of postmenopausal osteoporosis[1].
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites[1].
BCL6-IN-5 is a potent BCL6 inhibitor exacted from patent WO2018215801A1, example 1n, has a pIC50 of 5.82[1].
MMP13-IN-31f is a highly potent, selective, orally bioavailable MMP-13 inhibitor with IC50 of 0.036 nM; exhibits 5,000-fold selectivity for MMP-13 over MMP-2, >1,500-fold selectivity over MMP-10, and >27,000-fold selectivity over MMP-1, 3, 7, 8, 9, 14, and TACE; prevents IL-1/OSM induced in vitro degradation of BNC (70.8% inhibition of cartilage degradation at 1 µM).
Notoginsenoside FP2, a dammarane-Type Bisdesmoside isolated from the Fruit Pedicels of Panax notoginseng, has potential to treat cardiovascular disease[1][2].
Neuropeptide S human is a potent endogenous neuropeptide S receptor agonist (EC50= 9.4 nM). Neuropeptide S human increases locomotor activity and wakefulness in mice. Neuropeptide S human also reduces anxiety-like behavior in mice.
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
Carmine (Carmine red), a "semi-synthetic" dye, is a complex of aluminum and the natural dye Cochineal (Carminic acid). Cochineal is isolated from the native Mexican and South American insect. Carmine is a widely used "natural" food additive. Carmine provokes both an immediate hypersensitivity and a delayed systemic response with cutaneous expression[1][2].
Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709)[1].
HMMNI-d3 is deuterium labeled HMMNI. HMMNI (Hydroxy dimetridazole) is a hydroxy metabolite of Dimetridazole. Dimetridazole is a nitroimidazole class drug that combats protozoan infections[1].
MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.target: 2-SORA [1]In vivo: MK-1064 promotes sleep and increases both rapid eye movement (REM) and non-REM (NREM) sleep in rats at OX2R occupancies higher than the range observed for dual orexin receptor antagonists. MK-1064 increases NREM and REM sleep in dogs without inducing cataplexy. The reference for animal administration is 30 mg/kg. [2]
FAK-IN-8 (compound 5h) is a FAK inhibitor (IC50=5.32 µM). FAK-IN-8 has good anti-proliferative activity and can be used in cancer research[1].
Trimethyloctadecylammonium bromide is an inhibitor of dynamin, with an IC50 value of 1.9 μM for dynamin I. Trimethyloctadecylammonium bromide exhibits antibacterial activity against Staphylococcus aureus[1][2].
α,ε-Dibenzoyl-DL-lysine is a lysine derivative[1].
Ethofumesate, a chiral herbicide, acts by inhibiting mitosis and reducing photosynthesis and plant respiration[1].