Isonipecotic acid is a GABAA receptor partial agonist[1].
(Rac)-SAR131675 is the racemate of SAR131675. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM[1][2].
Vallesiachotamine, a known monoterpene indole alkaloid, possesses anti-tumor activity[1].
Diethylstilbestrol-d3 is deuterium labeled Diethylstilbestrol.
Ravoxertinib (GDC-0994) is an orally bioavailable ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
Ald-Ph-PEG4-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
DSPE-glutaric acid is a lipid. DSPE-glutaric acid can be used for the research of various biochemical[1].
PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective[1][2][3].
TUS-007 is a CANDDY molecular, modified from a proteasome inhibitor. However, TUS-007 hardly inhibits proteasome activity. TUS-007 is also an orally active and potent KRAS G12D/V degrader. TUS-007 can be applied in KRAS G12D/V chemical knockdown in cell-free. TUS-007 also exhibits tumor suppression[1]. Note: CANDDY refers to Chemical knockdown with Affinity aNd Degradation DYnamics.
AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions[1][2].
Cinsebrutinib is a Bruton's tyrosine kinase inhibitor, extracted from patent WO2021207549 (compound 5-6). Cinsebrutinib has the potential for cancer study.
Altenuene is a heptaketide isolated from an endolichenic fungal strain Nigrospora sphaerica[1].
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma[1][2].
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties[1][2][3].
McN5691 is a voltage-sensitive calcium channel blocker.
Fmoc-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
Benzyl-PEG7-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Firocoxib-d4 (ML 1785713-d4) is the deuterium labeled Firocoxib. Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1].
Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis[1].
Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin. Rhapontigenin is a potent inactivator of human P450 1A1 and is a good candidate for a cancer chemopreventive agent[1].
Methyl 2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetate, a natural coumarins derivative, is exploited for the synthesis of the switchable fluorescent substrates to be used in bacterial enzyme detection[1][2][3].
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 µM and 0.84 µM against wild-type and drug resistant HBV strains, respectively[1].
BI-3802 is a highly potent BCL6 degrader, inhibiting the BTB domain of BCL6, with an IC50 of ≤3 nM; BI-3802 has antitumor activity.
Emoghrelin, isolated from? Heshouwu Polygonum multiflorum, stimulates growth hormone secretion via activation of the ghrelin receptor[1].
Propoxur is a carbamate insecticide with a fast knockdown and long residual effect used against turf, forestry, and household pests and fleas.
Metamizol (Methamizole) is an anti-thyroid agent, which blocks thyroid hormone production from the thyroid gland. Metamizol can cause hepatotoxicity[1].
Diphenyl-2,2′,4,4′,6,6′-methylamine-d6 is the deuterium labeled Diphenyl-methylamine[1].
UK-52831, a calcium channel antagonist, is used potentially for the treatment of hypertension and myocardia ischemia.
(tert-Butoxycarbonyl)-L-leucylglycine is a Glycine (HY-Y0966) derivative[1].