BMS-751324 is a novel clinical prodrug of BMS-582949, which is a highly selective p38α MAPK inhibitor with IC50 of 13 nM; BMS-751324 is effectively bioconverted into parent drug BMS-582949 in vivo by alkaline phosphatase and esterase in a stepwise manner; demonstrates similar efficacy in rat LPS-induced TNFα pharmacodynamic model and rat adjuvant arthritis model compared with BMS-582949; BMS-751324 is indeed effective in addressing the pH-dependent absorption issue associated with BMS-582949.
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis[1].
Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is an FDA approved HER2-targeting ADC.
Caryolane-1,9β-diol (Treibs glycol; 3,6-Caryolanediol) is a natural compound isolated from the pods of Sindora sumatrana[1].
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, and CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer[1].
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively[1].
AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50= 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.
MRV03-037 is a selective colibactin-activated peptidase (ClbP) inhibitor that blocks the genotoxic effect of Colibactin (HY-145930) on eukaryotic cells. MRV03-037 prevents gut bacterial genotoxin production[1].
UK-2A (Antibiotic UK 2A) is a potent antifungal antibiotic. UK-2A shows antifungal activity[1][2].
D-Pentamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Pentamannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrPC) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis[1].
Saquinavir-d9 (Ro 31-8959-d9) is the deuterium labeled Saquinavir. Saquinavir(Ro 31-8959) is an HIV Protease inhibitor used in antiretroviral therapy. Saquinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.36 μM[1][2].
PNC-27 is an anticancer peptide, containing an HDM-2-binding domain. PNC-27 shows anti-tumor activity and can be used in acute myeloid leukemia research[1][2][3].
S-(+)-Mecamylamine (hydrochloride) is a neuronal nicotinic receptor modulator with antidepressant activity.
Bullatine A (BLA), a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A (BLA) is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses[1].Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed[2].
Warfarin sodium (WARF-42 sodium; Athrombine-K sodium) is a potent anticoagulant agent and a vitamin K1 recycling antagonist to deplete active vitamin K1. Warfarin sodium decreases blood coagulation and prevents blood clot formation by inhibiting vitamin K epoxide reductase[1][2].
Dipyrithione is a potent antimicrobial agent. Dipyrithione shows antifungal activity and antiproliferative activity. Dipyrithione induces apoptosis and cycle arrest at G1 phase. Dipyrithione shows anti-inflammatory activity in vivo. Dipyrithione shows anti-tumor activity. Dipyrithione has the potential for the research of dermatophytosis[1][2][3].
alpha-1,3-N-Acetylgalactosaminyltransferase (BgtA) is an acetylgalactose aminotransferase from Helicobacter mustelae which can specifically recognize Fucα1,2-Gal epitopes[1].
Synephrine (Oxedrine) hemitartrate, an alkaloid, is an α-adrenergic and β-adrenergic agonist derived from the Citrus aurantium. Synephrine hemitartrate is a sympathomimetic compound and can be used for weight loss[1][2].
DL-Tyrosine-d3 is the deuterium labeled DL-Tyrosine. DL-Tyrosine is an aromatic nonessential amino acid synthesized from the essential amino acid phenylalanine. DL-Tyrosine is a precursor for several important neurotransmitters (epinephrine, norepinephrine, dopamine)[1][2].
BNP (1-21), Pro (Human) is a peptide containg 21 amino acids[1].
Lasmiditan hydrochloride is a high-affinity, highly selective 5-HT1F receptor agonist (Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.IC50 value: 2.1 nM (Ki, 5-HT1F); >1000 nM (Ki, 5-HT1B/5-HT1D) [1]Target: 5-HT1F receptorin vitro: In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan show higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM.in vivo: In two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis).
12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway[1].12-HETE has both anti-thrombotic and pro-thrombotic effects[2]. 12-HETE is a neuromodulator[3].
CA inhibitor 1 is a potent HIV capsid inhibitor for HIV inhibition[1].
KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity.
TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.
Atrial Natriuretic Peptide (1-28), human, porcine, Biotin-labeled, one of three mammalian natriuretic peptides (NPs), has endocrine effects on fluid homeostasis and blood pressure. Atrial Natriuretic Peptide has the potential for cardiovascular diseases research[1][2].
Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity[1].
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research[1][2].
(+)-Bornyl acetate is found in pichtae essential oil (Siberian fir needle oil). (+)-Bornyl acetate has a stronger inhibitory effect on root growth of Arabidopsis seedlings[1][2][3].