Agroclavine is a natural, clavine type of ergot alkaloid. Agroclavine is a D1 dopamine receptor and α1-adrenoceptor agonist. Agroclavine also has anticancer and antimicrobial activities[1][2].
Galanthamine is a potent acetylcholinesterase (AChE) inhibitor with an IC50 of 500 nM.
Arimoclomol citrate (BRX-220 citrate) is a co-inducer of heat shock proteins (HSP)[1]. Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system[2].
Chlorhexidine diacetate is a biguanide disinfectant with rapid bactericidal activity against both Gram-positive and Gram-negative organism. The antibacterial effect of chlorhexidine diacetate is related to its action on the bacterial cell membrane and to precipitation of intracellular contents[1].
Helospectin II is a neuropeptide of the vasoactive intestinal peptide (VIP) family. Helospectin II has vasodilatory and antihypertensive activities, and decreases blood pressure. Helospectin II is originally isolated from the salivary gland venom of the lizard Heloderma suspectum[1][2].
UPF 1069 is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
Tyr-Somatostatin-14 is a customized peptide that adds a Tyrosine amino acid to Somatostatin-14.
LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor[1][2].
Esculentin 1A is a frog skin-derived antimicrobial peptide (AMP) with potent in vitro anti-Pseudomonas activity[1].
MethADP (sodium salt) is a specific CD73 inhibitor.
N3-Gly-Gly-Gly-OH is a oligo-Gly click chemistry reagent containing an azide group. Oligo-Gly also has been used as linker to combine different subunits of dimeric or oligomeric proteins or to create artificial multi-domain proteins. By modification into Gly-Gly-Gly-Ser motifs high solubility can be achieved[1][2][3].
AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
6-Oxohexanoic acid is a non-cleavable modified MMAF-C5-COOH linker and can be used in the synthesis of modified MMAF-C5-COOH, a drug-linker conjugate for ADC[1].
Vatinoxan hydrochloride (MK-467 hydrochloride;L-659066 hydrochloride) is a peripheral α2 adrenergic receptor antagonist.
17:0-16:1 PE-d5 is deuterium labeled 17:0-16:1 PE.
Bonvalotidine A is a lycoctonine-type C19-diterpenoid alkaloid isolated from the roots of Delphinium bonvalotii Franch[1].
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50 of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation[1][2].
N-Desethyl Bimatoprost is a N-desethyl metabolite of Bimatoprost (HY-B0191)[1].
[Des-Tyr1]-Met-Enkephalin, a tetrapeptide, is a degradationproduct of enkephalins[1].
Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. Deslanoside inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations [1][2][3].
CC-90011 is a potent and orally active LSD1 inhibitor.
De-4’-O-methylyangambin is a lignan that can be isolated from Z. armatum. lignans are reported to has anti-inflammatory activity[1].
Arabinose-d1 is the deuterium labeled Arabinose. Arabinose is an endogenous metabolite[1].
Z-VDVA-(DL-Asp)-FMK is a Z-VDVAD-FMK derivative. Z-VDVAD-FMK (HY-P1008) is a special inhibitor of caspase-2[1].
2,4-Dihydroxybenzaldehyde is an endogenous metabolite.
H-Glu-Tyr-Glu-OH is a biologically active peptide.
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
MC-Thailanstatin A is a drug-Linker conjugates for ADC. MC-Thailanstatin A can be used for synthesis of ADCs[1].
D-Fructose-d2 is the deuterium labeled D-Fructose. D-Fructose (D(-)-Fructose) is a naturally occurring monosaccharide found in many plants[1].
PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.