H-DL-Nle-OH is a leucine derivative[1].
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells[1][2].
Pirozadil is a hypolipidemic agent.
(R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer[1][2].
6-(N-Boc)caproic acid NHS is a protein cross-linking agent.
Influenza A virus-IN-7 (compound 16r) is a potent and orally active influenza A virus inhibitor with an IC50 of 3.43 µM and CC50 of >100 µM. Influenza A virus-IN-7 shows anti-IAV activity with low cytotoxicity. Influenza A virus-IN-7 inhibits the transcription and replication of viral RNA[1].
Ponceau S is the most commonly used stain for Western blotting. Ponceau S is applied as an acidic aqueous solution, and it is compatible with antibody-antigen binding, and stains the proteins on the membrane red[1][2].
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H4 receptor over the H3 receptor with a Ki value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively[1][2].
Inz-5 is a fungal-selective mitochondrial cytochrome bc1 inhibitor. Inz-5 impairs fungal virulence and prevents the evolution of drug resistance[1].
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin is a highly selective probe for human cytochrome P450 2A6 (CYP2A6)[1][2].
18:0 LYSO-PE is an agent that can induce [Ca2+]i increase.
Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Triptonoterpene Me ether (compound 5) is a rosinane-type diterpenoid compound, which can be isolated from the traditional Chinese medicine Tripterygium wilfordii Hook. f[1].
YK11 is a partial agonist of androgen receptor, with osteogenic activity.
DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients[1].
Butylparaben sodium strongly influences the later stages of the spermatogenesis in the testis through the deterioration of hormonal control and/or RNA and protein synthesis[1].
(R)-methyl 2-amino-4-methylpentanoate hydrochloride is a leucine derivative[1].
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity[1][2][3].
N6-Benzoyl-5'-O-(4,4'-dimethoxytrityl)-3'-O-(2-methoxyethyl)adenosine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Rhamnolipid RL2, is a rhamnolipid, shows antifungal activity[1][2].
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer[1].
Akt Substrate (Akt/SKG substrate) is a 7 amino acid synthetic peptide suitable as a substrate for Akt[1].
CFM-2 is a selective non-competitive AMPAR antagonist.IC50 value:Target: AMPAR antagonistin vitro: AMPA antagonists GYKI 52466 and CFM-2 inhibit the extracellular signal regulated kinase (ERK1/2) pathway, CFM-2 reduced phosphorylation of cAMP-responsive element binding protein (CREB), suppressed expression of cyclin D1, upregulated the cell cycle regulators and tumor suppressor proteins p21 and p53 and decreased number of lung adenocarcinoma cells in G2 and S phases of the cell cycle.in vivo: Pretreatment with CFM-2 delayed the progression of seizure rank during repeated administration of pentylentetrazole. At the end of the period of repeated pentylentetrazole treatment (6 weeks) the mean seizure score was 0 in vehicle treated controls, 4.3 in animals treated with vehicle + pentylentetrazole, 2.2 in rats treated chronically with CFM-2 (20 micromol kg(-1) i.p.) + pentylentetrazole and 1.0 in rats treated repeatedly with CFM-2 (50 micromol kg(-1) i.p.) + pentylenetetrazole. CFM-2 was also able to antagonize the long-term increase in sensitivity of the convulsant effects of GABA function inhibitors in pentylentetrazole-kindled animals [1]. CFM-2 has been proven to possess anticonvulsant activity in various models of seizures [2]. Intrathecal application of two selective non-competitive AMPAR antagonists, CFM-2 (25 and 50 microg) and GYKI 52466 (50 microg), significantly attenuated mechanical and thermal hypersensitivities on the ipsilateral hind paw at 2 and 24 h post-CFA injection. Neither CFM-2 nor GYKI 52466 affected the contralateral basal responses to thermal and mechanical stimuli [4].
Azido-PEG4-Amido-tri-(t-butoxycarbonylethoxymethyl)-methane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist with an IC50 of 7.2 nM and a Ki of 0.2 nM[1].
Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies[1].
Propargyl-PEG2-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Pentetreotide is a diethylenetriaminopentaacetic (DTPA) conjugate of Octreotide. Pentetreotide is an indium-labelled somatostatin analog and can be uesd to nuclear medicine imaging. Somatostatin receptor scintigraphy with Pentetreotide is effective in visualizing neuroendocrine tumors, and its metastasis[1][2].
JE-2147 (AG1776) is a potent dipeptide protease inhibitor with a Ki of 0.33 nM for HIV-1 protease. JE-2147 has effective activities against a wide spectrum of HIV-1, HIV-2, simian immunodeficiency virus, and various clinical HIV-1 strains in vitro[1][2].
HCV-IN-39 (Compound 18a) is a potent hepatitis C virus (HCV) nucleoside inhibitor with EC50 values of 0.644, 0.952 and 0.154 μM against GT1a, GT1b and GT1b CES1 replicons[1].