Kemptide (amide) is a heptapeptide with properties of a cytophilic substrate. Kemptide is a molecule preserving cell membrane intactness, is phosphorylated by PKI, the inhibitory protein specific for cAMP-dependent protein kinase (PK)[1].
Werner syndrome RecQ helicase-IN-3 is a potent and orally active werner syndrome recQ helicase (WRN) inhibitor with an IC50 value of 0.06 µM. Werner syndrome RecQ helicase-IN-3 shows antiproliferative activity. Werner syndrome RecQ helicase-IN-3 shows anticancer activity[1].
DCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects[1].
Regdanvimab (CT-P59) is a human monoclonal antibody that targets the receptor-binding domain of SARS-CoV-2 spike protein, blocking interaction with ACE2 for viral entry. Regdanvimab can be used for the research of COVID-19[1].
2-Aminoethan-1-ol-13C2 hydrochloride is the 13C labeled 2-Aminoethan-1-ol hydrochloride[1].
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF)[1].
SCO-PEG3-NHS is a PEG linker with a terminal imine(NH) group. SCO-PEG3-NHS is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2).
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity[1].
Sumatriptan (GR 43175) hydrochloride is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan hydrochloride can be used for migraine headache research[1][2].
Vorsetuzumab mafodotin (SGN-75) is an Auristatin-based anti-CD70 antibody-drug conjugate (ADC). Vorsetuzumab mafodotin consists of a humanized monoclonal antibody, Vorsetuzumab and an ADC cytotoxin MMAF. Vorsetuzumab mafodotin has antineoplastic activity[1].
Hydroxyzine pamoate is a histamine H1-receptor antagonist.Target: Histamine H1-ReceptorHydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and severity of EAE by 50% and the extent of mast cell degranulation by 70% in Lewis rats with allergic encephalomyelitis (EAE) [2]. Hydroxyzine (500 M) significantly increases transport of etoposide to the serosal site in the jejunal everted sacs. Hydroxyzine significantly reduces the efflux and approximately 2.4 ug/mL of etoposide in the jejunum and ileum. Hydroxyzine (0.2 μg/mL) significantly enhances the efflux of RH123 to the lumen [3].Hydroxyzine (500 μM) significantly decreases the steady-state etoposide concentration 2-fold, where the steady-state concentration reached about 0.055 μM/mL in Sprague-Dawley rats [3]. Hydroxyzine (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats [4].
Fmoc-Ile-Ser(psi(Me,Me)pro)-OH is a dipeptide.
Nicotredole (Tryptamide) is an orally active anti-inflammatory and analgesic agent. Nicotredole exhibits evident antiinflammatory effects of potency comparable with Phenylbutazone. Nicotredole has only weak ulcerogenic activity[1][2][3].
Tetramethylkaempferol is an antifungal agent. Tetramethylkaempferol shows antifungal activity against Candida albicansCandida albicans with an IC50 value of 17.63 µg/mL[1].
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM[1].
Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with Kd of 0.6-1.1 μM in the presence of CO.
Monomethyl auristatin E intermediate-11 is an intermediate reactant in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs)[1].
U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.IC50 value: 45.1 nM/4.5 nM(Ki, CA IX/CA XII) [1]Target: Carbonic anhydrase inhibitorin vitro: U-104 (50 μM) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 μM) significantly reduces migration in a dose-dependent manner in metastatic MDA-MB-231 LM2-4Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells [2]. in vivo: U-104 (38 mg/kg) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg) inhibits metastases formation in the 4T1 experimental metastasis mice model [1]. U-104 (38 mg/kg) significantly delay primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. U-104 (5 mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells [2].
TBI-166, a riminophenazine analogue, is an orally active anti-tuberculosis agent with fewer adverse reactions than the lead riminophenazine compound, Clofazimine (HY-B1046) [1][2][3].
KP1019 (FFC14A) is a Ru(III)-based anti-metastatic and cytotoxic anti-cancer agent. KP1019 induces DNA damage and apoptosis in cancer cells[1][2].
Amoxicillin Sodium is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.Target: AntibacterialAmoxicillin is a moderate-spectrum, bacteriolytic, β-lactam antibiotic in the aminopenicillin family used to treat bacterial infections caused by susceptible Gram-positive and Gram-negative microorganisms. It is usually the drug of choice within the class because it is better-absorbed, following oral administration, than other β-lactam antibiotics. Amoxicillin is susceptible to degradation by β-lactamase-producing bacteria, which are resistant to a narrow spectrum of β-lactam antibiotics, such as penicillin. For this reason, it is often combined with clavulanic acid, a β-lactamase inhibitor. This increases effectiveness by reducing its susceptibility to β-lactamase resistance. From Wikipedia.
Robustine, a furoquinoline alkaloid, from Dictamnus albus, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro[1].
Vanutide cridificar (ACC-001) is an aminoterminal Aβ1-7 peptide conjugate. Vanutide cridificar can be used for Alzheimer's disease (AD) research[1].
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a drug-linker conjugate for ADC with potent antitumor activity by using Monomethyl Dolastatin 10 (a potent tubulin inhibitor), linked via the ADC linker Vat-Cit-PAB.
MGL-3196 is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM.
Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC50 values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.
Bilanafos is a natural organic phosphine tripeptide antibiotic metabolized by Streptomyces hydroscopius or Streptomyces viridochromeogenes. Bialaphos has antimicrobial activity aganist Gram-negative and positive bacteria as well as some fungal plant diseases[1].