Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research[1][2][3][4].
Ethyl cellulose is a derivative of cellulose. Ethyl cellulose serves as a non-toxic and biodegradable polymer, with unique properties such as oleogel formation, delivery of active component, and film-forming ability in the food and pharmaceutical sectors. Ethyl cellulose can be used as an excipient, such as coating agent, flavoring agent, tablet filler. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs[1][2].
GS 4104, the ethyl ester prodrug of GS 4071, is an inhibitor of influenza virus neuraminidase with an IC50 of approximately 100 nM.
Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
8-Deazafolic acid is an antimicrobial drug for the folate-dependent bacteria, Streptococcus faecium (ATCC 8043) and Lactobacillus casei (ATCC 74691). 8-Deazafolic acid has activity against lymphoid leukemia L1210 in mice[1].
Antibacterial agent 39, an antibacterial agent, significantly lowers MIC value of antibacterial agent Ceftazidime[1].
Tenovin-1 is an inhibitor of sirtuin 1 and sirtuin 2, an activator of p53 and may have potential in the management of cancer.
(S)-2-((R)-2-Amino-4-methylpentanamido)-3-(4-hydroxyphenyl)propanoic acid hydrate is a tyrosine derivative[1].
Cabozantinib-d6 (XL184-d6) is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Clionamine B is an autophagy stimulating aminosteroid isolated from the sponge Cliona celata. Clionamine B strongly stimulates autophagy in human breast cancer MCF-7 cells[1].
Biotinyl-neuropeptide W-23 (human) is a biotinylated neuropeptide W-23 (human) (HY-P1035). Neuropeptide W-23 (human) is an agonist of NPBW1 (GPR7) and NPBW2 (GPR8)[1][2].
5-Acetylsalicylic acid has anti-inflammatory and is considered to be the active agent in inflammatory bowel disease (IBD)[1].
Senkyunolide C is a natural product, that can be isolated from the rhizome of Cnidium officinale[1].
Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.
Ganorbiformin B is a lanostane triterpenoid. Ganorbiformin B shares the same lanostane skeleton with known ganoderic acids. The C-3 epimer of ganoderic acid T exhibits potent antimycobacterial activity against Mycobacterium tuberculosis H37Ra[1].
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe[1].
Mal-PEG4-Val-Cit-PAB-PNP is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease[1].
Stiripentol-d9 (BCX2600-d9) is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
Isoagarotetrol is a natural product isolated from agalwood[1].
Exoticin is a natural product that can be isolated from the leaves of Nicotiana plumbaginifolia[1].
Phentolamine mesylate is a competitive, reversible α-adrenoceptor antagonist with an IC50 between 5 and 30 nM.
2-Aminoadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities[1]. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway[2].
PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.IC50 value: 8.2 nM [1]Target: Btk kinasePCI 29732(compound 1) has a 8.2 nM potency against Btk in a FRET based biochemical enzymology assay. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase, probably due to the difference at the “gatekeeper” residue [1].In human CD20+ B cells stimulated at the BCR, PCI-29732 blocked the transcriptional up-regulation of a panel of B-cell activation genes that occurs within 6 h of stimulation. Pulse exposure to the reversible inhibitor PCI-29732 did not result in BCR inhibition [2].
Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist. Target: NMDARapastinel is a robust cognitive enhancer and facilitates hippocampal long-term potentiation (LTP) of synaptic transmission in slices.
Histone H3 (116-136), C116-136 is a peptide spaning the C-terminus of histone H3, amino acids 116 to 136[1].
Narlaprevir is a potent, selective, orally bioavailable NS3 protease inhibitor(Ki=6 nM; EC90=40 nM)IC50 Value: 6 nM (Ki)Target: HCV NS3/4A Protease; HCVNarlaprevir (SCH 900518) is a potent inhibitor of the hepatitis C virus (HCV) nonstructural protein 3 serine protease that is primarily metabolized by the cytochrome P450-3A4 system. Narlaprevir administration resulted in a robust HCV-RNA decline and high SVR rates when followed by standard of care in both treatment-experienced and treatment-naive HCV genotype 1-infected patients.
IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor, extracted from patent WO2014150677A1, Compound example 1 enantiomer 1.
Triptonoterpene is a natural product that can be isolated from the roots of Tripterygium wilfordii Hook. f.[1].