Deoxyharringtonine is an alkaloid isolated from Cephalotaxus genus with significant anti-leukemic activity[1].
HEX3 is a fragment of the adenoviral hexon. Hexon is the major capsid protein of adenovirion and is comprised of three identical polypeptide chains.
Neuronotoxicity-IN-1, a pyridothiazine derivative, is a kainic acid neurotoxicity inhibitor. Neuronotoxicity-IN-1 is a neuroprotective agent[1].
Flavokawain 1i (DiNap) is an Hsp90 inhibitor. Flavokawain 1i (DiNap) has anti-cell proliferation activity and can be used in cancer research[1].
AXC-715 trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1[1]. AXC-715 trihydrochloride, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants[2].
Riligustilide (compound 2) is a kind of phthalide dimer. Riligustilide can be isolated from the radix of Angelica sinensis[1].
(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180)[1].
5'-O-TBDMS-dU can be used in the synthesis of oligoribonucleotides[1].
5-HT3-In-1 is extracted from patent EP0748807A1, compound example 8. It shows 5-HT3 inhibition activity.
6-Methoxy-2-(2-phenylethyl)chromone (compound 9) is a 2-(2-phenylethyl)chromone (¼2-(2-phenylethyl)-4H-1-benzopyran-4- one) derivative[1].
2,3-Pentanedione is a common constituent of synthetic flavorings and is used to impart a butter, strawberry, caramel, fruit, rum, or cheese flavor in beverages, ice cream, candy, baked goods, gelatins, and puddings. 2,3-Pentanedione also occurs naturally as a fermentation product in beer, wine, and yogurt and is releasedduring roasting of coffee beans[1].
PF-4618433 is a potent and selective PYK2 inhibitor, with an IC50 of 637 nM. PF-4618433 may be suitable for the research of osteoporosis, craniofacial and appendicular skeletal defects and for targeted bone regeneration[1][2].
R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1[1].
Flumatinib is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit) [1]Target: c-Abl; c-Kit; PDGRFβin vitro: HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, HH-GV-678 can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, HH-GV-678 has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2 [1]. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) [2].in vivo: The purpose of this study was to identify the metabolites of flumatinib in CML patients, with the aim of determining the main metabolic pathways off lumatinib in humans after oral administration. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry revealed 34 metabolites; 7 primary metabolites were confirmed by comparison with synthetic reference standards. The results show that the parent drugflumatinib was the main form recovered in human plasma, urine, and feces. The main metabolites of flumatinib in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis [3].
VD3-D6(Vitamin D3-26,26,26,27,27,27-d6) is the deuterated form of Vitamin D3; tools for determination of Vitamin D3 metabolites in human serum.
Anti-neurodegeneration agent 1 a neurodegeneration-targeting compound extracted from patent WO2008039514A1, Compound I.
Sulfametrole is an orally active and potent antibacterial. Sulfametrole can be used for infections research, such as HIV, severe pneumonia and UTIs (urinary tract infections)[1][2].
6-O-2-Propyn-1-yl-D-galactose is a glycolinker for the functionalization of cytotoxic drugs and applications in antibody-drug conjugation.
Heliomicin is an antimicrobial peptide from Heliothis Virescens[1].
2’-Deoxy-2’-fluoro-5-methyl-4’-thio-β-D-arabino uridine 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].
Fibrinogen Binding Inhibitor Peptide is a dodecapeptide (HHLGGAKQAGDV, H12), which is a fibrinogen γ-chain carboxy-terminal sequence (γ400-411). Fibrinogen Binding Inhibitor Peptide is a specific binding site of the ligand for activated glycoprotein (GP) IIb/IIIa.
Lonafarnib is an orally bioavailable farnesyl protein transferase (FPTase) inhibitor for H-ras, K-ras and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
Fmoc-NMe-PEG4-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
RO5028442 is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
(S)-2-(tert-Butoxycarbonylamino)succinic acid benzyl ester is an aspartic acid derivative[1].
Melredableukin alfa (RO-7049665) is a fusion protein that consists of a human IgG1-κ fused to a mutated human interleukin 2 (IL2 mutein) via a peptide linker. Melredableukin alfa can be used for the research of autoimmune hepatitis and ulcerative colitis[1].
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1].
Quinidine hydrochloride monohydrate is a clinical anti-arrythmic drug which is also a potent blocker of K+ channel with an IC50 of 19.9 μM.
Boc-PEG4-C2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Derazantinib (ARQ-087) dihydrochloride is an ATP competitive and orally activeFGFR inhibitor (IC50s: 1.8 nM for FGFR2, 4.5 nM for FGFR1 and 3). Derazantinib dihydrochloride inhibits FGFR phosphorylation. Derazantinib dihydrochloride inhibits tumor growth in multiple xenograft models[1][2].