Mal-PEG2-NH2 (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH is an ADC Linker that can be used to synthesize Drug-Linker Conjugates for ADC. Especially for the synthesis of Deruxtecan (HY-13631E), a toxic drug-linker conjugate[1].
Amino-PEG4-C2-amine is a PEG-based (4 units) PROTAC linker can be used in the synthesis of PROTACs.
Dapagliflozin impurity A (Compound A) is a dapagliflozin peroxide, a genotoxic impurity, can cause damage to human genetic material at very low concentrations, leading to genetic mutations and possibly tumorigenesis[1].
Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization[1].
SWS1 is a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM) with anticancer activity. SWS1 can increase the number of tumor-infiltrating lymphocytes and exhibit anti-tumor efficacy in the B16-F10 mouse model (TGI=66.1%)[1].
Niraparib tosylate (MK-4827 tosylate) is an excellent PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.
KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3[1].
(S)-Donepezil is a S-enantiomer of Donepezil (HY-14566). Donepezil is a specific and potent AChE inhibitor[1][2].
PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.
A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM.
Se-Methylselenocysteine hydrochloride, a precursor of Methylselenol, has potent cancer chemopreventive activity and anti-oxidant activity. Se-Methylselenocysteine hydrochloride is orally bioavailable, and induces apoptosis[1][2].
Trifluridine-13C,15N2 is the 13C and 15N labeled Trifluridine[1]. Trifluridine (Trifluorothymidine;5-Trifluorothymidine;TFT) is an irreversible thymidylate synthase inhibitor, and thereby suppresses DNA synthesis. Trifluridine is an antiviral drug for herpes simplex virus (HSV) infection. Trifluorothymidine also has anti-orthopoxvirus activity[2].
PI3K-IN-27 is a potent inhibitor of PI3K. PI3K belongs to a large family of lipid signaling kinase that plays key role in cellular process including cell growth, differentiation, migration and apoptosis. PI3K-IN-27 has the potential for the research of hyper-proliferative diseases like cancer and inflammation, or immune and autoimmune diseases (extracted from patent WO2021233227A1, compound 1)[1].
SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs[1][2].
N-Boc-N-methyl-D-Valinol is an ADC linker with BOC protecting group.
Zolimomab aritox (H65-RTA) is an immunocoupling compound consisting of a ricin (RTA) chain, a ribosomal inhibitory protein, coupled to a monoclonal antibody (H65) against the pan-T-cell antigen CD5. Zolimomab aritox has anticancer activity and can be used in cutaneous T-cell lymphoma studies[1].
h-NTPDase8-IN-1 (compound 2d) is a sulfamoyl-benzamides based and selective inhibitor for h-NTPDases8 (IC50=0.28 μM). h-NTPDases8 is involved in a variety of physiological and pathological functions，such as thrombosis，diabetes，inflammation，and cancer[1].
FBnG-(Cys-acetamide)-CH2-PEG3-CH2-CH2-CH2-NH2 is a linker of AUTAC4. AUTAC4 contains an p-fluorobenzylguanine (FBnG) and a phenylindole moiety, which can induce K63-linked polyubiquitination and degradation of mitochondria in HeLa cells[1].
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells[1].
(1R)-IDH889 is the inactive isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
Matuzumab (EMD 72000) is a humanized anti-EGFR monoclonal antibody that blocks EGFR activation and downstream signaling, inhibits tumor growth[1].
PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
Lipoamido-PEG3-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Lipoamido-PEG3-OH (compound TA-TEG-G2CN) can be used in the formation of a highly stable, dendronized gold nanoparticle (AuNP)-based drug delivery platform[1].
GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
Diflomotecan (BN 80915) is a potent inhibitor of topoisomerase I. Diflomotecan causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds[1].
1,4,5,6-Tetrahydroxy-7-(3-methylbut-2-enyl)xanthone is a nature product that could be isolated from the stem barks of Garcinia xanthochymus. 1,4,5,6-Tetrahydroxy-7-(3-methylbut-2-enyl)xanthone has antiproliferative active. 1,4,5,6-Tetrahydroxy-7-(3-methylbut-2-enyl)xanthone can be used in research of cancer[1].
PRMT5-IN-29 is a potent and orally active PRMT5 Inhibitor with an IC50 of 1.5 μΜ. PRMT5-IN-29 has the potential for advanced cancers research[1].
Norbiotinamine is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction[1].
TNKS-2-IN-2 is a potent and selective inhibitor of TNKS2 with an IC50 of 22 nM[1].