Pentostatin is an irreversible inhibitor of adenosine deaminase with Ki of 2.5 pM.
Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
Anagrelide, an inhibitor of phosphodiesterase type III (PDEIII) (IC50=36 nM), inhibits platelet production. Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide plays in the antithrombopoietic action. The platelet-lowering agent[1].
MeOIstPyrd is an anti-skin cancer agent. MeOIstPyrd inhibits cell proliferation, migration, and spheroid formation by activating the mitochondrial intrinsic apoptotic pathway. MeOIstPyrd induces DNA damage. MeOIstPyrd activates p53, and increases the half-life of p53 and stabilizes p53 by phosphorylating it at ser15. MeOIstPyrd binds to MDM2 in the p53 sub-pocket and blocks p53-MDM2 interaction[1].
Uracil-d1 is the deuterium labeled Uracil[1]. Uracil is a common and naturally occurring pyrimidine derivative and one of the four nucleobases in the nucleic acid of RNA[2].
Thalidomide-NH-amido-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
DMOG (Dimethyloxallyl Glycine) is a cell-permeable and competitive inhibitor of HIF-1α prolyl hydroxylase (HIF-PH).
AR-42(HDAC-42) is a HDAC inhibitor with IC50 30 nM.IC50 Value: 30 nMTarget: HDACin vivo: HDAC42 is potent in suppressing the proliferation of U87MG and PC-3 cells, in part, because of its ability to down-regulate Akt signaling. AR-42 inhibits the growth of PC-3 and LNCaP cells with IC50 of 0.48 μM and 0.3 μM, respectively. Compared to SAHA, AR-42 exhibits distinctly superior apoptogenic potency, and causes markedly greater decreases in phospho-Akt, Bcl-xL, and survivin in PC-3 cells. AR-42 treatment induces growth inhibition, cell- cycle arrest, apoptosis, and activation of caspases-3/7 in malignant mast cell lines. AR-42 treatment induces down-regulation of Kit via inhibition of Kit transcription, disassociation between Kit and heat shock protein 90 (HSP90), and up-regulation of HSP70. AR-42 treatment down-regulates the expression of p-Akt, total Akt, phosphorylated STAT3/5 (pSTAT3/5), and total STAT3/5. in vitro: In the transgenic adenocarcinoma of the mouse prostate (TRAMP) model, administration of AR-42 not only decreases the severity of prostatic intraepithelial neoplasia (PIN) and completely prevents its progression to poorly differentiated carcinoma, but also shifts tumorigenesis to a more differentiated phenotype, suppressing absolute and relative urogenital tract weights by 86% and 85%, respectively. AR-42 significantly reduces leukocyte counts, and prolongs survival in three separate mouse models of B-cell malignancy without evidence of toxicity.
HI-TOPK-032 is a potent and specific TOPK inhibitor.
Hexadecanoate-13C16 potassium is the 13C-labeled Hexadecanoate sodium. Hexadecanoate-13C16 potassium can induce the expression of glucose-regulated protein 78 (GRP78) and CCAAT/enhancer binding protein homologous protein (CHOP) in in mouse granulosa cells[1][2].
5’-Deoxy-5’-N,N-diethylamino thymidine 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].
Cot inhibitor-1 is a COT/Tpl2 inhibitor.
AZD-8055 is a novel ATP-competitive inhibitor of mTOR kinase with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
SLF is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC50 of 0.22 μM for FKBP12. SLF can be used in the synthesis of PROTAC[1][2][3].
SIRT6-IN-2 (Compound 5) is a selective SIRT6 inhibitor (IC50: 34 μM). SIRT6-IN-2 increases acetylation of H3K9 and increases glucose uptake in cultured cells. SIRT6-IN-2 also reduces T cell proliferation. SIRT6-IN-2 has immunosuppressive and chemosensitizing effects[1].
Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.
Biotin-PEG6-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Isoviolanthin is a flavonoid glycoside extracted from the leaves of Dendrobium officinale. Isoviolanthin reduces the migratory and invasive capacities of TGF-β1-treated HCC cells but exhibits no cytotoxic effects on normal live cells, and has potential as a therapeutic agent for the treatment of advanced-stage metastatic HCC[1].
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
A potent, selective STAT3 inhibitor that blocks STAT3 binding to its phosphopeptide ligand (IC50=20 uM) and inhibits IL-6-mediated phosphorylation of STAT3; inhibits nuclear translocation of phosphorylated Stat3 with IC50 of 39 uM, induces apoptosis preferentially of breast cancer cell lines with constitutive Stat3 activation.
LXS196 is a potent and orally active protein kinase C (PKC) inhibitor under Phase I clinical trials for the treatment of uveal melanoma.
USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM[1].
IDO-IN-16 (compound 5) is an IDO inhibitor, with an IC50 of 36 nM[1].
Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
2'-Ethyl Simvastatin (compound 6) is a Mevinolin analog, with HMG-CoA reductase inhibition[1].
Pantoprazole-d6 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI)[1]. Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142)[3][4].
INI-43, a Kpnβ1 inhibitor, interferes with the nuclear localization of Kpnβ1 and known Kpnβ1 cargoes, NFAT, NFκB, AP-1 and NFY[1].
N4-Benzoyl-5-methyl-2’-O,4’-C-methylenecytidine is a cytidine analog. Cytidine analogs have a mechanism of inhibiting DNA methyltransferases (such as Zebularine, HY-13420), and have potential anti-metabolic and anti-tumor activities[1].