5’-O-DMTr-2’,2’-difluoro-dC(Bz)-3’-CED-phosphoramidite 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].
XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
2′,3′-Didehydro-2′,3′-dideoxy-5-fluorouridine 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].
2’,3’,5’-Tri-O-acetyl-5-(trifluoromethyl)uridine is a thymidine analog. Analogs of this series have insertional activity towards replicated DNA. They can be used to label cells and track DNA synthesis[1].
Pravastatin sodium is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.Target: HMG-CoA reductasePravastatin (marketed as Pravachol or Selektine) is a member of the drug class of statins, used in combination with diet, exercise, and weight-loss for lowering cholesterol and preventing cardiovascular disease.Pravastatin is primarily used for the treatment of dyslipidemia and the prevention of cardiovascular disease. It is recommended to be used only after other measures such as diet, exercise, and weight reduction have not improved cholesterol levels.The evidence for the use of pravastatin is generally weaker than for other statins. The antihypertensive and lipid-lowering treatment to prevent heart attack trial (ALLHAT), failed to demonstrate a difference in all-cause mortality or nonfatal myocardial infarction/fatal coronary heart disease rates between patients receiving pravastatin 40mg daily (a common starting dose) and those receiving usual care.
IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts[1][2].
3'-Amino-3'-deoxyadenosine is an antitumor agent extracted from Helminthosporium[1].
ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
ATR-IN-17 (compound 88) is a potent ATR kinase inhibitor. ATR-IN-17 shows good anticancer activity in LoVo cells, with an IC50 of 1 nM[1].
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
NF-κB/PON1-IN-1 (Compound 16) is a NF-κB/PON1 pathway inhibitor. NF-κB/PON1-IN-1 has antioxidant (IC50 = 45.76 µM) and hepatoprotective activities[1].
Pyroxamide is a potent inhibitor of histone deacetylase 1 (HDAC1) with an ID50 of 100 nM. Pyroxamide can induce apoptosis and cell cycle arrest in leukemia.
Allitinib tosylate (AST-1306 TsOH) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.IC50 value: 0.5/3 nM (EGFR/Erb2)[1]Target: EGFR/Erb2;Mutant EGFR T790M/L858RAllitinib functions as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, respectively. Further studies showed that Allitinib inactivated pathways downstream of these receptors and thereby inhibited the proliferation of a panel of cancer cell lines. Allitinib is a potent(pM) and selective inhibitor of EGFR and ErbB4 (IC50 = 500pM and 800 pM, respectively). AST-1306 blocks phosphorylation of EGFR and also prevents downstream pathways. Allitinib also dose-dependently inhibits EGF-induced EGFR phosphorylation in the A549 cancer cell line.
Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively[1][2].
Antioxidant agent-4 (Compound 2) is an effective antioxidant molecule with antilipid peroxidative activity[1].
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase[1].
2’-Deoxy-2’-fluoro-alpha-D-arabinoguanosine 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].
3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative with antitumor activity.
DGKα&ζ-IN-1 (Compound II) is a DGK target inhibitor. DGKα&ζ-IN-1 can enhance the function of T cells, and has a synergistic effect with PD-1, which has therapeutic effects IN both immune and tumor[1].
5-HT2 agonist-1 (Compound 24) free base is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders[1].
KX2-391 is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
PRT4165 is a potent inhibitor of PRC1-mediated H2A ubiquitylation.
Membrane-Permeable Sequence, MPS is a cell-penetrating peptide (CPP). Membrane-Permeable Sequence, MPS can be used for the research of membrane crossing mechanism[1].
Cabozantinib-d4 is 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.
Glaucocalyxin B is an ent kaurane diterpenoid isolated from the Chinese traditional medicine Rabdosia japonica with anticancer and antitumor activity; decreases the growth of HL-60 cells with an IC50 of approximately 5.86 μM at 24 h.
CEP-32496 is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM.
E3 Ligase Ligand-Linker Conjugates 2 incorporates a ligand for the E3 ubiquitin ligase, and a PROTAC linker, which bring together target protein and ubiquitinating machinery.
Urocanic acid-13C3 is the 13C labeled Urocanic acid[1]. Urocanic acid, produced in the upper layers of mammalian skin, is a major absorber of ultraviolet radiation (UVR)[2].