Acolbifene (EM652) is a fourth-generation selective estrogen receptor antagonist with a LC50 value of 22±3 nM.
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.IC50 value: 20 nM (HER1); 30 nM (HER2) [1]Target: HER1/HER2in vitro: BMS-599626 inhibited HER1 and HER2 with IC50 of 20 and 30 nmol/L, respectively, and was highly selective when tested against a broad panel of diverse protein kinases. Biochemical studies suggested that BMS-599626 inhibited HER1 and HER2 through distinct mechanisms. BMS-599626 abrogated HER1 and HER2 signaling and inhibited the proliferation of tumor cell lines that are dependent on these receptors, with IC50 in the range of 0.24 to 1 micromol/L. BMS-599626 was highly selective for tumor cells that depend on HER1/HER2 and had no effect on the proliferation of cell lines that do not express these receptors. In tumor cells that are capable of forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization and downstream signaling [1]. At the molecular level, in HN-5 cells the agent inhibited the expression of pEGFR, pHER2, cyclins D and E, pRb, pAkt, pMAPK, pCDK1 and 2, CDK 6, and Ku70 proteins. The drug also induced accumulation of cells in the G1 cell cycle phase, inhibited cell growth, enhanced radiosensitivity, and prolonged the presence of γ-H AX foci up to 24 h after radiation [2].in vivo: BMS-599626 had antitumor activity in models that overexpress HER1 (GEO), as well as in models that have HER2 gene amplification (KPL4) or overexpression (Sal2), and there was good correlation between the inhibition of receptor signaling and antitumor activity [1]. The drug given before and during irradiation improved the radioresponse of HN5 tumors in vivo [2].
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities[1].
Ribociclib (LEE011) is a highly specific CDK4/6 inhibitor with IC50s of 10 nM and 39 nM, respectively.
Taplitumomab paptox is an anti-CD19 monoclonal antibody. Taplitumomab paptox can be used in cancer research.
PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM.
JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia[1].
Propargyl-PEG2-Ms is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
JAK-IN-35 (compound TG46) is a JAK2 inhibitor that canb be used in cancer research[1].
Bis-PEG2-NHS ester is a nonclaevable 2-unit PEG linker for antibody-drug-conjugation (ADC).
PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.
Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM[1].
Aristolone is a sesquiterpene isolated from Aristolochia debilis[1].
Hippuryl-L-phenylalanine is a substrate of carboxypeptidase. Carboxypeptidase is a protease enzyme that related with obesity, epilepsy and neurodegeneration. Hippuryl-L-phenylalanine can be used for the determination of carboxypeptidase activity[1][2].
HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers[1][2].
10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC50=1.28 μM)[1].
4-Di-1-ASP is a styryl dye used to stain glioma cells in living brain tissue for analysis of cell structure, viability, proliferation and endocytosis, cytokinesis and phagocytosis, as well as for observation of mitochondrial structures in living cells. 4-Di-1-ASP fluoresces green when imaged microscopically (λex /λem = 475/606 nm) [1][2].
ALDH1A3-IN-3 (compound 16) is a potent inhibitor of ALDH1A3, with an IC50 of 0.26 μM. ALDH1A3-IN-3 is also a good ALDH3A1 substrate. ALDH1A3-IN-3 can be used for the research of prostate cancer[1].
MDH1-IN-1 (Compound 5i) is a potent inhibitor of MDH1 with an IC50 of 6.79 μM. MDH1-IN-1 has the potential for the research of cancer diseases[1].
PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.IC50 value: 22 nMTarget: Src kinase inhibitorin vitro: PD173955 inhibits the growth of MDA-MB-468 and MCF-7 breast cancer cells with IC50s of 500 nM and 1 μM, respectively, with an accumulation of suspended cells. Cells treated with PD173955 show a near complete redistribution to the G2-M phase of the cell cycle in comparison with control cells, and quantitation of mitotic indices by immunofluorescence microscopy shows an accompanying accumulation of mitotic cells.PD173955 shows antimitotic activity in breast cancer cells with high or low src and yes kinase activities, the antimitotic activity of PD173955 is independent of cell type or malignant transformation [1]. PD173955 inhibits both the active and inactive forms of Abl. By contrast, Imatinib only inhibits the active form of the enzyme. In addition, the Ki for inhibition of Abl by PD173955 is very low, making it a more potent inhibitor of Abl and a more effective inhibitor of cancer cell proliferation than Imatinib [2]. PD173955, a Src family-specific tyrosine kinase inhibitor, increases the susceptibility of HT29 cells to anoikis in a dose- and time-dependent manner [3].
Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively[1].
IDO1/2-IN-1 (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 exhibits antitumor activies. Orally active[1].
Spiruchostatin A is a potent HDAC inhibitor with an IC50 value of 2 nM. Spiruchostatin A can induce apoptosis, has antitumor activity and may be used in leukemia studies[1][2].
WRN inhibitor 2 (example 118) is a WRN (Werner Syndrome ATP dependent helicase enzyme) inhibitor, with pIC50 ≥ 7.0[1].
SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
MMP-13-IN-1 is a potent and selective inhibitor of MMP-13 with a IC50 value of 16 nM. MMP-13-in-1 can be used for atherosclerosis research[1].
SMARCA-BD ligand 1 hydrochloride for Protac is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC[1].
GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM [1].
WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.