EZH2-IN-9 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-9 has the potential for the research of cancer diseases (extracted from patent WO2021180235A1, compound 17)[1].
PROTAC_ERRα is a potent and selective ERRα degrader. PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%[1].
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent PARP1 inhibitor with an IC50 value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) [1].
AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal.
Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway[1]. Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein[2].
hCAIX-IN-13 (Pt2) is an inhibitor of CAIX (arbonic anhydrase IX) with an IC50 value of 6.57 μM. hCAIX-IN-13 inhibits growth of cancer cells and induces cell apoptosis, it can be used for the research of cancer[1].
TJ191 is a selective anti-cancer small molecule that targets low TβRIII-expressing malignant T-cell leukemia/lymphoma cells (MOLT-3 IC50=0.26 uM); selectively targets certain cancer cells without affecting the proliferation of other cancer cells or normal fibroblasts or immune cells (over 600-fold selectivity), TβRIII acts as a predictive marker for TJ191 sensitivity in malignant T-cells.
Nocodazole is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells.
PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity[1].
KRAS G12C inhibitor 40 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 40 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 70)[1].
Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
YB-0158 (Wnt pathway inhibitor 2) is a reverse-turn peptidomimetic and a potent colorectal cancer stem cell (CSC) targeting agent. YB-0158 disrupts Sam68-Src interactions and induces apoptosis in CRC cells. Anti-cancer activities[1].
(-)-Haplomyrfolin is a natural lignan with anticancer effects[1].
Tiazofurin is a synthetic nucleoside analogue with antineoplastic activity. Tiazofurin is anabolized intracellularly to tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH).
ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader. ARD-69 induces degradation of androgen receptor (AR) protein in AR-positive prostate cancer cell lines. ARD-69 suppresses AR-regulated gene expression[1].
CLK inhibitor T3 (T3) is a highly potent, selective, and cell-based stable CDC-like kinase (CLK) inhibitor with 0.67, 15 and 110 nM for CLK1,2 and 3, respectively; displays 200-300-fold selectivity over other dual specificity kinases such as DYRK1A and DYRK1B; induces dose-dependent reduction in exon recognition and exhibits an overlapping, but greater effect on transcriptome splicing compared to KH-CB19.
TLR7/8 agonist 4 hydroxy-PEG10-acid (compound 9) is a drug-linker conjugate for ADC with potent antitumor activity by using TLR7/8 agonist 4 (HY-139018; a TLR7/8 agonist), linked via the cleavable ADC linker hydroxy-PEG10-acid (HY-133307)[1].
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells[1]. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells[2].
Crocin II is isolated from the fruit of Gardenia jasminoides with antioxidant, anticancer, and antidepressant activity.Crocin II inhibits NO production with an IC50 value of 31.1 μM.Crocin II suppresses the expressions of protein and m-RNA of iNOS and COX-2[1].
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
N1-Acetylspermine is an endogenous metabolite present in Urine that can be used for the research of Leukemia[1][2].
dCeMM1 is a RBM39 glue degrader. dCeMM1 shows functions by re-directing the activity of the CRL4DCAF15 ligase. dCeMM1 decreases the expression of RBM39 levels in WT KBM7 cells[1].
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research[1].
6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research[1].
Glycoside St-J (Compound 2) is a triterpenoid saponin. Glycoside St-J has antitumor activity and inhibits HeLa cell proliferation. Glycoside St-J Isolates from natural Anemone flaccida. Glycoside St-J can be used in the development of new anticancer agents [1].
2’-Deoxy-2’-fluoro-6-S-methyl-6-thio-arabino-inosine 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].
CT1113 is a potent USP28 and USP25 inhibitor. CT1113 decreases the MYC level in vivo，exhibits anti-tumor activity in mouse pancreatic cancer CDX model[1].
SMER28 is an autophagy activator acting via an mTOR-independent mechanism. SMER28 prevents the accumulation of amyloid beta peptide.
FGFR4-IN-16 (CY-15-2) is a covalent inhibitor of FGFR-4 for cancer research[1].
CRT0066101 dihydrochloride is a potent and specific PKD inhibitor with IC50 values of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.