Cancer Targeted Therapy

Pazelliptine (Pazellipticine) is a DNA topoisomerase inhibitor and antitumour agent.

IDO-IN-16 (compound 5) is an IDO inhibitor, with an IC₅₀ of 36 nM.

Glyoxalase I inhibitor 2 (compound 26) is a potent glyoxalase I (GLO1) inhibitor with an IC₅₀ of 0.5 µM. Glyoxalase I inhibitor 2 has the potential for the research of depression and anxiety.

EGFR-IN-147 (compound ID-5841161) is a potent inhibitor of EGFR, with the inhibition rate of 14% at 1 μM. EGFR-IN-147 has the potential for the research of cancer.

Thalidomide (methylamino)acetaldehyde is an E3 ubiquitinase ligand-linker conjugate. Thalidomide (methylamino)acetaldehyde can be used to synthesize WZH-17-002 (HY-174315).

VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC₅₀ values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC₅₀: 3.403 µM).

Tetrahydrouridine-d₃ is the deuterium labeled Tetrahydrouridine. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.

Thalidomide-NH-C14-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-NH-C14-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).

Iodoacetyl-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Bromo-C4-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC₅₀s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC₅₀ values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3.

EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC₅₀s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research.

hsa-miR-3140-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

hsa-miR-6877-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3.

2-Methyl-2’-deoxyadenosine 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.

Deltaflexin3 is a potent PDE6D inhibitor. Deltaflexin3 reduces the signaling of Ras and selectively decreases the KRAS mutant and PDE6D-dependent cancer cells growth.

CHNQD-01522 is a microtubule inhibitor targeting the colchicine binding site on β-tubulin. CHNQD-01522 binds to the colchicine binding site on β-tubulin, inhibits microtubule polymerization, and evades P-glycoprotein transport in cancer cells. CHNQD-01522 inhibits proliferation, suppresses tumor cell colony formation, arrests cell cycle in G2/M phases, and induces apoptosis in cancer cells. CHNQD-01522 upregulates of Bax and activation of caspase-9 and caspase-3. CHNQD-01522 shows anti-tumor efficacy in subcutaneous and orthotopic hepatocellular carcinoma xenograft tumor models. CHNQD-01522 can be used for the research of hepatocellular carcinoma.

UMI-77-d₄ is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.

AM-8735 is a potent and selective MDM2 inhibitor with an IC₅₀ of 25 nM.