Cancer Targeted Therapy

Cbz-NH-PEG2-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo.

PROTAC PD-L1 degrader-2 is a PD-L1 PROTAC degrader with an IC₅₀ of 197.4 nM and a K_d of 301 nM. PROTAC PD-L1 degrader-2 induces PD-L1 endocytosis, drives degradation via the proteasomal and lysosomal pathways, and inhibits the PD-1/PD-L1 interaction. As an immune activator, PROTAC PD-L1 degrader-2 increases the levels of CD4⁺, CD8⁺, granzyme B and perforin. PROTAC PD-L1 degrader-2 can be used in studies related to colon cancer immunology.

PRMT5-IN-35 (Compound 87) is a potent, selective and orally active PRMT5 inhibitor with an IC₅₀ value of 1 nM. PRMT5-IN-35 can be used in cancer research.

SANT 2 is a potent Hh-signaling pathway antagonist. SANT 2 interferes with the expression of Gli1. SANT 2 causes developmental delay in medaka embryos. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers.

Bortezomib-d₈ is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).

hsa-miR-545-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

Butane-1,4-diyldiphosphonic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

PROTAC HER3-binding moiety 1 (compound 1b) is a Her3 Ligand for PROTAC.

(S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.

Nitrovin hydrochloride is an antibacterial growth promoter. Nitrovin hydrochloride induces ROS-mediated non-apoptotic and apoptotic-like cell death by targeting TrxR1. Nitrovin hydrochloride has anticancer activity, with IC₅₀ values of 1.31-6.60 μM for tumor and normal cells.

N3-PEG3-VC-PAB-MMAF (Comp T-88-5) is a drug-linker conjugate containing the ADC linker N3-PEG3-VC-PAB and the tubulin inhibitor MMAF. N3-PEG3-VC-PAB-MMAF is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HVH-2930 is a HSP90 C-terminal domain inhibitor with high oral bioavailability. HVH-2930 downregulates HSP90 client proteins, inhibits the HER2 signaling pathway, induces apoptosis, and suppresses the proliferation of breast cancer cells. HVH-2930 inhibits the proliferation of tumors sensitive or resistant to Trastuzumab (HY-P9907). HVH-2930 is applicable to relevant research on breast cancer.

m-PEG4-phosphonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

E16-uPA24 is a chimeric peptide targeting urokinase-type plasminogen activator receptor (uPAR). E16-uPA24 modifies senescent cells surface with polyglutamic acid, promoting immune cell-mediated responses through glutamate recognition. E16-uPA24 induces immune clearance of senescent cells and restores tissue homeostasis by enhancing immune cells recruitment and directly coupling senescent cells and immune cells. E16-uPA24 can be used for tissue degeneration, chronic inflammatory disease and age-related tumorigenesis research.

HDAC10-IN-3 (Compound 2a) is a potent HDAC10 inhibitor with an IC₅₀s of 0.41, 37, 350 and 4500 nM against HDAC10, HDAC6, HDAC8 and HDAC1. HDAC10-IN-3 exhibits moderate cytotoxicity in KB and SK-OV-3 cells, but does not show significant cytotoxicity against most cancer cell lines. HDAC10-IN-3 can be used for the study of cancers.

HDAC-IN-52 is a pyridine-containing HDAC inhibitor, with IC₅₀s of 0.189, 0.227, 0.440 and 0.446 μM for HDAC1, HDAC2, HDAC3, and HDAC10, respectively. HDAC-IN-52 can be used for the research of cancer.

Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC₅₀ of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma.

MSC2530818 (Standard) is the analytical standard of MSC2530818. This product is intended for research and analytical applications. MSC2530818 is a potent, selective and orally available CDK8 inhibitor with an IC₅₀ of 2.6 nM for CDK8.

PROTAC KRAS G12C (Compound 432) degrader-2 is a PROTAC degrader that targets KRAS^G12C by recruiting cereblon. PROTAC KRAS G12C degrader-2 covalently modifies KRAS^G12C. PROTAC KRAS G12C degrader-2 can be used for the research of non-small cell lung cancer.