Cancer Targeted Therapy

NH-bis(PEG3-azide) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. NH-bis(PEG3-azide) 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.

VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC₅₀ values of 0.2-1 nM.

Silydianin is a flavonolignan. Silydianin can be obtained from Silybum marianum. Silydianin inhibits PTP1B with an IC₅₀ of 17.38 μM. Silydianin inhibits both monophenolase and diphenolase of tyrosinase significantly, with IC₅₀s of 2.6 μM and 16.5 μM, respectively. Silydianin induces Apoptosis and reduces cytokines (IL-4 and IL-5). Silymarin has antioxidant, cytoprotective and immunomodulatory effects. Silydianin has antitumor activity against prostate cancer. Silymarin can be used in allergic asthma research.

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC₅₀ of 2.4 μM.

Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.

Vizenpistat (SR-8541A) is an orally active ENPP1 inhibitor. Vizenpistat increases cGAMP levels, blocks 2′3′-cGAMP hydrolysis, inhibits adenosine production, regulates innate immune signaling mediated by the STING pathway, and modulates anti-tumor immune responses. Vizenpistat is applicable to research related to breast cancer and metastatic microsatellite-stable colorectal cancer.

Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (K_d:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC₅₀ of 2.26 μM. Naphthol AS-E can be used for cancer research.

PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.

WWQ-03-012 is a selective DESI2 inhibitor with an IC₅₀ of 47.3 nM. WWQ-03-012 binds covalently to DESI2, blocks its enzymatic activity, and inhibits DESI2-mediated deSUMOylation, deubiquitination and stabilization of mutant JAK2, thereby promoting the complete degradation of mutant JAK2 via the intracellular ubiquitin-proteasome system and inducing apoptosis, while exerting no significant effect on wild-type JAK2. WWQ-03-012 can be used for research on myeloproliferative neoplasms (MPN) and secondary acute myeloid leukemia (sAML), especially for hematological malignancies carrying the JAK2-V617F mutation and those resistant to Ruxolitinib (HY-50856).

PROTAC EGFR degrader 8 (T-184) is a PROTAC degrader that targets EGFR for degradation by recruiting cereblon. It induces EGFR protein degradation with a DC₅₀ of 10.18 nM. The IC₅₀ values of PROTAC EGFR degrader 8 for inhibiting the growth of H1975, PC-9 and HCC827 cells are 7.72, 121.9 and 14.21 nM, respectively. PROTAC EGFR degrader 8 inhibits the proliferation of EGFR-mutant non-small cell lung cancer cells and can be used in studies related to non-small cell lung cancer.

Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase (belongs to the ALDH family) and protoporphyrinogen oxidase inhibitor.

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

iMAC2 hydrochloride is a potent MAC (mitochondrial apoptosis-induced channel) inhibitor, with an IC₅₀ of 28 nM and a LD₅₀ of 15000 nM. iMAC2 hydrochloride shows anti-apoptotic effect. iMAC2 hydrochloride blocks cytochrome c release.

G280-9 is a 9 amino acid native epitope peptide. G280-9 is a relevant target expressed on melanoma.

Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.

Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to monkey/human MHC class II. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can inhibits tumor cells proliferation and induce apoptosis. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) increases cellular reactive oxygen species (ROS) and loss of mitochondrial membrane potential in human endothelial cells. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can be used for the researches of cancer and infection, such as lymphoma.

XZ338 is a highly potent and selective BCL-XL PROTAC degrader derived from A-1331852 (HY-19741), with a DC₅₀ of 0.43 nM in MOLT‑4 cells. XZ338 induces the formation of a ternary complex with BCL-XL and VHL E3 ligase, mediates target protein degradation via the ubiquitin-proteasome system, and exhibits significantly weaker degradation activity in platelets than in tumor cells. XZ338 possesses anti-cancer activity. XZ338 can be used in the research of T-cell acute lymphoblastic leukemia (T-ALL).

Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation.

HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC₅₀ values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC₅₀ of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.

Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers.