Cancer Targeted Therapy

TNF-α-IN-1 (Compound I-7) is a TNF-α inhibitor. TNF-α-IN-1 can be studied in research for cancers, heart disease, autoimmune disease and infections.

PROTAC AURKA degrader 3 is a selective AURKA PROTAC degrader, with DC₅₀ values of 2.05, 157.85 and 43.05 nM against AURKA, AURKB and TTK, respectively. PROTAC AURKA degrader 3 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC AURKA degrader 3 can be used for research related to acute myeloid leukemia.

L-779450 is a potent and selective B-Raf kinase inhibitor with a K_d of 2.4 nM.

JQ-1-Azidopropylamine is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker (HY-151862), which recruits E3 ligases. JQ-1-Azidopropylamine can be used for synthesis of PROTAC JY-21 (HY-174975).

Azido-PEG3-C6-Cl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG3-C6-Cl 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.

SP11 is a mitochondrial fission protein 1 (Fis1) inhibitor with an IC₅₀ of 9.4 μM. SP11 binds only to activated Fis1 by engaging Cys41. SP11 preserves mitochondrial integrity and function during oxidative stress, inhibits hydrogen peroxide-induced mitochondrial ROS production, mitochondrial fragmentation, and Drp1 mitochondrial translocation. SP11 can be used for the research of parkinson’s disease.

Vonsetamig (REGN5459) is a human bispecific antibody targeting BCMA and CD3. Vonsetamig triggers T-cell activation, induces plasma cell depletion, and triggers low-level cytokine release. Vonsetamig can be used for the research of relapsed/refractory multiple myeloma.

hsa-miR-200c-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.

M3541 is an orally effective DNA-dependent protein kinase (DNA-PK) inhibitor. M3541 inhibits ionizing radiation-induced ATM autophosphorylation and phosphorylation of downstream substrates (KAP1, CHK2, p53), blocks DSB end resection and homologous recombination repair, and simultaneously induces non-homologous end joining, G2-M phase arrest, polyploidization, and cell death. M3541 can be used for research on solid tumors, acute myeloid leukemia, non-small cell lung cancer, triple-negative breast cancer, etc..

CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells.

MG-HuR2 is a molecular glue degrader targeting HuR (ELAVL1) with a K_d of 0.2018 μM. MG-HuR2 recruits the E3 ubiquitin ligase RNF126 and induces proteasome-dependent degradation of HuR. MG-HuR2 exhibits a unique biphasic degradation profile. MG-HuR2 reduces the expression of HuR and its downstream targets Bcl2/FOXQ1, inhibits breast cancer cell proliferation, enhances cytotoxicity and apoptosis (apoptosis), and suppresses the growth of 3D breast cancer tumor spheres. MG-HuR2 can be used in studies related to breast cancer and HuR-targeted protein degradation.

Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.

NH2-PEG1-CH2CH2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs.

NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with K_is of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.

L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments.

PDS-0330 is a specific and potent Claudin-1 inhibitor. PDS-0330 interferes with claudin-1/Src association and inhibits colorectal cancer (CRC) progression and metastasis.

Necrostatin-1 (Nec-1) (inactive control) is an inactive analog of Necrostatin-1 (HY-15760). Necrostatin-1 is a potent necroptosis inhibitor.

Tigecycline tetramesylate (GAR-936 tetramesylate) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC₅₀ and MIC₉₀ are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.

FKB04 is a telomeric repeat binding factor 2 (TRF2) inhibitor that exerts its antitumor activity by disrupting the telomere maintenance mechanism in liver cancer cells, leading to T-loop defects, telomere shortening, and cellular senescence. Additionally, FKB04 can inhibit tumor growth in a human liver cancer xenograft mouse model (with Huh-7 cells implanted in BALB/c mice). FKB04 can be used in liver cancer research.

7-Aminoheptanoic acid is a PROTAC linker. 7-Aminoheptanoic acid can be used to synthesize PROTAC molecules (e.g. HL-8 (HY-143275)).