Cancer Targeted Therapy

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

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.

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.

Bosutinib isomer is a ligand or inhibitor with high binding affinity for both Wee1 and Wee2, with K_d values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively.

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.

LY3177833 (Example 4) is an orally active CDC7 and pMCM2 inhibitor with IC₅₀ values of 3.3 nM and 290 nM, respectively. LY3177833 is a senescence inducer.

7-Hydroxychromone is a Src kinase inhibitor with an IC₅₀ of <300 μM.

5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a K_i of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia.

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.

(-)-Syringaresinol is an orally active isomer of syringaresinol (HY-N8307) found in Annona Montana. (-)-Syringaresinol exhibits antioxidant, anti-inflammatory, and anticancer activities. (-)-Syringaresinol can alleviate ulcerative colitis via the PI3K-Akt/MAPK/Wnt signaling pathway. (-)-Syringaresinol inhibits HL-60 cell proliferation by arresting the G1 phase and inducing apoptosis. (-)-Syringaresinol inhibits LPS (HY-D1056)-induced microglial activation by downregulating the NF-κB p65 signaling pathway and its interaction with ERβ, exerting anti-neuroinflammatory effects.

Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC₅₀=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence.

3-(2-Pyridyldithio)propanoic Acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

TMX-2039 is a pan-CDK inhibitor for both cell cycle CDKs (CDK1, CDK2, CDK4, CDK5 and CDK6) and transcriptional CDKs (CDK7 and CDK9), with IC₅₀s of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5 and 25 nM, respectively. TMX-2039 acts as a Ligands for Target Protein for PROTACs.

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC₅₀ values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.

Azido-PEG6-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-alcohol is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG6-alcohol 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.

c-Myc inhibitor 6 (compound A102) is a c-Myc inhibitor. c-Myc inhibitor 6 decreases cancer cell viability and degrades c-Myc protein. c-Myc inhibitor 6 can be used for the research of c-Myc imbalance, such as cancer, cardiovascular diseases, and viral infection.

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.

MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a K_d of 4.1 μM. MB710 shows anticancer activity in p53-Y220C cell lines.

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.

Fmoc-Asp-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).