Cancer Targeted Therapy

PERK-IN-3 is a potent PERK inhibitor with an IC₅₀ of 7.4 nM.

Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC₅₀ of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC₅₀s of 221 nM and 916.3 nM, respectively.

Azido-PEG3-S-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG3-S-PEG4-t-butyl ester 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.

DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6).

PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 ( IC₅₀ ≤10nM). PARP7-IN-19 can be used in the research area of tumors.

CRM1-IN-3 (B28) is a noncovalent CRM1 inhibitor. CRM1-IN-3 can be used for the research of protein localization and tumor.

STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells.

hsa-miR-210-3p 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-4445-5p 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.

hsa-miR-548az-5p 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.

ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC₅₀s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC₅₀s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner.

N6-Methyl-3’-O-(2-methoxyethyl) adenosine 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.

PROTAC BRD4 Degrader-22 is a BRD4 PROTAC degrader with a DC₅₀ of 0.59 nM. At high concentrations, PROTAC BRD4 Degrader-22 induces partial degradation of BRD3 and BRD2, but exhibits selectivity for IKZF3. PROTAC BRD4 Degrader-22 can be used in leukemia-related research.

FGFR4-IN-22 (compound 10f) is a potent inhibitor of FGFR4, with the IC₅₀ of 5.4 nM. FGFR4-IN-22 serve as a potential lead compound targeting FGFR4 for anti-HCC agent development.

Lck degrader-1 is a molecular glue degrader that recruits cereblon to target LCK and CK1α. Lck degrader-1 promotes the formation of the LCK/CRBN-DDB1 ternary complex with an EC₅₀ of 77.1 nM, and induces the degradation of LCK and CK1α. LCK degradation induced by Lck degrader-1 depends on the G415-containing helical G-loop degron, and maintains LCK-degrading activity in cells with the LCK T316I gatekeeper mutation. Lck degrader-1 can be used for research related to T-cell acute lymphoblastic leukemia (T-ALL) and LCK inhibitor resistance.

Keap1-Nrf2-IN-29 (Compound 1a), a Curcumin (HY-N0005) analog, is a Keap1 protein inhibitor. Keap1-Nrf2-IN-29 exhibits significant inhibitory activity against A549, PC-3 and MCF-7 cells. Keap1-Nrf2-IN-29 can be used for the study of prostate cancer.

W-GTF01 is a MGAT1 inhibitor. W-GTF01 blocks the MGAT1-catalyzed glycosylation of CD73, and inhibits CD73 dimerization, membrane translocation and adenosine production. W-GTF01 restores the function of IFNγ-producing CD8⁺ T cells, enhances tumor infiltration and activation of CD8⁺ T cells, and suppresses tumor growth. W-GTF01 can be used in research related to triple-negative breast cancer.

7-Coumaryl triflate is a type 17β-HSD1 inhibitor of 17β-hydroxysteroid dehydrogenase. Its IC₅₀ is 360 nM and K_i is 173 nM. 7-Coumaryl triflate shows selectivity for 17β-HSD2 and has no detectable affinity for ERα or ERβ. 7-Coumaryl triflate can be used in related research on hormone-dependent breast cancer.

hsa-miR-8067 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.

mmu-miR-351-5p 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.