Cancer Targeted Therapy

Myosin light chain kinase fragment 11-19 amide (MLCK(11-19) amide) is a substrate-specific peptide inhibitor of MLCK. Myosin light chain kinase fragment 11-19 amide inhibits hypotonicity-induced Ca²⁺ entry. Myosin light chain kinase fragment 11-19 amide can be used in the research of human cervical cancer.

hsa-miR-4468 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.

hsa-miR-548m 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.

eCF506-d₅ (NXP900-d₅) is deuterated labeled eCF506 (HY-112096). eCF506 is a highly potent and orally active YES1/SRC kinase inhibitor with an IC₅₀ of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer.

N-(3-Methylbutyl)adenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277).

mmu-miR-499-3p 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.

mmu-miR-7056-5p 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.

rno-miR-463-3p 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.

SBP-5147 is an orally active ULK1/ULK2 inhibitor, with an IC₅₀ of 2 nM against ULK1 and an IC₅₀ of 53 nM against ULK2. SBP-5147 inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagy flux, downregulates the expression of ATG13 and ATG101, upregulates the expression of MHC-I, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. SBP-5147 is applicable to research related to non-small cell lung cancer^[1].

mmu-miR-1943-3p 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.

mmu-miR-6373 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-7234-3p 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.

BRM/BRG1 ATP-IN-7 (Compound Cpd69) is a selective dual BRM (SMARCA2) and BRG1 (SMARCA4) inhibitor with IC₅₀ values of 12 nM and 8 nM, respectively. BRM/BRG1 ATP-IN-7 is promising for research of BRM/BRG1-dependent cancers (e.g., non-small cell lung cancer, Ewing sarcoma) and virus-associated diseases (e.g., HPV infection).

Aspergillusidone D (Compound 1), a brominated depsidone, is a Aromatase inhibitor with an IC₅₀ of 0.8  μM. Aspergillusidone D can be isolated from fungus Aspergillus unguis cultured in KBr medium. Aspergillusidone D has potent cytotoxicity against cancers cells, such as MOLT-3 cells. Aspergillusidone D can be used for cancers like breast cancer research.

Hydroxy-PEG24-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Biotin-PEG12-hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

SRE-II, an amide derivative, is an activatable photosensitizer for photodynamic cancer research with decreased fluorescence and photosensitizing capabilities. SRE-II can be further converted into the active photosensitizer SDU Red via carboxylesterase-catalyzed amide bond cleavage. SRE-II induces DNA damage and cell apoptosis in the presence of light. SRE-II can act as a promising theranostic agent for triple-negative breast cancer.

SH-E4A-66 is a C²-COUPLr (COvalent Protein Ligator) with carbazole scaffold barring heterogeneous cysteine reactive warheads (acrylamide and chloroacetamide). SH-E4A-66 is capable of coupling with EML4-ALK (EC₅₀=1.5 μM) and inhibiting the activity of EML4-ALK kinase (IC₅₀=2.3 μM).

KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC₅₀ of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies.

Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC₅₀s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research.