Cancer Targeted Therapy

hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual Carbonic Anhydrase(CA) IX/XII with K_i values of 4.7 nM and 8.3 nM for hCA XII and hCA IX, respectively. hCA/VEGFR-2-IN-1 (compound 13a) is a potent VEGFR-2 inhibitor with IC₅₀ values 26.3 nM. hCA/VEGFR-2-IN-1 has anticancer activity.

CHX-3107 is a casein kinase 2 inhibitor .

CAIX/CAXII-IN-2 (compound 23) is a CAIX/CAXII inhibitor, with K_i values ​​of 8.9 nM and 5.3 nM for CAIX/CAXII, respectively. CAIX/CAXII-IN-2 can be used in cancer research.

mmu-miR-7649-3p 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.

hsa-miR-4725-5p 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.

hsa-miR-6507-5p 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.

mmu-miR-101a-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.

mmu-miR-466l-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-7035-5p 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.

Pantoprazole-d₃ is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).

HDAC8-IN-15 is a selective HDAC8 inhibitor with an IC₅₀ of 0.40 μM. HDAC8-IN-15 increases the acetylation level of the HDAC8 substrate SMC3 without altering the total protein level of SMC3. HDAC8-IN-15 reduces cancer cell viability, inhibits colony formation, slows cell migration, induces apoptosis, and causes cell cycle arrest at the SubG1 phase. HDAC8-IN-15 can be used in studies related to neuroblastoma.

L-NMMA (Tilarginine) citrate is a non-selective and competitive inhibitor of nitric oxide synthase. L-NMMA citrate inhibits three subtypes, namely nNOS, eNOS, and iNOS, and reduces NO production. L-NMMA citrate alleviates mechanical allodynia, thermal hyperalgesia, and choroidal fibrosis. L-NMMA citrate is applicable to research related to nociception, bone cancer pain, and myopia.

Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of the MEK1 Derived Peptide Inhibitor 1 (HY-P4133). Myristoyl-MEK1 Derived Peptide Inhibitor 1 inhibits ERK activation with an IC₅₀ of 10 μM.

ABT 737-d₈ is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

STAT3-IN-5 is a potent STAT3 inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC₅₀ value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer.

Tubulin/HDAC-IN-3 (compound 12a) is a potent tubulin/HDAC dual inhibitor. Tubulin/HDAC-IN-3 effectively disrupts tubulin polymerization (IC₅₀: 5.4 μM). Tubulin/HDAC-IN-3 exhibits potent HDAC1/8 inhibitory activities, with IC₅₀ values of 0.155 and 0.177 μM, respectively. Tubulin/HDAC-IN-3 works through blocking cellular cycle, inducing apoptosis and inhibiting colony formation.

IDO1-IN-32 (Compound 45) is a potent and orally effective IDO1 inhibitor with an IC₅₀ of 10 pM. IDO1-IN-32 exhibits significant anti-proliferative activity against Hela cells. IDO1-IN-32 can significantly inhibit tumor growth in CT26 and LCC transplanted mouse models by activating anti-tumor immunity. IDO1-IN-32 can be used for research on colon cancer and breast cancer.

LNP23 is a selective PI3Kα inhibitor with an IC₅₀ of 5.15 nM. LNP23 inhibits PI3K/AKT signaling and induces apoptosis and G1 phase arrest in MCF-7 cells. LNP23 also inhibits cancer cell proliferation, colony formation, and migration. LNP23 can be used for breast cancer and lung adenocarcinoma research.

HDAC6-IN-25 (compound 8) is a selective inhibitor of HDAC6, with the IC50 of 0.6 nM.

rno-miR-101b-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.