Cancer Targeted Therapy

Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET V804L is a mutant of RET. RET V804L Recombinant Human Active Protein Kinase is a recombinant RET V804L protein that can be used to study RET V804L-related functions.

LCK ligand-1 is a ligand targeting LCK, which serves as a target protein ligand for the synthesis of the PROTAC degrader SJ45566 (HY-162676).

CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC₅₀ = 0.034 μM, CBP IC₅₀ = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC₅₀ values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.

UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC₅₀ of 695.30 nM and a K_D of 114.3 nM for ULK1; it inhibits hERK1 with an IC₅₀ of 179.90 nM and a K_D of 114 nM for ERK1; it shows weak binding to ERK2 with a K_D of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer.

PROTAC CRABP-II Degrader-2 is a cellular retinoic acid-binding protein (CRABP-II) SNIPER degrader. PROTAC CRABP-II Degrader-2 hijacks the cIAP1 E3 ligase to induce ubiquitination and proteasomal degradation of CRABP-II. PROTAC CRABP-II Degrader-2 can be used for the research of neuroblastoma.

hsa-miR-4457 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-548f-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-6872-3p 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.

mmu-miR-3070-3p 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.

mmu-miR-6915-3p 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.

3-Phenylpropyl isothiocyanate has a stronger inhibitory effect on N-nitrosomethyl-benzylamine (NMBA) tumorigenesis. 3-Phenylpropyl isothiocyanate has chemopreventive effects.

Finasteride (Standard) is the analytical standard of Finasteride. This product is intended for research and analytical applications. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC₅₀ of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.

TMV-IN-1, chalcone derivative, is a tobacco mosaic virus (TMV) inhibitor. TMV-IN-1 has good therapeutic activity and protective activity against TMV with EC₅₀ values of 70.7 μg/mL and 60.8 μg/mL, respectively. TMV-IN-1 can be used for the research of infection, inflammation and tumor.

6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.

Onvitrelin ucalontide (Phor18-LHRH (338613); EP-100) is a luteinizing hormone-releasing hormone (LHRH) receptor ligand. Onvitrelin ucalontide binds to functional LHRH receptors on cancer cells and mediates targeted cytotoxicity. Onvitrelin ucalontide reduces tumor volume, weight and the number of viable tumor cells in xenograft models. Onvitrelin ucalontide can be used for the research of breast cancer, ovarian cancer and prostate cancer.

hsa-miR-23b-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-181b-2-3p 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.

T-3256336 is a potent and orally active cIAP1 and XIAP inhibitor with IC₅₀s of 1.3, 200 nM, respectively. T-3256336 shows anti-tumor activity.

N4-Benzoyl-5-methylcytidine 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.

BET-IN-29 (Compound 1) is a bromodomain and the terminal motif (BET) inhibitor. BET-IN-29 can be used for the study of cancer, inflammation, metabolism, neurological diseases, and infectious diseases.