Cancer Targeted Therapy

GSK235 is an orally active, selective and allosteric endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor with pIC₅₀ values of 8.45 and 7.59 for human and mouse ERAP1, respectively. GSK235 exhibits over 1000-fold selectivity for the two most homologous enzymes, ERAP2 and IRAP. GSK235 can regulate the immunopeptidome of cancer cells and enhance cancer cell antigenicity. GSK235 can be used for the study of colorectal cancer and arthritis.

NCATS-SM1440 is a glycolysis inhibitor and metabolic regulator that targets LDHA and LDHB (IC₅₀=0.06 μM and 0.03 μM, respectively). Upon binding to LDHA, NCATS-SM1440 blocks the glycolysis pathway and reduces lactate production. NCATS-SM1440 drives the shift of pyruvate metabolism toward mitochondrial metabolism, effectively disrupting the dependence of cancer cells on aerobic glycolysis. NCATS-SM1440 can be widely used in research related to cancer, Ewing's sarcoma, and other related conditions.

Kuwanon H (Standard) is the analytical standard of Kuwanon H. This product is intended for research and analytical applications. Kuwanon H is a selective non-peptide bombesin receptor antagonist and platelet activation inhibitor. Kuwanon H also acts as a specific antagonist of GRP-preferring receptors, with a K_i value of 290 nM for mouse GRP-R and 6500 nM for rat NMB-R. Kuwanon H inhibits the phosphorylation of AKT, mTOR, ERK, cPLA₂ and p38, and upregulates TRIB3. It induces endoplasmic reticulum stress, apoptosis and autophagosome formation. Kuwanon H blocks calcium mobilization, mitogenic signaling, DNA synthesis, dense granule secretion, thromboxane A₂ generation and integrin αIIb/β₃ activity. It inhibits collagen-induced platelet aggregation and fibronectin adhesion, and delays clot retraction. Kuwanon H inhibits melanoma cell growth in vitro and in vivo, and enhances the sensitivity of melanoma cells to CDDP. It can be used in research related to melanoma, small cell lung cancer and thrombosis.

hsa-miR-2355-5p 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-4490 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-556-3p 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.

Nitromifene is an antagonist of estrogen receptor (ER).

RSH-7 is a potent BTK and FLT3 inhibitor with IC₅₀s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.

2’-Deoxy-2’-fluoro- N3-(2S)-(2-amino-3-carbonyl)-propyluridine 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.

BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels.

m-PEG4-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Cdc7-IN-15 (Example 108) is a cdc7 kinase inhibitor. Cdc7-IN-15 can be used for cancer research.

PKRA83 (PKRA7) hydrochloride is a potent PK2 antagonist that competes for PK2 binding to its receptors, PKR1 and PKR2. PKRA83 hydrochloride potently inhibits PK2 receptors with IC₅₀ values of 5.0 nM and 8.2 nM for PKR1 and PKR2, respectively. PKRA83 hydrochloride exhibits anticancer, antiarthritis, and antiangiogenic activities.

hsa-miR-9902 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-466b-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-7028-5p 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.

rno-miR-3579 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.

Aliskiren-d₆ (hydrochloride) is is deuterium labeled Aliskiren, which is a direct renin inhibitor.

PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity.

NSC81111 is a potent and orally active EGFR-TK inhibitor with an IC₅₀ of 0.15 nM. NSC81111 has anticaner effects.