Bladder Cancer

Sphingosine-1-phosphate (S1P) is an agonist of S1P_1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca²⁺ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids. Sphingosine-1-phosphate stimulates the DNA synthesis, cell proliferation and migration.

α-Linolenic acid (ALA (free base); C18:3 (9Z,12Z,15Z) (free base); C18:3 n-3 (free base)) is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.

Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer.

Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

Enfortumab vedotin-ejfv is an anti-Nectin-4 antibody-drug conjugate. Enfortumab vedotin-ejfv is a fully humanized IgG1 antibody conjugated to the microtubule disrupting agent MMAE (HY-15162) via a protease-cleavable Val-Cit linker. The antibody portion is Enfortumab (HY-P99016), and the drug-linker conjugate for ADC is VcMMAE (HY-15575). Nectin-4 is an adhesion protein involved in cellular processes and tumorigenesis, and Enfortumab vedotin-ejfv is indicated for the inhibition of locally advanced or metastatic urothelial carcinoma.

Human UGT1A6 is a UDP-glucuronosyltransferase. UGT1A6 catalyzes the glucuronidation of 5-hydroxytryptamine (HY-B1473A), 1-Naphthol (HY-Y1309), and Acetaminophen (HY-66005). Human UGT1A6 can be used in studies related to the pathogenesis of bladder cancer.

Scopadulciol is an orally effective β-catenin degrader, HSV-TK activator and proton pump inhibitor. By inducing β-catenin degradation, Scopadulciol downregulates the expression of downstream target genes such as cyclin D1, c-myc, and survivin; it also upregulates DR4/DR5 and downregulates Bcl-2, thereby exerting cytotoxicity and inducing apoptosis in cancer cells. Scopadulciol enhances the tumor-killing and bystander effects of prodrugs via activating HSV-TK, and can inactivate HSV-1. It shows synergistic antiviral effects when combined with Acyclovir (HY-17422) or Ganciclovir (HY-13637), with no cytotoxicity as a single agent. Scopadulciol can be applied in research related to bladder cancer, cervical cancer, glioblastoma, and digestive system cancers.

GRWD5769 is an orally potent ERAP1 inhibitor. GRWD5769 regulates the peptide repertoire presented by MHC-I, alters TCR diversity/clonality, reprograms antigen-experienced T cells, induces novel T cell responses, drives tumor cell killing, and alleviates T cell exhaustion. GRWD5769 can be used in the research of advanced solid malignancies, microsatellite-stable colorectal cancer, non-small cell lung cancer, bladder cancer, hepatocellular carcinoma, head and neck squamous cell carcinoma, and cervical cancer.

Trastuzumab vedotin (MRG002; Trastuzumab MMAE) is an antibody-drug conjugate and cytotoxin targeting HER2, with a K_d of 7.50E-11 M for human HER2. After binding to HER2, Trastuzumab vedotin undergoes internalization and lysosomal trafficking, delivering a cytotoxic payload to HER2-expressing cells and inducing tumor regression in in vivo xenograft models with HER2-expressing tumors. The anti-tumor activity of Trastuzumab vedotin is enhanced when used in combination with anti-PD-1 antibodies, and it exhibits preclinical anti-tumor activity in drug-resistant breast cancer, gastric cancer, and urothelial carcinoma PDX models. Trastuzumab vedotin has low antibody-dependent cellular cytotoxicity activity and can be used in studies related to HER2-positive breast cancer, HER2-positive gastric cancer, and unresectable locally advanced or metastatic HER2-positive urothelial carcinoma.

Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003).

Samrotamab (PR-1498487) is a humanized IgG1-κ chimeric monoclonal antibody targeting LRRC15, with a K_d of 5.42 nM for human LRRC15. Samrotamab can be used to synthesize antibody-drug conjugates (ADC). Samrotamab disrupts the LRRC15-SCG5 signaling module, binds to a membrane-proximal conformational epitope within the C-terminal leucine-rich repeat region of LRRC15, and binds to the lateral edge of the LRR solenoid while leaving the canonical concave β-sheet surface fully exposed. Samrotamab reduces the viability of bladder cancer cells, inhibits clonogenic growth, impairs cell migration, and compromises cell invasion. Samrotamab induces compensatory upregulation of LRRC15 transcripts while suppressing the expression of SCG5 mRNA. Samrotamab is applicable to research related to urothelial carcinoma, sarcoma, osteosarcoma, and undifferentiated pleomorphic sarcoma.

RNase A (Bovine pancreatic RNase) is a widely used Endonuclease in DNA purification by specifically hydrolyzing cytosine or uracil residues of RNA. RNase A degrades the RNA in the RNA/DNA duplex. RNase A catalyses the breakdown of 3',5'-phosphodiester linkages of single stranded RNA. RNase A family members in organisms are tightly involved in various physiological and pathological processes including cell growth and development, proliferation, differentiation and migration. Dysregulation of RNase A activity or expression level is closely related to pancreatic, ovarian, bladder and thyroid cancer. RNase A has tumor cell-killing ability. RNase B, Bovine Pancreas (Ribonuclease B, Bovine Pancreas) is the N-glycosylated form of RNase A. RNase B, Bovine Pancreas can promote the folding of polypeptide chains and play a role similar to molecular chaperones.

Insulin glargine is a long-acting insulin analog. Insulin glargine has the effect of lowering blood sugar and can be used in the research of diabetes. In addition, high doses of Insulin glargine can promote the proliferation of bladder cancer cells.

BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8⁺ T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields.

Daratumumab (PBS) (Anti-Human CD38) is the first-in-class human-specific anti-CD38 monoclonal antibody (IgG1). Daratumumab (PBS) has anti-multiple myeloma (MM) effect. Daratumumab (PBS) impairs MM cell adhesion, which results in an increased sensitivity of MM to proteasome inhibition.

Durvalumab (anti-PD-L1)(MEDI 4736) is a human anti-PD-L1 protein monoclonal antibody. Durvalumab (anti-PD-L1) completely blocks PD-L1 binding to PD-1 and CD80, IC ₅₀ are 0.1 and 0.04 nM respectively, has anti-tumor activity.

Dabogratinib (TYRA-300) is an orally active, selective FGFR3 inhibitor with an IC₅₀ of 11 nM. Dabogratinib exhibits antitumor activity against urothelial carcinoma and solid tumors. Dabogratinib downregulates the FGFR3 and ERK1/2 signaling pathways, and induces tumor growth inhibition and regression in FGFR3-altered xenograft models. Dabogratinib promotes chondrocyte proliferation and differentiation, drives endochondral bone formation and overall body growth, partially restores long bone proportions, and improves craniofacial and spinal morphology. Dabogratinib can be used for the research of metastatic urothelial carcinoma, achondroplasia and hypochondroplasia.

PLX51107 is a potent and selective BET inhibitor, with K_ds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (K_d, in the 100 nM range).

Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.

QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC₅₀ of 10 nM for BRD4 BD1 Protein.