dr-5

Cyproterone acetate (Cyproterone 17-O-acetate) binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.Cyproterone binds the androgen receptor (AR), thereby preventing androgen-induced receptor activation in target tissues and inhibiting the growth of testosterone-sensitive tumor cells. Cyproterone Acetate is the acetate salt of a synthetic steroidal antiandrogen with weak progestational and antineoplastic activities. This agent also exerts progestational agonist properties at the level of the pituitary that reduce luteinizing hormone (LH), resulting in reductions in testicular androgen secretion and serum testosterone levels. Treatment with cyproterone alone results in incomplete suppression of serum testosterone levels.

Bioymifi (DR5 Activator) is an effective activator of the TRAIL receptor DR5, binding to the extracellular domain (ECD) of DR5 with a Kd of 1.2 μM. Bioymifi can serve as a novel mimetic of TNF-related apoptosis-induced ligand (TRAIL), inducing DR5 aggregation as a sole inducer, and stimulating cell apoptosis.

Conatumumab (AMG 655) is a monoclonal agonist antibody targeting human death receptor 5 [DR5, TRAILR2] with a dissociation constant (Kd) of 1 nM for long DR5 and 0.8 nM for short DR5. It induces apoptosis in various tumor types through caspase activation and can be used to study advanced solid tumors.

Drozitumab (PRO 95780) is a fully humanized antibody targeting the death receptor DR5 that shows anti-tumor activity against rhabdomyosarcoma, binds to the death receptor DR5 and induces apoptosis, and can be used in the study of triple-negative breast cancer.

Lexatumumab (GHS-ETR 2) is a human excitatory monoclonal antibody targeting TRAIL receptor 2 that has anticancer activity and induces apoptosis in malignant mesothelioma. Lexatumumab can be used to study malignant pleural mesothelioma (MPM).

Benufutamab (GEN1029) is an agonistic antibody targeting death receptor 5 (DR5) with anti-tumor activity, used in the study of solid tumors.

Tilogotamab (GEN-1029) is an agonistic hexameric complex targeting two independent epitopes on DR5, used for studying multiple myeloma (MM).

Anti-Mouse DR5/CD262 Antibody (MD5-1) is an inhibitor derived from a hamster in the United States, specifically targeting the mouse DR5/CD262 as an IgG, κ antibody.

MS67 is a potent and selective degrader of WD40 repeat domain protein 5 (WDR5) with a dissociation constant (Kd) of 63 nM, exhibiting no activity against protein methyltransferases, kinases, G-protein-coupled receptors (GPCRs), ion channels, and transporters, and notably demonstrating significant anticancer properties.

WDR5-0103 hydrochloride[890190-22-4(free base)] (WD-Repeat Protein 5-0103) is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).

WDR5-47 is a potent small molecule to disturb the interaction of MLL1-WDR5 with IC50 value of 0.3μM.

MM-589 is a potent WD repeat domain 5 (WDR5) inhibitor and mixed lineage leukemia (MLL) protein-protein interaction.

MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and a modulator of mixed lineage leukemia (MLL) protein-protein interaction.

WIN site inhibitor 1 is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM), with anti-cancer activity.

Homer is a specific probe targeting WDR5. In MV4-11 cells, Homer induces the degradation of WDR5 protein with a DC50 of 53 nM. At a concentration of 1 µM, Homer reduces WDR5 protein levels in MV4-11 cells without affecting its mRNA expression.

WDR5ligand 2 is a ligand for WDR5 and can be utilized in the synthesis of PROTAC WDR5degrader 1.

WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazinone-based inhibitor of the WD repeat domain 5 (WDR5). It is useful in cancer research.

WDR5degrader-1 is a cereblon (CRBN) degrader that recruits WDR5. It selectively targets CRBN's new substrate IKZF1 for the degradation of WDR5.

WDR5-IN-8 is a WDR5 inhibitor with an IC50 value of 15.5 nM. It displays significant antiproliferative activity in two human acute leukemia cell lines and possesses antitumor properties.

WDR5-MYC-IN-2 is an inhibitor of the WDR5-MYC protein-protein interaction (PPI) with an IC50 of 0.59 μM. It is utilized in research on MYC-driven cancers and in the development of other potent WDR5-MYC PPI inhibitors.

Dexrazoxane (ICRF-187) is an anticancer drug used to block mitosis and arrest dividing cells. It is an iron chelator and provides cardioprotection against anthracycline toxicity.

WDR5-0103 (WD-Repeat Protein 5-0103) is an effective and specific WD repeat-containing protein 5 (WDR5) antagonist (Kd: 450 nM).

MS33 is a highly effective degrader of the WDR5 protein, exhibiting Kd values of 870 nM and 120 nM for VCB and WDR5, respectively. It induces degradation of WDR5 through an E3 ligase VHL-mediated and proteasome-dependent mechanism. MS33 holds promise for furthering research in the field of acute myeloid leukemia.

WDR5-IN-5 is a selective, orally active inhibitor targeting the WD repeat domain 5 (WDR5) WIN site.WDR5-IN-5 exhibits high affinity for WDR5 (Ki<0.02 nM).WDR5-IN-5 exhibits anti-cancer cell proliferation and a good pharmacokinetic profile.