WDR5 Degrader

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a K_d of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects.

MS33 is a potent WDR5 degrader, with K_ds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia.

WDR5 degrader-1 is a selective Cereblon-recruiting WDR5 PROTAC degrader. WDR5 degrader-1 induces ubiquitination and degradation of WDR5. WDR5 degrader-1 can be used in the research of pancreatic cancer and leukemia.

XF067-68 (example 132) is a PROTAC for targeted degradation of WD40 repeat domain protein 5 (WDR5). XF067-68 can be usde for the study of WDR5-mediated diseases.

OICR41114 is a WDR5 PROTAC degrader with an EC₅₀ of 40 nM. OICR41114 binds both DCAF1 and WDR5, and its binding affinity for DCAF1 is significantly enhanced in the presence of WDR5 (K_D increases from 59 nM to 5 nM). OICR41114 exerts antiproliferative effects on MV4-11 cells. OICR41114 can be used for the research of acute myeloid leukemia.

WDR5B Human Pre-designed siRNA Set A contains three designed siRNAs for WDR5B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

WDR5 Human Pre-designed siRNA Set A contains three designed siRNAs for WDR5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

XF056-132 free base (MS132N) is an inactive WDR5 PROTAC degrader with a K_d value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 free base binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 free base can be used in the research of pancreatic ductal adenocarcinoma.

PROTAC WDR5 degrader 2 is a WDR5 PROTAC degrader. PROTAC WDR5 degrader 2 induces WDR5 degradation via the ubiquitin-proteasome system by forming a ternary complex with WDR5 and an E3 ligase. PROTAC WDR5 degrader 2 can be used in leukemia-related research.

XF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a K_d value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma.

PROTAC WDR5 degrader 1 is a heterobifunctional WDR5 PROTAC degrader with a DC₅₀ value of 53 nM and a K_d value of 18 nM, exhibiting selective WDR5 degradation activity and cell permeability. PROTAC WDR5 degrader 1 induces proliferation defects in leukemia cells, with enhanced efficacy in cells overexpressing VHL. PROTAC WDR5 degrader 1 is applicable to research related to acute myeloid leukemia.

MS40 is a WDR5 PROTAC degrader with a DC₅₀ of 42 nM in MV4;11 MLL-rearranged acute myeloid leukemia (AML) cells. MS40 induces WDR5 degradation dependent on WDR5, CRBN and the proteasome, dissociates the MLL/KMT2A complex from chromatin, reduces H₃K₄me2 levels, degrades IKZF1/IKZF3, the novel substrates of CRBN, inhibits the transcription of WDR5/MLL and IKZF target genes, and suppresses cancer cell growth. MS40 can be used in the research of MLL-rearranged acute myeloid leukemia, breast cancer, Burkholderia infection and cystic fibrosis-associated bacterial infections.