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WDR5-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) DNA/RNA Synthesis (1) HDAC (1) Ligands for Target Protein for PROTAC (1) PROTACs (2) WDR5 (12)
By Research Areas:	Cancer (10)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-133121

*WDR5-IN-1*	Apoptosis WDR5	Cancer
WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a K_d of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC₅₀ of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines .

HY-153331

DDO-2213	WDR5	Cancer
DDO-2213 is an orally active and potent *WDR5-MLL1* inhibitor, with an IC₅₀ of 29 nM and a K_d value of 72.9 nM for the WDR5 protein. DDO-2213 selectively inhibits MLL (mixed lineage leukemia) histone methyltransferase activity and the proliferation of MLL translocation-harboring cells. DDO-2213 can be used for MLL fusion leukemia research .

HY-148817

WDR5-0102	WDR5	Cancer
WDR5-0102 is an inhibitor of *WDR5. WDR5-0102 specifically targets the WIN* site of *WDR5, disrupts the WDR5-MLL1* interaction, and reduces the histone methyltransferase activity of MLL1. WDR5-0102 exerts dose-dependent toxicity on MDSC-like cells and reduces their osteopontin levels, while showing extremely low cytotoxicity to pancreatic cancer cells. WDR5-0102 can be used in the research of related diseases such as acute myeloid leukemia, lymphoid leukemia, biphenotypic leukemia and pancreatic cancer .

HY-178751

Z116334910	WDR5	Cancer
Z116334910 is a promising *WDR5-MLL1* interaction disruptor. Z116334910 can be used for the study of cancer .

HY-162014

*WDR5 degrader-1*	PROTACs WDR5	Cancer
WDR5 degrader-1 (compound 25) is a cereblon (CRBN)-recruiting WDR5 degrader. WDR5 degrader-1 selectively degraded WDR5 over the CRBN neo-substrate IKZF1 .

HY-157659

WDR5-47	WDR5	Others
WDR5-MLL1 antagonist 1 (compound 47) is a compound optimized through protein crystal structure guidance. It has stronger antagonistic activity against WDR5-MLL interaction with a dissociation constant (Kd) of 0.3μM.

HY-178752

Z88418521	WDR5	Cancer
Z88418521 is a ligand for the *WDR5-MLL1* complex. Z88418521 may help disrupt the interaction of the *WDR5-MLL1* complex. Z88418521 can be used in cancer research, especially in leukemia .

HY-163774

WDR5-MYC-IN-1	WDR5	Cancer
WDR5-MYC-IN-1 (compound 4o) is a potent *WDR5-MYC* interaction inhibitor with a Ki value of 1.0 µM. WDR5-MYC-IN-1 shows antiproliferative activity .

HY-168487

PROTAC WDR5 degrader 1	DNA/RNA Synthesis PROTACs WDR5	Others
PROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting *WDR5. PROTAC WDR5 degrader 1* is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A) .

HY-168475

DD0-2363	Apoptosis WDR5 HDAC	Cancer
DD0-2363 (Compound 32d) is a dual-target inhibitor of *WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis* in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia .

HY-168488

WDR5 ligand 2	WDR5 Ligands for Target Protein for PROTAC	Cancer
WDR5 ligand 2 is the ligand for *WDR5* and can be used for synthesis of PROTAC WDR5 degrader 1 (HY-168487) .

HY-183959

DC_M5_2	WDR5	Cancer
DC_M5_2 is a WD40 repeat domain protein 5 (WDR5) inhibitor with an IC₅₀ of 9.63 μM and a K_D of 13.8 μM. DC_M5_2 binds to the WDR5 pocket that interacts with the MLL1 peptide, blocking the *WDR5-MLL1* protein-protein interaction . DC_M5_2 can be used in leukemia-related research .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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WDR5-IN-1

Inhibitors & Agonists