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WDR5-IN-6 is a WDR5 inhibitor, targeting to WBM site. WDR5-IN-6 inhibits cell proliferation of neuroblastoma cell lines with potent anti-tumor activity. WDR5-IN-6 shows high synergy with OICR-9429 (HY-16993), a WDR5 inhibitor targeting to WIN site. WDR5-IN-6 can be used for reasearch in neuroblastoma .
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5(WDR5).WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
WDR5-IN-1 is a potent and selective WD repeat domain 5(WDR5) inhibitor, with a Kd 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 .
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.
Wdr5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Wdr5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Wdr5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Wdr5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
WDR5-IN-8 is a WDR5 inhibitor with IC50 value of 15.5 nM. WDR5-IN-8 shows good anti-proliferative activity in two human acute leukemia cell lines. WDR5-IN-8 has antitumor activity .
WDR5-IN-7 (Compound 22) is an orally bioavailable benzoxazepinone-based WD repeat domain 5 (WDR5) inhibitor. WDR5-IN-7 can be used for the research of anti-cancer .
WDR5-IN-4 (Compound C6) is a WIN site inhibitor of chromatin-associated WD repeat domain 5 protein (WDR5),Kd The value is 0.1 nM. WDR5-IN-4 is able to displace WDR5 from chromatin and reduce the expression of related genes, causing translation inhibition and nucleolar stress. Has anti-cancer effects .
WDR5-IN-4 TFA (Compound C6) is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5(WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity .
WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5(WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases .
WDR5-0102 is an inhibitor targeting WDR5-MLL1 interface (Kdis=7 μM, Kd=4 μM). WDR5-0102 suppresses MLL1 HMT activity, but not human H3K4 methyltransferase SETD7 and six other HMTs: G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5 .
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.
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.
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) .
MS33 is a potent WDR5 degrader, with Kds 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 .
OICR-0547 is a negative control, closely related derivative of OICR-9429 (HY-16993). OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction. OICR-0547 is an inactive control compound that no longer binds to WDR5 .
MM-589 (racemic mixture) TFA, is a racemic mixture of MM-589 TFA (HY-100869A). MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex .
MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
Dimethyl-F-OICR-9429-COOH a ligand for WD40 repeat domain protein 5 (WDR5) extracted from patent WO2019246570A1 intermediate 19. Dimethyl-F-OICR-9429-COOH can be used in the synthesis of PROTACs .
OICR-9429 is high affinity WD repeat domain 5(WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
WM-586 is a covalent WDR5 inhibitor. WM-586 specifically decreases WDR5 and MYC interaction with an IC50 of 101 nM. WM-586 is used in research on a variety of cancers including neuroblastoma, breast cancer, bladder cancer and colorectal cancer .
MS67 is a potent and selective WD40 repeat domain protein 5(WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .
DDO-2213 is an orally active and potent WDR5-MLL1 inhibitor, with an IC50 of 29 nM and a Kd 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 .
MM-589 is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM .
WM-662 is a WDR5-MYC interaction inhibitor, with an IC50 of 18 μM. WM-662 has potential for the research of cancer, aging, and neurodegenerative disorders .
OICR-9429-N-C2-NH2 is a ligand for Wd40 repeat domain protein 5(WDR5) extracted from patent WO2019246570A1, intermediate 2. OICR-9429-N-C2-NH2 can be used in the synthesis of PROTACs .
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .
CS-VIP 8 TFA is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 TFA induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 TFA is promising for research of hematological diseases such as leukemia .
OICR41114 (PROTAC 4) is a WDR5-targeting PROTAC degrader. OICR41114 degrades endogenous WDR5 with an EC50 and Dmax values of 40 nM and 49%, respectively. OICR41114 degrades HiBiT-tagged WDR5 in a proteasome-dependent manner . OICR41114 is composed of target protein ligand (red part) Dimethyl-F-OICR-9429-COOH (HY-141799), E3 ligase ligand (blue part) OICR-8268-acrylic acid (HY-169390) and PROTAC linker (black part) Amino-PEG9-amine (HY-140210). The conjugate of E3 ligase ligand and linker is OICR-8268-acrylic acid-amino-PEG9-amine (HY-169391).
DBL-6-13 is an inhibitor for WDR5 with a moderate binding affinity of 6.8 μM (microscale thermophoresis assay) and 9.1 μM (fluorescence polarization assay) .
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 .
MM-401 (TFA) is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos [5].
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .
CS-VIP 8 TFA is a selective allosteric WDR5 protein inhibitor (Ki= 0.008 μM). CS-VIP 8 TFA induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 TFA is promising for research of hematological diseases such as leukemia .
MM-401 is a MLL1 H3K4 methyltransferase inhibitor. MM-401 inhibits MLL1 activity (IC50 = 0.32 μM) by blocking MLL1-WDR5 interaction. MM-401 can induce cell cycle arrest, apoptosis and differentiation. MM-401 can be used for the research of MLL leukemia .
MLL3-WDR5-Ash2L-RbBP5-DPY30 Protein, Human (His) is the recombinant human-derived MLL3-WDR5-Ash2L-RbBP5-DPY30, expressed by E. coli , with N-6*His labeled tag. ,
WDR5 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 37 kDa, targeting to WDR5. It can be used for WB,IHC-P,FC assays with tag free, in the background of Human, Mouse, Rat.
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.
Wdr5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Wdr5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Wdr5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Wdr5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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.
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