BBDDL2059
BBDDL2059 is a selective covalent inhibitor of histone methyltransferase EZH2 with an IC50 of 1.5 nM for EZH2-Y641F. BBDDL2059 inhibits lymphoma cell growth at nanomolar concentrations and can be used for anticancer research.
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- No. CAS: 2691174-27-1
- Fòrmula: C27H36N4O4S
- Peso molecular:512.66
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Descripciòn
IC50 & Target
[1]|
EZH2 Y641F mutant type 1.5 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DB | IC50 |
>3 μM
Compound: 16; BBDDL2059
|
Antiproliferative activity against human DB cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human DB cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
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[PMID: 37203326] |
| KARPAS-422 | IC50 |
0.064 μM
Compound: 16; BBDDL2059
|
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human KARPAS-422 cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
|
[PMID: 37203326] |
| OPM-2 | IC50 |
>3 μM
Compound: 16; BBDDL2059
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Antiproliferative activity against human OPM-2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human OPM-2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
|
[PMID: 37203326] |
| Pfeiffer | IC50 |
0.022 μM
Compound: 16; BBDDL2059
|
Antiproliferative activity against human Pfeiffer cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human Pfeiffer cells expressing EZH2 Y641N mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
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[PMID: 37203326] |
| SU-DHL-2 | IC50 |
>3 μM
Compound: 16; BBDDL2059
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Antiproliferative activity against human SUDHL2 cells expressing EZH2 mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human SUDHL2 cells expressing EZH2 mutant assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
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[PMID: 37203326] |
| U2932 | IC50 |
>3 μM
Compound: 16; BBDDL2059
|
Antiproliferative activity against human U2932 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human U2932 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
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[PMID: 37203326] |
| WSUDLCL2 | IC50 |
>3 μM
Compound: 16; BBDDL2059
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Antiproliferative activity against human WSUDLCL2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
Antiproliferative activity against human WSUDLCL2 cells expressing wild-type EZH2 assessed as inhibition of cell proliferation incubated for 6 days by CCK8 assay
|
[PMID: 37203326] |
In Vitro
BBDDL2059 (Compound 16) ( 0-65 nM; 6 days) inhibits cell growth in KARPAS-422 and Pfeiffer cells[1].
BBDDL2059 ( 0-1 μM; 48-96 hours) inhibits EZH2 enzymatic activity and maintains long-lasting inhibition of EZH2 after washing out[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KARPAS-422 cells and Pfeiffer cells
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Concentration:0-65 nM
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Incubation Time:6 day
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Result:Inhibited cell growth with IC50s of 64 nM and 22 nM for KARPAS-422 and Pfeiffer cells, respectively.
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Cell Line:KARPAS-422 cells and Pfeiffer cells
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Concentration:0.05,0.1,0.5,1 μM
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Incubation Time:48-96 hours
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Result:Effective reduces H3K27me3 in Pfeiffer cells in a concentration- and time-dependent manner.
Significantly inhibited the levels ofH3K27me3 in cells after treated within 96h after being washed out, and the levels of H3K27me3 were still lower than negative control after 120 h.
In Vivo
Pharmacokinetic parameters for BBDDL2059 (Compound 16) in rats[1]
| Route | Dose (mg/kg) | T1/2 (h) | Cmax (ng/mL) | AUC0-last (h•ng/mL) | CL (mL•min-1/kg-1) | Vss (L/kg) | F (%) |
| iv | 3 | 0.28 | / | 4886 | 11.1 | 161 | / |
| po | 10 | / | 29.5 | 8.16 | / | / | 0.05 |
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