2. Epigenetics
  3. Histone Methyltransferase
  4. 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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BBDDL2059 Chemical Structure

BBDDL2059 Chemical Structure

CAS No. : 2691174-27-1

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Description

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[1].

IC50 & Target[1]

EZH2 Y641F mutant type

1.5 nM (IC50)

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.

BBDDL2059 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: KARPAS-422 cells and Pfeiffer cells
Concentration: 0-65 nM
Incubation Time: 6 day
Result: Inhibited cell growth with IC50s of 64 nM and 22 nM for KARPAS-422 and Pfeiffer cells, respectively.

Western Blot Analysis[1]

Cell Line: KARPAS-422 cells and Pfeiffer cells
Concentration: 0.05,0.1,0.5,1 μM
Incubation Time: 48-96 hours
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

BBDDL2059 (Compound 16) (3 mg/kg for i.v., 10 mg/kg for p.o.) shows a T1/2 of 0.28 h (i.v.), and oral bioavailability (F%) of 0.05% in rats[1].
Pharmacokinetic parameters for BBDDL2059 (Compound 16) in rats[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Animal Model: Rats(Pharmacokinetic assay)[1]
Dosage: 3 or 10 mg/kg
Administration: Oral gavage (p.o.), Intravenous injection (i.v.)
Result: Showed a T1/2 of 0.28h (i.v.) and oral bioavailability (F%) of 0.05%.
Molecular Weight

512.66

Formula

C27H36N4O4S
CAS No.
SMILES

O=C(C1=CC(CNC(C=C)=O)=CC(N(C2CCOCC2)CC)=C1C)NCC3=C(C=C(NC3=O)C)SC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BBDDL2059 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BBDDL20592691174-27-1BBDDL 2059BBDDL-2059Histone MethyltransferaseHistone Methyltransferase,EZH2covalent inhibitorcancerKARPAS-422Pfeiffer cellsInhibitorinhibitorinhibit

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