1. Epigenetics
  2. Histone Methyltransferase
  3. BI-9321 trihydrochloride

BI-9321 trihydrochloride 

Cat. No.: HY-114208A
Handling Instructions

BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells.

For research use only. We do not sell to patients.

BI-9321 trihydrochloride Chemical Structure

BI-9321 trihydrochloride Chemical Structure

CAS No. : 2387510-87-2

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Description

BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

IC50 & Target

Kd: 166 nM (NSD3-PWWP1)[1]

In Vitro

BI-9321 trihydrochloride is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 trihydrochloride downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].

Molecular Weight

469.81

Formula

C₂₂H₂₄Cl₃FN₄

CAS No.

2387510-87-2

SMILES

NCC1=CC(C)=C(C2=C(C3=CC=NC4=CC(F)=CC=C34)N(C)C=N2)C(C)=C1.[H]Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BI-9321 trihydrochlorideHistone MethyltransferaseNSD3PWWP1histoneprobeMycmessengerRNAInhibitorinhibitorinhibit

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BI-9321 trihydrochloride
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