EN219
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MedKoo CAT#: 464832

CAS#: 380351-29-1

Description: EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114. It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50 = 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 µM. EN219 (1 µM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP human breast cancer cells in a proteomic profiling assay. It has been linked to the bromodomain and extra terminal domain (BET) inhibitor ligand (+)-JQ1 for use as a proteolysis-targeting chimera (PROTAC) to degrade bromodomain-containing protein 4 (BRD4) in 231MFP cells.

Chemical Structure

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EN219
CAS# 380351-29-1
Instruction

Theoretical Analysis

MedKoo Cat#: 464832
Name: EN219
CAS#: 380351-29-1
Chemical Formula: C17H13Br2ClN2O
Exact Mass: 453.91
Molecular Weight: 456.562
Elemental Analysis: C, 44.72; H, 2.87; Br, 35.00; Cl, 7.76; N, 6.14; O, 3.50

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
50mg USD 1250 2 Weeks
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Synonym: EN219; EN 219; EN-219;

IUPAC/Chemical Name: 1-(3,5-bis(4-bromophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-2-chloroethan-1-one

InChi Key: CXRHMHAKZPJNKS-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H13Br2ClN2O/c18-13-5-1-11(2-6-13)15-9-16(22(21-15)17(23)10-20)12-3-7-14(19)8-4-12/h1-8,16H,9-10H2

SMILES Code: BrC1=CC=C(C2N(N=C(C2)C3=CC=C(C=C3)Br)C(CCl)=O)C=C1

Appearance: Solid powder

Purity: >95% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 21.90
DMSO 5.0 10.95
Ethanol 1.0 2.19

Preparing Stock Solutions

The following data is based on the product molecular weight 456.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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