WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H556145
CAS#: 757192-67-9
Description: EN106 is a potent inhibitor of FEMIB. EN106 targets FEM1B, an E3 ligase recently discovered as the critical component of the cellular response to reductive stress. By targeting C186 in FEM1B, EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1. EN106 can be used as a covalent recruiter for FEM1B in TPD applications by demonstrating that a PROTAC linking EN106 to the BET bromodomain inhibitor JQ1 or the kinase inhibitor dasatinib leads to the degradation of BRD4 and BCR-ABL, respectively.
Hodoodo Cat#: H556145
Name: EN106
CAS#: 757192-67-9
Chemical Formula: C13H13ClN2O3
Exact Mass: 280.0615
Molecular Weight: 280.708
Elemental Analysis: C, 55.62; H, 4.67; Cl, 12.63; N, 9.98; O, 17.10
This product is not in stock, which may be available by custom synthesis.
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Synonym: EN106; EN-106; EN 106
IUPAC/Chemical Name: 2-chloro-N-(2-cyanoethyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acetamide
InChi Key: GLDJSVHDOXCYPT-UHFFFAOYSA-N
InChi Code: InChI=1S/C13H13ClN2O3/c14-9-13(17)16(5-1-4-15)10-2-3-11-12(8-10)19-7-6-18-11/h2-3,8H,1,5-7,9H2
SMILES Code: O=C(N(CCC#N)C1=CC=C(OCCO2)C2=C1)CCl
Appearance: To be determined
Purity: >98% (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
The following data is based on the product molecular weight 280.708 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.
| 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 |
Henning NJ, Manford AG, Spradlin JN, Brittain SM, Zhang E, McKenna JM, Tallarico JA, Schirle M, Rape M, Nomura DK. Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications. J Am Chem Soc. 2022 Jan 19;144(2):701-708. doi: 10.1021/jacs.1c03980. Epub 2022 Jan 7. PMID: 34994556; PMCID: PMC8928484.
