HA14-1

• CAS: 65673-63-4
• Catalog Number: ACM65673634
• Category: Inhibitors
• Molecular Weight: 409.24
• Molecular Formula: C17H17BrN2O5
• Description: HA14-1 is a potent Bcl-2 inhibitor with potential anticancer activity. HA14-1 induces apoptosis in various human cancer cells. HA14-1 suppressed NF-kappaB activation through inhibition of phosphorylation and degradation of IkappaBalpha. This inhibition was correlated with suppression of NF-kappaB-dependent gene products (c-myc, cyclin D1, cox-2, and IAP-1). Additionally, HA14-1 also markedly sustained TNF-alpha-mediated JNK activation.
• Synonyms: HA-141, HA 141, HA141
• IUPAC Name: (R)-ethyl 2-amino-6-bromo-4-((R)-1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
• Canonical SMILES: O=C(C1=C(N)OC2=C(C=C(Br)C=C2)[C@H]1[C@H](C#N)C(OCC)=O)OCC
• InChI: InChI=1S/C17H17BrN2O5/c1-3-23-16(21)11(8-19)13-10-7-9(18)5-6-12(10)25-15(20)14(13)17(22)24-4-2/h5-7,11,13H,3-4,20H2,1-2H3/t11-,13-/m0/s1
• InChI Key: SXJDCULZDFWMJC-AAEUAGOBSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >5 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: HA14-1 is a Bcl-2/Bcl-XL antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC50 of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 49.89; H, 4.19; Br, 19.53; N, 6.85; O, 19.55
• Exact Mass: 408.03208
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: HA14-1 potentiated BIRD-2-induced Ca(2+) release from the ER and apoptosis in both BIRD-2-sensitive DLBCL cell lines (SU-DHL-4) and in primary B-CLL cells.; Reference: Int J Dev Biol. 2015;59(7-9):391-8. https://pubmed.ncbi.nlm.nih.gov/26260683/
• In Vivo Activity: TBD
• Shipping: 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.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).