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(R)-SL18

Chemical Structure : (R)-SL18

CAS No.:

(R)-SL18 (ANXA3 degrader (R)-SL18)

Catalog No.: PC-20755Not For Human Use, Lab Use Only.

(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.
(R)-SL18 directly binds to ANXA3 (SPR Kd=0.58 uM) and increases its ubiquitination, thereby inducing ANXA3 degradation with moderate family selectivity.
(R)-SL18 inhibits cell proliferation against TNBC cells with IC50 of 2.52 uM for MDA-MB-231 and 1.64 uM for MDA-MB-468, induces apoptosis.
(R)-SL18 showed certain selectivity for the anti-proliferative activity of ANXA3 high-expressing cells over ANXA3 low-expressing cells.
(R)-SL18 induced ANXA3 selective degradation mainly via the ubiquitin-proteasome system.
(R)-SL18 showed excellent family selectivity toward ANXA3 degradation (except ANXA6) in vitro.
(R)-SL18 (1-5 uM) inhibited the wnt/β-catenin signaling pathway in MDA-MB-231 cells.
(R)-SL18 (20 mg/kg, i.p.) suppressed tumor growth in TNBC PDX model.

Physicochemical Properties

M.Wt 597.06
Formula C26H21ClN6O5S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

S=C(SCC(NC(NC1=CC(Cl)=CC=C1[N+]([O-])=O)=O)=O)N[C@@H]2N=C(C3=CC=CC=C3)C4=CC=CC=C4N(C)C2=O

References

1. Liang Y, et al. Acta Pharm Sin B. 2023 Apr;13(4):1686-1698.

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