ACBI1 | Degrader (PROTAC) of SMARCA2, SMARCA4, PBRM1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
In Vivo

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SMARCA2
  • IC50, Ki:770 nM Binary; 26 nM Ternary; 450 nM Binary (Ki); 16 nM Ternary (Ki)
  • DC 50:6 nM
SMARCA4
  • IC50, Ki:770 nM Binary; 26 nM Ternary; 450 nM Binary (Ki); 16 nM Ternary (Ki)
  • DC 50:11 nM
PBRM1
  • IC 50:770 nM Binary; 26 nM Ternary; 450 nM Binary (Ki); 16 nM Ternary (Ki)
  • DC 50:32 nM
Degrader (PROTAC)
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Mass Spectrometry
Selectivity Assessment Description:
Effects of ACBI1 and cis-ACBI1 @ 333 nM for 8 h on the proteome of MV-4-11 cells were assessed by ...

Potency
Cellular
In Vitro

SMARCA2

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-019-0294-6

SMARCA4

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-019-0294-6

PBRM1

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1038/s41589-019-0294-6

Negative Control Compounds

cis-ACBI1

Orthogonal Probes def

PFI-3
SGC-SMARCA-BRDVIII

Chemical Information

Molecular Formula C49H58FN9O7S
SMILEs Cc1ncsc1-c1ccc(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)C2(F)CC2)C(C)(C)C)c(OCCOc2ccc(CN3CCN(c4cc(-c5ccccc5O)nnc4N)CC3)cc2)c1
InChI InChI=1S/C49H58FN9O7S/c1-30-42(67-29-53-30)32-11-12-33(26-52-45(62)39-24-34(60)28-59(39)46(63)43(48(2,3)4)54-47(64)49(50)15-16-49)41(23-32)66-22-21-65-35-13-9-31(10-14-35)27-57-17-19-58(20-18-57)38-25-37(55-56-44(38)51)36-7-5-6-8-40(36)61/h5-14,23,25,29,34,39,43,60-61H,15-22,24,26-28H2,1-4H3,(H2,51,56)(H,52,62)(H,54,64)/t34-,39+,43-/m1/s1
Molecular weight 935.42 Da
AlogP 0.0
HBond acceptors 16
HBond donors 6
Atoms 125

Vendors

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Expert Reviews


(on 2 Nov 2021 )
Cellular Use Rating
ACBI1 is a well characterized and potent degrader for SMARCA2/4 and PBRM1. Researchers demonstrate proteome selectivity and a target-dependent phenotypic response in multiple AML cell lines. The probe...
(on 2 Nov 2021 )
Cellular Use Rating
This is a well-characterized chemical probe that degrades SMARCA2/4, PBRM1 of the SWI/SNF complex. Based on proteomics data, it does not degrade the other components of the complex. A dose-response (not...
(on 6 Feb 2026 )
Cellular Use Rating
Very good probe and an excellent tool to study the BAF chromatin remodelling complex. Provides details on the reliance of its ATPase domains to form the full complex structure. Meets most criteria for...
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