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

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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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
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
Notes: In the negative control compound, cis-ACBI1, the hydroxy proline of the VHL binding part is in the inactive cis-conformation, which prevents binding to VHL and thereby protein degradation. This prevents binding to VHL, formation of a triple complex and thereby protein degradation. This compound is useful to differentiate phenotypic effects not caused by protein degradation in comparison with its active trans isomer ACBI1. Furthermore, the difference between binding to the bromodomain of SMARCA2 and SMARCA4 and its degradation can be studied in vitro.

Orthogonal Probes def

PFI-3
SGC-SMARCA-BRDVIII
GNE-064

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 5.254320000000003
HBond acceptors 16
HBond donors 6
Atoms 125

Vendors

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Expert Reviews

by SERP
(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...
by SERP
(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...
by SERP+
(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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