The probe and control may be requested here.
A collaboration between the Drug Discovery Program at the Ontario Institute for Cancer Research (OICR) and the Structural Genomics Consortium (SGC) has resulted in the discovery of OICR-41103, a chemical probe for DCAF1 (DDB1-Cul4 associated factor 1).
OICR-41103 binds potently to DCAF1-WDR with a KD value of 2 nM (SPR). In a nanoBRET assay, OICR-41103 displaces a tracer (chemically based on a literature molecule) from DCAF1-WDR with EC50/EC90 values of 130 and 700 nM, respectively.
| Probe | Negative control | |
 |  | |
OICR-41103 |
| OICR-41103N |
Probe publication:
OICR-41103 as a chemical probe for the DCAF1 WD40 domain
Serah W Kimani, Mahmoud Noureldin, Brian Wilson, Laurent Hoffer, Stuart R Green, Magdalena M Szewczyk, Héctor González-Álvarez, Mohammed Mohammed, Manuel Chan, Chiara Krausser, Alice Shi Ming Li, Taraneh Hajian, Sarah Tucker, Dhananjay Joshi, Punit Saraon, Brigitte Thériault, Ji Sup Kim, Vijayaratnam Santhakumar, Peter Loppnau, Yanjun Li, Almagul Seitova, Aiping Dong, Taira Kiyota, Tobias Hammann , Paul Gehrtz, Bhashant Patel, Vaibhavi Rathod, Anand Vala, Bhimsen Rout, Paras Jagodra, Peter J Brown , Ahmed Aman, Jailall Ramnauth, Gennady Poda , David Uehling , Cheryl H Arrowsmith, Dalia Barsyte-Lovejoy, Richard Marcellus, Suzanne Ackloo, Ahmed Mamai, Rima Al-Awar , Levon Halabelian
https://pubmed.ncbi.nlm.nih.gov/40683980/
Related publications:
Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity
https://pubmed.ncbi.nlm.nih.gov/39580491/
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins.
Ackloo S, Li F, Szewczyk M, Seitova A, Loppnau P, Zeng H, Xu J, Ahmad S, Arnautova YA, Baghaie AJ, Beldar S, Bolotokova A, Centrella PA, Chau I, Clark MA, Cuozzo JW, Dehghani-Tafti S, Disch JS, Dong A, Dumas A, Feng JA, Ghiabi P, Gibson E, Gilmer J, Goldman B, Green SR, Guié MA, Guilinger JP, Harms N, Herasymenko O, Houliston S, Hutchinson A, Kearnes S, Keefe AD, Kimani SW, Kramer T, Kutera M, Kwak HA, Lento C, Li Y, Liu J, Loup J, Machado RAC, Mulhern CJ, Perveen S, Righetto GL, Riley P, Shrestha S, Sigel EA, Silva M, Sintchak MD, Slakman BL, Taylor RD, Thompson J, Torng W, Underkoffler C, von Rechenberg M, Walsh RT, Watson I, Wilson DJ, Wolf E, Yadav M, Yazdi AK, Zhang J, Zhang Y, Santhakumar V, Edwards AM, Barsyte-Lovejoy D, Schapira M, Brown PJ, Halabelian L, Arrowsmith CH.
https://www.rcsb.org/structure/9D4E
This week, in honor of National Postdoc Appreciation Week, we are excited to spotlight the incredible contributions of the Structural Genomics Consortium (SGC) postdoctoral researchers across all our research sites. These talented individuals are the engine driving forward innovative, open-access research in previously unexplored areas of biology.