PROTAC Degrader

Cat. No.

A40380

CAS No.

2257497-15-5

PROTAC BRD3 degrader-1

PROTAC BRD3 Degrader-1 is a potent and selective proteolysis-targeting chimera (PROTAC) designed to degrade BRD3. Its mechanism involves the targeted degradation of BRD3, leading to the downregulation of H3K18ac while sparing BRD2 and BRD4. This compound demonstrates significant efficacy in reducing intraocular inflammation in the experimental autoimmune uveitis mouse model and inhibits pro-inflammatory responses in microglial cells, making it a valuable tool for uveitis research.

Cat. No.

A40386

CAS No.

2891464-61-0

PROTAC SMARCA2 degrader-21

PROTAC SMARCA2 degrader-21 is a targeted protein degradation compound that selectively degrades the SMARCA2 protein through the ubiquitin-proteasome system. It demonstrates potent biological activity with a DC50 value of 10-50 nM in A549 cells and exhibits even greater efficacy in MV411 cells, achieving a DC50 of less than 1 nM for SMARCA2 while showing limited degradation of SMARCA4 (DC50 >100 nM). This compound is useful for investigating the functional roles of SMARCA2 in cancer biology and therapeutic development.

Cat. No.

A40390

CAS No.

2270875-93-7

SMARCA2-IN-8

SMARCA2-IN-8 is a selective inhibitor of the SWI/SNF chromatin remodeling complexes SMARCA2 and SMARCA4, exhibiting potent activity with IC50 values of 5 nM and 6 nM, respectively. This compound effectively inhibits the proliferation of SMARCA2-mutated cancer cells, specifically SKMEL5, with an AAC50 of 5 nM and downregulates SMARCA2-dependent KRT80 gene expression at an AAC50 of 10 nM. SMARCA2-IN-8 demonstrates substantial antitumor efficacy and favorable pharmacokinetic properties in preclinical mouse models, making it a valuable tool for investigating chromatin remodeling in cancer research.

Cat. No.

A40391

CAS No.

3055207-38-7

BRD4 degrader-6

BRD4 degrader-6 is a dimeric PROTAC degrader targeting the BRD4 protein, demonstrating a DC50 of less than 0.1 μM. This compound facilitates the ubiquitination and subsequent degradation of BRD4, contributing to its anticancer properties. It serves as a valuable tool for studying BRD4-related pathways and potential therapeutic strategies in cancer research.

Cat. No.

A40392

CAS No.

2568277-87-0

PROTAC SMARCA2/4-degrader-6

PROTAC SMARCA2/4-degrader-6, a targeted degrader of SMARCA2 and SMARCA4, employs a proteolysis-targeting chimeric approach to facilitate the degradation of these proteins. This compound demonstrates significant potential in cancer research by selectively lowering SMARCA2/4 levels, thereby disrupting oncogenic signaling pathways. Its unique structure includes a ligand for SMARCA2/4 and a VHL ligand to promote ubiquitination and subsequent proteasomal degradation, making it a valuable tool for elucidating the role of these proteins in tumor biology.

Cat. No.

A40395

CAS No.

2570470-42-5

PROTAC BRD2/BRD4 degrader-1

PROTAC BRD2/BRD4 degrader-1 is an effective PROTAC targeting the BET proteins BRD4 and BRD2 with high selectivity. This compound facilitates the rapid and reversible degradation of BRD4 and BRD2, while sparing BRD3, making it a powerful tool for research into solid tumors. Its composition includes a BET inhibitor, a linker, and thalidomide, which targets cereblon (CRBN) and cullin 4A. This degrader demonstrates potential in cancer therapeutics with a minimal cytotoxic effect on cells.

Cat. No.

A40399

CAS No.

3050690-26-8

BRD-SF2

BRD-SF2 is a BRD4-targeted PROTAC degrader that facilitates the selective degradation of the BRD4 protein. With a DC50 of 17.2 μM, it utilizes a VHL ligand and a specific linker to induce proteasomal degradation. This compound is valuable for research applications in cancer biology and epigenetics, providing insights into the role of BRD4 in transcriptional regulation and cellular processes.

Cat. No.

A40404

CAS No.

3033588-00-7

PROTAC SMARCA2/4 degrader-36

PROTAC SMARCA2/4 degrader-36 is a selective dual degrader targeting SMARCA2 and SMARCA4, demonstrating DC50 values of 0.22 nM and 0.85 nM, respectively. This compound exhibits significant anti-cell proliferation activity, making it a valuable tool for research in cancer biology and epigenetic regulation. It employs a unique mechanism of action involving targeted protein degradation, which can provide insights into the functional roles of SMARCA2 and SMARCA4 in various cellular processes.

Cat. No.

A40410

CAS No.

2568276-88-8

PROTAC SMARCA2/4-degrader-17

PROTAC SMARCA2/4-degrader-17 is an innovative PROTAC degrader designed to target the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF chromatin remodeling complex. This compound effectively induces the degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, exhibiting DC50 values of less than 100 nM for both targets. It presents a valuable tool for research studies focused on the modulation of chromatin dynamics and cancer biology.

Cat. No.

A40412

CAS No.

3099581-74-2

PROTAC SMARCA2/4 degrader-39

PROTAC SMARCA2/4 degrader-39 is a selective degrader that targets the SMARCA2 (BRM) and SMARCA4 (BRG1) proteins through the PROTAC mechanism. This compound exhibits significant efficacy in promoting the degradation of these chromatin remodeling proteins, which is crucial in various oncological contexts, particularly non-small cell lung cancer and colorectal cancer. Researchers may find this degrader valuable for studying the molecular mechanisms underlying tumor growth and developing innovative therapeutic strategies.

Cat. No.

A40415

CAS No.

2189497-60-5

EN884

EN884 is a selective degrader of BRD4, functioning through a SKP1- and proteasome-dependent mechanism. This compound facilitates targeted protein degradation and is applicable in synthetic proteolysis targeting chimeras (PROTACs) research. EN884 is valuable for investigating the role of BRD4 in various biological processes and disease contexts.

Cat. No.

A40416

CAS No.

2568273-82-3

PROTAC SMARCA2/4-degrader-29

PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a selective degrader aimed at the catalytic subunits of the SWI/SNF chromatin remodeling complexes, SMARCA2 and SMARCA4. This compound effectively induces the degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, achieving a degradation concentration (DC50) of less than 100 nM for both targets. It is designed for use in research focused on chromatin regulation, epigenetic modifications, and related therapeutic applications.

Cat. No.

A40423

CAS No.

2375455-53-9

RAJQ14

RAJQ14 is a PROTAC degrader that selectively targets BRD4, facilitating its degradation through the ubiquitination-independent pathway. By binding to the 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14, RAJQ14 recruits BRD4 to the proteasome, promoting proteolytic degradation. This compound is an invaluable tool for cancer research, enabling studies of the mechanisms underlying BRD4 modulation and its role in tumor biology.

Cat. No.

A40425

CAS No.

2641510-88-3

PROTAC SMARCA2 degrader-28

PROTAC SMARCA2 degrader-28 is a selective PROTAC agent that targets SMARCA2, effectively inducing its degradation with a DC50 of 3 nM in HiBiT A549 cells. This compound utilizes a bifunctional mechanism, linking a ligand for SMARCA2 with an E3 ligase ligand, facilitating targeted protein degradation. It serves as a potent tool for research applications aimed at studying SMARCA2's role in cellular processes and its potential implications in cancer therapeutics.

Cat. No.

A40431

CAS No.

3031540-97-0

EBET-1593

EBET-1593 is a selective BET PROTAC degrader that facilitates the ubiquitination and subsequent degradation of BET proteins. This compound serves as a lead payload for the synthesis of antibody-drug conjugates (ADCs), such as 84-EBET, which exhibits anti-tumor activity against pancreatic ductal adenocarcinoma. EBET-1593 is integral for research in targeted protein degradation and therapeutic strategies in oncology.

Cat. No.

A40432

CAS No.

2568277-57-4

PROTAC SMARCA2/4-degrader-19

PROTAC SMARCA2/4-degrader-19 is designed to target the catalytic subunits of the SWI/SNF complex, specifically SMARCA2 and SMARCA4. This potent degrader effectively leads to the degradation of SMARCA2 in MV411 and A549 cells with a DC50 of less than 100 nM, as well as SMARCA4 in MV411 with a similar DC50. It serves as a valuable tool for researching the functional roles of these proteins in cancer biology and therapeutic development.

Cat. No.

A40437

CAS No.

3104449-57-9

dBAZ2

dBAZ2 is a novel PROTAC degrader targeting BAZ2A and BAZ2B, demonstrating DC50 values of 180 nM and 250 nM, respectively. This compound facilitates the ubiquitination and subsequent proteasomal degradation of BAZ2A and BAZ2B, making it a valuable tool for studying their biological roles. dBAZ2 is suitable for research applications in cancer biology, epigenetics, and the exploration of targeted protein degradation mechanisms.

Cat. No.

A40439

CAS No.

2571123-81-2

AR/BET protein degrader-1

AR/BET protein degrader-1 is a PROTAC designed to selectively target and degrade both the Androgen Receptor (AR) and BET proteins. This compound exhibits potent biological activity in modulating protein levels, making it a valuable tool for cancer research. It facilitates novel therapeutic strategies aimed at overcoming resistance mechanisms, thereby enhancing the understanding of cancer biology and treatment options.

Cat. No.

A40444

CAS No.

2760247-27-4

PROTAC SMARCA2 degrader-26

PROTAC SMARCA2 degrader-26 is a specific degrader targeting the SMARCA2 protein. This compound exhibits potent activity, inducing a degradation of 94% for SMARCA2 and 57% for SMARCA4 in VCaP cells. Additionally, PROTAC SMARCA2 degrader-26 demonstrates significant antiproliferative effects, making it a valuable tool for research applications aimed at investigating the roles of SMARCA proteins in cancer and other diseases.

Cat. No.

A40446

CAS No.

2568055-24-1

SMARCA2-IN-2

SMARCA2-IN-2 is a specific inhibitor of SMARCA2, demonstrating an IC50 range of 101-500 µM. This compound is relevant for investigations into cancer biology, as it provides insights into the role of SMARCA2 in tumorigenesis. Its ability to selectively modulate SMARCA2 activity makes it a valuable tool for understanding epigenetic regulation in cancer research.

Cat. No.

A40447

CAS No.

2568273-83-4

PROTAC SMARCA2/4-degrader-31

PROTAC SMARCA2/4-degrader-31 is a targeted degradative agent designed to induce proteolytic degradation of the catalytic subunits SMARCA2 and SMARCA4 within the SWI/SNF chromatin remodeling complex. This compound demonstrates effective degradation of SMARCA2 in A549 cells with a DC50 of less than 100 nM and SMARCA4 in MV411 cells, also with a DC50 below 100 nM. It is a valuable tool for studying the functional roles of these proteins in cancer biology and epigenetic regulation.

Cat. No.

A40452

CAS No.

2567913-00-0

PROTAC SMARCA2 degrader-19

PROTAC SMARCA2 degrader-19 is a targeted protein degradative compound designed to degrade the SMARCA2 protein via a PROTAC mechanism. It demonstrates significant efficacy in A549 and MV411 cell lines with a DC50 of less than 100 nM. Additionally, this compound exhibits a reduced degradation effect on SMARCA4 in MV411 cells, with a DC50 exceeding 1000 nM. This specificity makes PROTAC SMARCA2 degrader-19 a valuable tool for studying the biological roles of SMARCA2 and its potential implications in cancer research.

Cat. No.

A40454

CAS No.

2660324-41-2

PROTAC SMARCA2 degrader-20

PROTAC SMARCA2 degrader-20 (Compound I-40) is an innovative PROTAC molecule designed to selectively target and degrade the SMARCA2 protein. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, offering a unique approach to modulate its biological activity. It is primarily utilized in cancer research to explore novel therapeutic pathways and to investigate the role of SMARCA2 in tumorigenesis and other related mechanisms.

Cat. No.

A40456

CAS No.

2417369-73-2

cBu-Cit-GAL-02-221

Synonyms: cBu-Cit-PROTAC BRD4 Degrader-5

cBu-Cit-GAL-02-221 is a PROTAC-linker conjugate designed to facilitate the degradation of BRD4 through its association with cBu-Cit. This compound effectively inhibits BRD4 activity in both HER2-positive and HER2-negative breast cancer cell lines, making it a valuable tool for cancer research. Additionally, cBu-Cit-GAL-02-221 features a single bond, allowing for conjugation with antibody-drug conjugates (ADCs) to create a potent pharmacological agent.

Cat. No.

A40457

CAS No.

2407163-44-2

PROTAC BRD4 Degrader-27

PROTAC BRD4 Degrader-27 is a PROTAC compound that selectively degrades BRD4 by recruiting E3 ubiquitin ligases, while minimizing effects on BRD2 and BRD3. This agent has demonstrated the ability to inhibit KLF5 transcription factor expression and exhibit anti-cancer activity. The compound consists of a Thalidomide-derived E3 ubiquitinase ligand, a γ-Aminobutyric acid linker, and a BRD4-targeting ligand, enabling effective degradation of the target protein in cellular models. Research applications include exploration of BRD4's role in cancer progression and therapeutic intervention strategies.