PROTAC Degrader

Cat. No.

A24729

CAS No.

2439058-23-6

HDAC6 degrader-1

HDAC6 degrader-1 is a PROTAC degrader targeting HDAC6, exhibiting a DC50 value of 3.8 nM in MM.1S cells. This compound efficiently induces the degradation of HDAC6 through a bifunctional strategy, linking a ligand for the E3 ligase Pomalidomide with a ligand for the target protein Nexturastat A via a specialized linker. Its application is vital for investigating the role of HDAC6 in cellular processes and potential therapeutic effects in various diseases.

Cat. No.

A24730

CAS No.

2411085-89-5

MG-277

MG-277 is a PROTAC GSPT1 degrader that induces degradation of the translation termination factor GSPT1 via a Cereblon E3 ligase mechanism, with a DC50 of 1.3 nM. This compound exhibits potent anticancer activity, significantly inhibiting tumor cell growth in a p53-independent manner, demonstrating IC50 values of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells. MG-277 is a valuable tool for cancer research, particularly in studies involving protein degradation and cellular mechanisms of tumorigenesis.

Cat. No.

A24732

CAS No.

3004503-12-9

NUCC-0226272

NUCC-0226272 is a potent PROTAC that facilitates the targeted degradation of EZH2. This compound exhibits significant anti-proliferative effects, making it a valuable tool for investigating the role of EZH2 in cancer biology. Its application in cancer research provides insights into potential therapeutic strategies for malignancies associated with EZH2 dysregulation.

Cat. No.

A24733

CAS No.

2951015-29-3

YD23

YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 and H1975 cell lines, respectively. This reagent induces the degradation of SMARCA2, exhibiting synthetic lethality towards SMARCA4-deficient cells and selectively inhibiting growth in SMARCA4 mutant lung cancer cells. YD23 also reduces chromatin accessibility in SMARCA4 deficient cells, impacting genes associated with cell cycle and growth regulation. It is a valuable tool for researching non-small cell lung cancer (NSCLC) and evaluating tumor growth in SMARCA4-mutant xenograft models.

Cat. No.

A24734

CAS No.

2365172-19-4

XZ739

XZ739 is a Cereblon-dependent PROTAC degrader targeting BCL-XL, a member of the Bcl-2 protein family. Demonstrating a DC50 value of 2.5 nM in MOLT-4 cells after 16 hours of treatment, XZ739 effectively induces cell death through caspase-mediated apoptosis. This compound is valuable for research applications focused on studying apoptosis, cancer therapeutics, and the modulation of protein degradation pathways.

Cat. No.

A24735

CAS No.

2384184-40-9

KB02-SLF

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader designed to facilitate targeted protein degradation. It achieves this by covalently modifying DCAF16, an E3 ligase, thereby enhancing the stability of FKBP12 degradation within biological systems. The compound consists of a molecular glue linking the ubiquitin E3 ligase ligand KB02 with SLF, enabling efficient degradation of FKBP12 for various research applications in protein regulation and degradation pathways.

Cat. No.

A24820

CAS No.

3026420-38-9

PROTAC BRD4 Degrader-8

PROTAC BRD4 Degrader-8 is a proteolysis-targeting chimera (PROTAC) that engages both von Hippel-Lindau (VHL) and BRD4, exhibiting IC50 values of 1.1 nM for BRD4 BD1 and 1.4 nM for BRD4 BD2. This compound effectively promotes the degradation of BRD4 protein in PC3 prostate cancer cells, making it a valuable tool for research into BRD4-related signaling pathways and cancer therapeutics. Its high potency highlights its potential use in studying mechanisms of protein regulation and developing novel cancer treatments.

Cat. No.

A24821

CAS No.

2380000-55-3

β-NF-JQ1

β-NF-JQ1 is a PROTAC that targets bromodomain-containing (BRD) proteins by leveraging β-NF as a ligand for the Aryl Hydrocarbon Receptor (AhR) E3 ligase. This compound facilitates the degradation of BRD proteins through the recruitment of AhR, leading to effective protein knockdown. β-NF-JQ1 demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and the development of targeted therapeutic strategies.

Cat. No.

A24822

CAS No.

2832961-58-5

CBPD-268

CBPD-268 is a highly potent CBP/p300 PROTAC degrader, exhibiting a DC50 value of ≤ 0.03 nM. This compound effectively induces degradation of CBP/p300 and demonstrates significant inhibition of cell growth, showcasing its antitumor potential. CBPD-268 is particularly relevant for research into androgen receptor-positive prostate cancer, facilitating studies on novel therapeutic strategies.

Cat. No.

A24824

CAS No.

2451573-87-6

dTAGV-1-NEG

dTAGV-1-NEG is a diastereomer that acts as a heterobifunctional negative control for dTAGV-1, specifically targeted at FKBP12(F36V). This compound is utilized in research to study the selectivity and efficacy of FKBP12(F36V) degraders, helping to elucidate cellular mechanisms and pathways influenced by FKBP12 modulation. Its role as a control reagent makes it essential for validating experimental results in protein degradation studies.

Cat. No.

A24825

CAS No.

2740582-16-3

SHP2-D26 isomer-1

SHP2-D26 isomer-1 is an isoform of the SHP2-D26 degrader, designed specifically for targeted protein degradation applications. This compound does not induce degradation of SHP2 at concentrations ranging from 3 to 1000 nM. As a component of PROTAC technology, SHP2-D26 isomer-1 serves as a valuable tool for studying SHP2's role in signaling pathways and assessing the therapeutic potential of SHP2 modulation in various diseases.

Cat. No.

A24826

CAS No.

2924557-42-4

SNX7886

SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways.

Cat. No.

A24827

CAS No.

2052306-13-3

PROTAC TBK1 degrader-2

PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases.

Cat. No.

A24828

CAS No.

3050872-59-5

MS8847

MS8847 is a powerful EZH2 PROTAC degrader that utilizes the E3 ligase von Hippel-Lindau (VHL) to promote the degradation of EZH2 through the ubiquitin-proteasome system. This compound demonstrates robust anti-proliferative effects in acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cell lines. MS8847 serves as a valuable tool for investigating the role of EZH2 in oncogenic signaling pathways and developing targeted therapies for EZH2-dependent malignancies.

Cat. No.

A24829

CAS No.

2769753-64-0

DB-3-291

DB-3-291 is a potent and selective PROTAC degrader targeting the protein CSK, exhibiting a Kd of 1 nM. This compound facilitates the degradation of CSK through its specific interaction with the E3 ligase, enabling in-depth studies of CSK-related biological pathways and providing insights into potential therapeutic strategies. It is valuable for researchers investigating targeted protein degradation and cancer biology.

Cat. No.

A24830

CAS No.

2984236-79-3

PROTAC KRAS G12C degrader-1

PROTAC KRAS G12C degrader-1 is a Cereblon-based PROTAC targeting the KRAS G12C mutant. This compound promotes the formation of a dimer between Cereblon and KRAS G12C, leading to the degradation of GFP-tagged KRAS G12C in reporter cell systems. It serves as a valuable tool for research on targeted degradation strategies in KRAS-driven cancers.

Cat. No.

A24831

CAS No.

2305936-56-3

TD-165

TD-165 is a PROTAC (proteolysis-targeting chimera) that targets cereblon (CRBN) for selective degradation of proteins. This compound features a CRBN ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group, facilitating targeted ubiquitination and proteolytic degradation of specific proteins involved in cellular processes. TD-165 is suitable for research applications focused on targeted protein degradation, therapeutic development, and elucidating protein function in various biological contexts.

Cat. No.

A24832

CAS No.

2369022-68-2

PROTAC PARP1 degrader

PROTAC PARP1 Degrader functions as a targeted protein degradation agent that specifically targets PARP1 through the MDM2 E3 ligase. This compound effectively induces PARP1 cleavage and promotes apoptosis in cancer cells, making it valuable for research in cancer therapies. The structure includes the MDM2 ligand, the PARP1 ligand, and a PEG-based linker, facilitating efficient delivery and degradation of the target protein.

Cat. No.

A24833

CAS No.

2633632-34-3

PROTAC BRD9 Degrader-4

PROTAC BRD9 Degrader-4 is a bifunctional degrader targeting BRD9 through the proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces degradation of BRD9, thereby altering oncogenic pathways associated with various cancers. This compound is utilized in cancer research to study the therapeutic potential of BRD9 modulation and the implications of targeted degradation in tumor biology.

Cat. No.

A24835

CAS No.

2655656-99-6

Zomiradomide

Synonyms: KT-413

Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses.

Cat. No.

A24836

CAS No.

2353493-69-1

PRO-6E

PRO-6E is a PROTAC that targets Cereblon to induce degradation of the MET protein. It achieves up to 81.9% degradation of MET at 1 μM in MKN-45 cells, effectively inhibiting tumor growth both in vitro and in vivo. Additionally, PRO-6E promotes apoptosis and cell cycle arrest, making it a valuable tool for research on MET-related oncogenic processes.

Cat. No.

A24837

CAS No.

2769753-53-7

DB1113

DB1113 is a bifunctional compound designed for targeted protein degradation of various kinases. It effectively induces degradation of ABL1, ABL2, BLK, CDK4, CDK11B, EPHA3, MAPK7, RIPK1, and others, facilitating the investigation of kinase-related signaling pathways. DB1113 is suitable for research focusing on diseases or disorders associated with dysregulated kinase activity, providing a valuable tool for exploring therapeutic interventions in cancer and other conditions.

Cat. No.

A24838

CAS No.

2451573-90-1

dTAG-13-NEG

dTAG-13-NEG serves as a negative control for dTAG-13, a PROTAC-based bifunctional degrader that selectively targets FKBP12F36V in the presence of a protein of interest. While dTAG-13 promotes the degradation of FKBP12F36V, dTAG-13-NEG allows for the assessment of specificity and background in experimental setups involving this pathway. This compound is essential for validating experimental results when studying protein degradation mechanisms and their implications in cellular biology.

Cat. No.

A24839

CAS No.

3033109-92-8

SMD-3040

SMD-3040 is a selective SMARCA2 PROTAC degrader with a DC50 of 12 nM and a maximal degradation efficiency of 91%. This compound effectively inhibits tumor cell proliferation, demonstrating significant antitumor activity. SMD-3040 is particularly useful in studies related to various tumors, including melanoma.

Cat. No.

A24840

CAS No.

1957234-97-7

PROTAC BET Degrader-10

PROTAC BET Degrader-10 is a selective degrader targeting the BET protein BRD4 through a PROTAC mechanism, featuring a DC50 of 49 nM. This compound utilizes ligands for Cereblon and BRD4, promoting the ubiquitination and subsequent degradation of BRD4. It serves as a valuable tool for investigating the role of BRD4 in various biological processes and cancer-related research applications.