PROTAC Degrader

Cat. No.

A84559

CAS No.

2762181-19-9

MS83

MS83 is a novel PROTAC that employs a KEAP1 ligand to target and degrade BRD4, along with its homologs BRD3 and BRD2. By harnessing the ubiquitin-proteasome system, MS83 facilitates targeted protein degradation, providing a powerful tool for dissecting the functional roles of BRD4 in cellular processes. This compound is particularly relevant for research on cancer and epigenetic regulation, offering insights into therapeutic strategies that leverage targeted protein degradation.

Cat. No.

A84560

CAS No.

2087490-46-6

ERK-CLIPTAC

ERK-CLIPTAC is a PROTAC molecule designed to selectively induce the degradation of extracellular signal-regulated kinase (ERK). By harnessing the cellular ubiquitin-proteasome system, it offers a novel approach to modulate ERK activity. This compound is valuable for research applications focused on ERK-related signaling pathways and their implications in various diseases, including cancer and neurodegenerative disorders.

Cat. No.

A84561

CAS No.

2363154-39-4

Photo-lenalidomide-acid

Photo-lenalidomide-acid is a photochemical agent designed for use in PHOTACs (photo-controllable PROTACs). This compound consists of an E3 ligase ligand linked to a photoswitch and a ligand specific to a protein of interest, allowing precise optical control of protein degradation. Its innovative mechanism facilitates targeted protein modulation in cellular studies and therapeutic applications, making it a valuable tool for researchers investigating protein dynamics.

Cat. No.

A84562

CAS No.

2244684-50-0

CMP98

CMP98 is a PROTAC designed as a negative control for CM11, targeting the von Hippel-Lindau (VHL) protein. Unlike its active counterparts, CMP98 does not induce degradation of VHL, making it a valuable tool for validating the specificity and efficacy of VHL-dependent degradation studies. This compound can be utilized in research applications involving protein degradation pathways and the exploration of PROTAC mechanisms.

Cat. No.

A84563

CAS No.

2667598-05-0

PROTAC ERα Y537S degrader-1

PROTAC ERα Y537S degrader-1 is designed to selectively target and degrade the estrogen receptor-alpha (ERα) variant Y537S by recruiting an E3 ubiquitin ligase. This molecular tool facilitates the modulation of estrogen signaling pathways, providing a research application in the study of hormone-driven cancers. By utilizing a combination of a linker and a protein-binding domain, it enhances the degradation efficiency of the mutant receptor, enabling insights into the role of ERα Y537S in tumor biology and potential therapeutic strategies.

Cat. No.

A84564

CAS No.

2704616-86-2

PROTAC BRD9 Degrader-5

PROTAC BRD9 Degrader-5 is a proteolysis-targeting chimera (PROTAC) that facilitates the targeted degradation of the bromodomain-containing protein BRD9. This compound employs the cellular ubiquitin-proteasome pathway to promote the selective elimination of BRD9, leading to the modulation of biological pathways associated with cancer and other diseases. It serves as a valuable tool for researchers investigating the role of BRD9 in various cellular processes and therapeutic interventions.

Cat. No.

A84565

CAS No.

2229856-58-8

CCT367766

CCT367766 is a third-generation heterobifunctional PROTAC designed to target and degrade the pirin protein through the CRBN-DDB1 complex. This compound effectively reduces pirin expression at low concentrations, demonstrating an IC50 of 490 nM. It exhibits high binding affinities for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. CCT367766 serves as a valuable chemical tool for probing the biological functions of pirin and advancing research in proteolysis-targeting chimeras.

Cat. No.

A84566

CAS No.

3033545-34-2

phoBET1

phoBET1 is a photocaged-PROTAC targeting BRD4 for selective degradation. This compound harnesses light-activated control to induce the degradation of BRD4 protein, resulting in significant suppression of tumor growth. Its unique photocaging mechanism allows for spatial and temporal regulation of protein activity, making it a valuable tool for studying the role of BRD4 in cancer biology and therapeutic applications.

Cat. No.

A84567

CAS No.

2953426-48-5

PROTAC TTK degrader-2

PROTAC TTK degrader-2 is a potent degrader that targets threonine tyrosine kinase (TTK), demonstrating DC50 values of 3.1 nM in COLO-205 cells and 12.4 nM in HCT-116 cells. This compound effectively induces target protein degradation and exhibits anticancer activity in a xenograft mouse model of human colorectal cancer derived from COLO-205 cells. It serves as a valuable tool for investigating TTK's role in cancer biology and may aid in the development of novel therapeutic strategies.

Cat. No.

A84568

CAS No.

3094092-93-7

SIAIS630121-NC

SIAIS630121-NC is a negative control compound designed for use alongside the NAMPT (nicotinamide phosphoribosyltransferase) PROTAC degrader SIAIS630121. This compound demonstrates no degradation activity on NAMPT, serving as a baseline reference for experimental validation. SIAIS630121-NC is essential for researchers studying the effects of NAMPT degradation and the role of PROTAC technology in targeted protein modulation.

Cat. No.

A84569

CAS No.

2568273-85-6

SMARCA2 degrader-20

SMARCA2 degrader-20 is a potent PROTAC that targets the SMARCA2 protein for degradation, exhibiting a DC50 of less than 100 nM in A549 cells. This degrader is valuable for studying the functional consequences of SMARCA2 depletion in cancer biology and epigenetic regulation. Its high efficacy facilitates research into targeted protein degradation strategies and their therapeutic potential in oncology.

Cat. No.

A84570

CAS No.

2229711-08-2

(Rac)-Vepdegestrant

Synonyms: (Rac)-ARV-471

(Rac)-Vepdegestrant targets the estrogen receptor (ER) as a PROTAC (proteolysis-targeting chimera) degrader, effectively inducing the proteasomal degradation of estrogen receptors in breast cancer cells. This hetero-bifunctional compound enhances the interaction between ER-alpha and an E3 ligase complex, resulting in significant ubiquitylation. (Rac)-Vepdegestrant exhibits potent biological activity, showcasing a half-maximal degradation concentration (DC50) of approximately 2 nM in ER-positive breast cancer cell lines, making it a valuable tool for studying ER-related signaling pathways and potential therapeutic applications in breast cancer research.

Cat. No.

A84571

CAS No.

2633631-78-2

PROTAC BRD9 Degrader-2

PROTAC BRD9 Degrader-2 is a bifunctional degrader that targets the BRD9 protein utilizing the PROTAC mechanism. This compound facilitates the targeted ubiquitination and subsequent degradation of BRD9, thus significantly influencing cancer-related pathways. It is instrumental in cancer research, particularly in studies aimed at understanding the role of BRD9 in tumorigenesis and developing potential therapeutic strategies.

Cat. No.

A84572

CAS No.

2568276-43-5

PROTAC SMARCA2 degrader-17

PROTAC SMARCA2 degrader-17 (compound I-290) is a potent PROTAC degrader designed to selectively target and degrade the SMARCA2 protein. It demonstrates effective degradation in A549 cells with a DC50 value of less than 100 nM and achieves a maximum degradation rate exceeding 90% after 24 hours of treatment. This reagent is valuable for research in cancer biology and the investigation of SMARCA2-related pathways.

Cat. No.

A84573

CAS No.

2568276-37-7

PROTAC SMARCA2 degrader-16

PROTAC SMARCA2 degrader-16 (compound I-278) is a PROTAC designed to selectively degrade the SMARCA2 protein. It demonstrates significant biological activity by efficiently reducing SMARCA2 levels in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is invaluable for research applications involving the modulation of SMARCA2 in cancer biology and therapeutic development.

Cat. No.

A84574

CAS No.

2770571-17-8

PROTAC SMARCA2 degrader-25

PROTAC SMARCA2 degrader-25 is a potent heterobifunctional molecule that targets SMARCA2 for degradation via the proteasome pathway. With a DC50 value of less than 0.01 μM, this compound efficiently engages the target protein using a specific ligand, a link to facilitate the interaction, and an E3 ligase ligand to promote ubiquitination. Its high efficiency makes it a valuable tool in investigating the role of SMARCA2 in various biological processes and diseases.

Cat. No.

A84575

CAS No.

2568273-79-8

PROTAC SMARCA2/4-degrader-32

PROTAC SMARCA2/4-degrader-32 is a PROTAC degrader that targets SMARCA2 and SMARCA4 proteins. It demonstrates effective degradation of these proteins in A549 cells, achieving DC50 values below 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is suitable for research applications focusing on the regulation of chromatin remodeling and its implications in various cancers.

Cat. No.

A84577

CAS No.

2568273-64-1

PROTAC SMARCA2/4-degrader-16

PROTAC SMARCA2/4-degrader-16 (compound I-337) is a potent PROTAC degrader designed to selectively target and degrade SMARCA2 and SMARCA4 proteins. It demonstrates significant biological activity in A549 cells, achieving DC50 values of less than 100 nM and over 90% maximum degradation rate (Dmax%) after 24 hours of treatment. This compound is valuable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in tumor biology and for exploring targeted protein degradation strategies.

Cat. No.

A84579

CAS No.

3025533-68-7

PROTAC ERα Degrader-8

PROTAC ERα Degrader-8 is a highly potent degrader of estrogen receptor alpha (ERα), demonstrating a DC50 value of 6 nM in MCF7 breast cancer cells. This compound harnesses the proteolysis-targeting chimera (PROTAC) technology to selectively induce the degradation of ERα, facilitating studies on estrogen signaling pathways and potential therapeutic interventions in hormone-driven cancers. Its application in research provides insight into targeting ERα-related pathways for cancer treatment strategies.

Cat. No.

A84580

CAS No.

3019907-96-8

F1-RIBOTAC

F1-RIBOTAC is a ribonuclease-targeting chimera (RIBOTAC) that functions by enhancing the activity of RNase L to selectively degrade QSOX1-a mRNA. This targeted approach results in a significant reduction in QSOX1-a expression, making F1-RIBOTAC a valuable tool for cancer research. Its design integrates RNA ligands and RNase L ligands, providing a novel modality for studying RNA degradation pathways in malignant cells.

Cat. No.

A84581

CAS No.

2568277-42-7

PROTAC SMARCA2 degrader-12

PROTAC SMARCA2 degrader-12 is a molecule specifically designed to induce degradation of the SMARCA2 protein. This PROTAC exhibits potent biological activity, effectively degrading SMARCA2 proteins in A549 cells with a DC50 value of less than 100 nM and achieving over 90% maximum degradation after 24 hours of treatment. This reagent is suitable for research applications focusing on targeted protein degradation and the functional analysis of SMARCA2 in cancer biology.

Cat. No.

A84582

CAS No.

2421260-43-5

PROTAC ERα Degrader-10

PROTAC ERα Degrader-10 (Compound 160a) is a potent degrader targeting estrogen receptor alpha (ERα) with a DC50 of 0.37-1.1 nM in cell lines such as MCF7, T47D, and CAMA-1. This compound effectively induces degradation of ERα, demonstrating significant antitumor activity in mouse models. It is a valuable tool for investigating ERα-related signaling pathways and exploring therapeutic strategies for ERα-positive breast cancers.

Cat. No.

A84585

CAS No.

2760703-21-5

TD-802

TD-802 is an androgen receptor (AR) PROTAC degrader that demonstrates substantial microsomal stability. It exhibits notable antitumor efficacy in vivo, making it a valuable tool for investigating metastatic castration-resistant prostate cancer. This compound is essential for research aimed at understanding AR modulation and its impacts on cancer progression.

Cat. No.

A84586

CAS No.

2933253-85-9

PROTAC SMARCA2/4-degrader-35

PROTAC SMARCA2/4-degrader-35 is an efficient degrader targeting the SMARCA2 and SMARCA4 proteins, demonstrating a DC50 of less than 2.5 nM. This compound promotes the ubiquitination and subsequent degradation of the target proteins via the recruitment of E3 ligases. Its potent biological activity makes it valuable for research applications focused on epigenetics and cancer biology, particularly in studies targeting the modulation of chromatin remodeling complexes.

Cat. No.

A84588

CAS No.

2568276-73-1

PROTAC SMARCA2 degrader-14

PROTAC SMARCA2 degrader-14 is a targeted protein degradation compound designed to selectively degrade the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, it achieves maximum degradation rates exceeding 90% in A549 cells following a 24-hour treatment. This reagent serves as a valuable tool for research applications focused on elucidating the role of SMARCA2 in various biological processes and therapeutic contexts.