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PROTAC Degrader

PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.

Cat. No.

A84589

CAS No.

3104316-26-6

Chlorohexane-PEG-clozapine

Chlorohexane-PEG-clozapine is a HaloTag PROTAC degrader that employs clozapine to selectively target and promote the degradation of HaloTag fusion proteins. It effectively reduces luminescence intensity and decreases the protein levels of Halo-Eluc, facilitating the study of target protein dynamics and function. This reagent is valuable for research applications focusing on targeted protein degradation and modulation of protein levels in cellular systems.

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Cat. No.

A84590

CAS No.

3057446-82-6

KL-465

KL-465 is a PROTAC degrader designed to target and degrade MAGE-A3, exhibiting a DC50 of 2 μM in HeLa cells. This compound effectively inhibits the viability of MAGE-A3 positive cancer cell lines, including HCT116, A375, and HeLa, making it a valuable tool for cancer research. Its unique mechanism facilitates targeted protein degradation, offering potential insights into therapeutic interventions for tumors expressing MAGE-A3.

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5 mg

$550.00

10 mg

$970.00

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Cat. No.

A84592

CAS No.

2892523-74-7

PROTAC SMARCA2/4 degrader-41

PROTAC SMARCA2/4 degrader-41 is a potent degrader targeting the SMARCA2 and SMARCA4 proteins, exhibiting DC50 and IC50 values both below 0.1 μM. This compound facilitates the selective degradation of these ATP-dependent chromatin remodelers, making it a valuable tool for studying SMARCA2/4-related or SMARCA2/4-deficient cancers. Its application in cancer research can aid in elucidating the role of these proteins in tumorigenesis and therapeutic resistance.

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Cat. No.

A84593

CAS No.

3061366-76-2

PROTAC DYRK2 degrader 1

PROTAC DYRK2 degrader 1 is a selective degrader targeting DYRK2, functioning through the ubiquitin-proteasome system. It exhibits DC50 values of 1.607 μM in MDA-MB-231 cells and 3.265 μM in HeLa cells, effectively inducing DYRK2 degradation. This compound is valuable for research focused on triple-negative breast cancer and cervical cancer, facilitating the exploration of targeted protein degradation mechanisms in these malignancies.

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Cat. No.

A84594

CAS No.

3025781-93-2

PROTAC ERα Degrader-7

PROTAC ERα Degrader-7 is a highly effective degradative compound specifically targeting estrogen receptor alpha (ERα). It operates through a PROTAC mechanism and exhibits a DC50 value of 0.000006 µM, demonstrating its potent biological activity. This compound features a cereblon-binding moiety and an ERα-binding ligand, characterized by a benzofused partially saturated six-membered carbocyclic or heterocyclic ring structure. PROTAC ERα Degrader-7 is valuable for research applications focused on hormone signaling and therapeutic strategies in hormone-responsive cancers.

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Cat. No.

A84595

CAS No.

2769735-56-8

Folate-MS432

Folate-MS432 selectively targets MEKs through a PROTAC mechanism, facilitating their degradation in a folate receptor-dependent manner. This compound demonstrates significant efficacy in cancer cells, providing a powerful tool for investigating the role of MEK degradation in tumor biology. Folate-MS432 is valuable for research applications focusing on therapeutic strategies that manipulate signaling pathways in cancer treatment.

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Cat. No.

A84596

CAS No.

3031840-37-3

NEP168

NEP168 is a potent ERα PROTAC degrader that utilizes the GID4 E3 ligase for targeted protein degradation. This compound effectively reduces ERα levels, offering valuable insights into estrogen receptor-related signaling pathways. NEP168 serves as a crucial tool for investigating breast cancer biology and may aid in the development of novel therapeutic strategies.

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Cat. No.

A84597

CAS No.

2568277-89-2

PROTAC SMARCA2/4-degrader-7

PROTAC SMARCA2/4-degrader-7 is a selective protein degrader that targets SMARCA2 and SMARCA4 proteins. Demonstrating effective degradation in A549 cells, it achieves DC50 values of less than 100 nM and results in more than 90% degradation after 24 hours of treatment. This compound serves as a valuable tool for investigating the roles of SMARCA2 and SMARCA4 in cancer biology and other research applications involving epigenetic regulation.

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Cat. No.

A84598

CAS No.

2568277-48-3

PROTAC SMARCA2/4-degrader-22

PROTAC SMARCA2/4-degrader-22 is a targeted protein degradation reagent designed to selectively degrade SMARCA2 and SMARCA4 proteins. This compound effectively reduces SMARCA2 and SMARCA4 levels in A549 cells, achieving DC50 values of less than 100 nM and exceeding 90% maximum degradation rate after 24 hours of treatment. It is a valuable tool for research into the role of these proteins in various biological processes and disease states.

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Cat. No.

A84599

CAS No.

2408832-28-8

Arg-TERRα

Arg-TERRα is a mini-PROTAC designed to target estrogen-related receptor alpha (ERRα). This compound facilitates the degradation of ERRα via the N-end rule pathway, effectively suppressing the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα serves as a valuable tool for investigating the role of ERRα in breast cancer research and therapeutic development.

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Cat. No.

A84600

CAS No.

2633632-05-8

PROTAC BRD9 Degrader-3

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9 through the PROTAC mechanism, facilitating targeted protein degradation. This compound exhibits potent biological activity by selectively degrading BRD9, which plays a critical role in various cancer pathways. It is intended for use in cancer research to elucidate the functional significance of BRD9 and to explore novel therapeutic strategies in oncology.

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Cat. No.

A84601

CAS No.

2858738-65-3

ITK degrader 2

ITK Degrader 2 is a PROTAC-based compound that specifically targets and degrades the interleukin-2-inducible T-cell kinase (ITK) with a DC50 value of less than 10 nM. In pharmacokinetic studies in mice, this orally active degrader demonstrates a maximum concentration (Cmax) of 0.87 μM and achieves peak plasma levels (Tmax) at 2 hours post-administration. At a dosage of 90 mg/kg, ITK Degrader 2 effectively reduces ITK levels by 20% within 6 hours, making it a valuable tool for exploring ITK-related signaling pathways and their implications in immune responses.

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Cat. No.

A84602

CAS No.

3081180-48-2

PROTAC BRD9 Degrader-8

PROTAC BRD9 Degrader-8 is a selective BRD9 PROTAC degrader that operates through targeted protein degradation, exhibiting a DC50 of 16 pM. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis, making it a valuable tool for studies focused on acute myeloid leukemia and diffuse large B-cell lymphoma. Its mechanism provides a unique approach to modulating BRD9 levels in therapeutic research.

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Cat. No.

A84603

CAS No.

2568276-71-9

PROTAC SMARCA2/4-degrader-11

PROTAC SMARCA2/4-degrader-11 is a targeted protein degradation tool that specifically promotes the degradation of the SMARCA family of proteins. With a DC50 value of less than 100 nM, this compound effectively induces the destruction of SMARCA2 and SMARCA4. Its unique design features an inhibitor component, a linker, and an E3 ligase ligand, facilitating the targeted removal of these proteins, making it a valuable reagent for research into cancer biology and epigenetic regulation.

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Cat. No.

A84604

CAS No.

2568276-78-6

PROTAC SMARCA2 degrader-15

PROTAC SMARCA2 degrader-15 is a targeted PROTAC that selectively degrades the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, this compound achieves over 90% maximum degradation (Dmax%) within 24 hours in A549 cells. Its ability to modulate SMARCA2 levels makes it a valuable tool for research exploring the role of this protein in cancer biology and epigenetic regulation.

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Cat. No.

A84605

CAS No.

3032848-64-6

BT-PROTAC

BT-PROTAC is a proteolysis targeting chimera (PROTAC) that enables the targeted degradation of specific proteins through a bioorthogonal activation mechanism. By accurately controlling PROTAC activity, it facilitates the selective modulation of protein levels within cells. This compound is valuable for research applications focused on the study of protein function, cellular signaling pathways, and the development of targeted therapeutic strategies.

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Cat. No.

A84606

CAS No.

2682255-44-1

A031

A031 is a potent PROTAC degrader targeting the androgen receptor (AR), demonstrating an IC50 value of less than 0.25 μM for effective AR protein degradation. This compound has shown a significant inhibitory effect on tumor growth in zebrafish models of human prostate cancer (VCaP). A031 is a valuable tool for investigating AR-mediated signaling pathways and potential therapeutic strategies in prostate cancer research.

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Cat. No.

A84607

CAS No.

2715104-46-2

PROTAC HMGCR Degrader-2

PROTAC HMGCR Degrader-2 selectively targets HMG-CoA reductase (HMGCR) for degradation through the VHL-dependent ubiquitin-proteasome system, exhibiting an IC50 value of 0.25 μM and a DC50 of 0.12 μM in Insig-silenced HepG2 cells. This compound effectively reduces cellular cholesterol levels, making it valuable for research related to hyperlipidemia. Its mechanism of action enables precise modulation of cholesterol biosynthesis pathways, providing insights into lipid metabolism and potential therapeutic interventions.

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Cat. No.

A84608

CAS No.

2568277-50-7

PROTAC SMARCA2/4-degrader-23

PROTAC SMARCA2/4-degrader-23 is a targeted proteolysis-targeting chimera (PROTAC) designed to degrade SMARCA2 and SMARCA4 proteins. This compound effectively induces degradation of both targets in A549 cells, exhibiting a DC50 of less than 100 nM and achieving a maximum degradation rate exceeding 90% after 24 hours of treatment. It is suitable for use in studies aimed at understanding the functional roles of SWI/SNF chromatin remodeling complexes in cancer and other disease models.

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Cat. No.

A84609

CAS No.

2568279-34-3

PROTAC SMARCA2 degrader-10

PROTAC SMARCA2 degrader-10 is a targeted protein degrader that specifically engages and promotes the degradation of SMARCA2. This compound demonstrates effective degradation of SMARCA2 proteins in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. It serves as a valuable tool for research applications focused on elucidating the biological roles of SMARCA2 and its implications in cancer biology and therapeutics.

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Cat. No.

A84610

CAS No.

2568523-72-6

PROTAC SMARCA2 degrader-6

PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC agent specifically designed to target and induce the degradation of SMARCA2 proteins. This compound effectively degrades SMARCA2 in A549 cells, achieving a DC50 value of less than 100 nM and demonstrating a maximum degradation rate exceeding 90% within 24 hours of treatment. It serves as a powerful tool for investigating the role of SMARCA2 in various biological processes and potential therapeutic applications in cancer research.

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Cat. No.

A84611

CAS No.

2711006-74-3

ZXH-4-137

ZXH-4-137 is a potent and selective CRBN degrader that utilizes the PROTAC mechanism to promote targeted protein degradation. This compound effectively recruits the E3 ubiquitin ligase CRBN to facilitate the degradation of specific proteins, making it a valuable tool for studying protein function and regulation. It has applications in cellular assays and therapeutic research aimed at diseases associated with protein homeostasis.

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25 mg

$1,275.00

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Cat. No.

A84612

CAS No.

3035210-39-7

PROTAC Cbl-b-IN-1

PROTAC Cbl-b-IN-1 is a potent Cbl-b PROTAC degrader, exhibiting a DC50 of less than 30 nM. This compound effectively induces the targeted degradation of the Cbl-b protein, making it a valuable tool for cancer research. Its ability to modulate protein levels through degradation pathways allows for in-depth studies of Cbl-b's role in tumor biology and therapeutic interventions.

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Cat. No.

A84613

CAS No.

3033871-15-4

PROTAC erf3a Degrader-2

PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC designed to target and degrade eRF3a (GSPT1) and SRD5A3 proteins. By inducing the ubiquitination and subsequent proteasomal degradation of these proteins, it effectively inhibits cancer cell proliferation in various models, including the 22Rv1 prostate cancer cell line. PROTAC erf3a Degrader-2 is applicable for research related to multiple cancer types, including prostate, ovarian, liver, cervical, and breast cancers, as well as leukemia.

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Cat. No.

A84614

CAS No.

2568507-10-6

PROTAC SMARCA2/4-degrader-3

PROTAC SMARCA2/4-degrader-3 is a potent SMARCA2/4 degrader that utilizes the VH032-NH2 framework for targeted protein degradation. It exhibits a degradation potency (DC50) of less than 100 nM in MV4-11 cells, facilitating the selective depletion of SMARCA2 and SMARCA4 proteins. This compound is valuable for research applications involving chromatin remodeling and cancer biology, providing insights into the functional roles of these proteins in various cellular contexts.

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