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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.

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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Cat. No.

A84616

CAS No.

2568273-68-5

PROTAC SMARCA2/4-degrader-1

PROTAC SMARCA2/4-degrader-1 is a PROTAC degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively degrades these proteins in A549 cells, exhibiting a DC50 of less than 100 nM and achieving over 90% degradation after 24 hours of treatment. This compound is suitable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in various biological processes and disease models.

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Cat. No.

A84617

CAS No.

2582803-80-1

ND1-YL2

ND1-YL2 is a PROTAC that selectively targets and degrades SRC-1 through the N-degron pathway. This compound has demonstrated significant inhibition of cancer cell invasion and migration both in vitro and in vivo. ND1-YL2 serves as a valuable tool in cancer research, providing insights into the role of SRC-1 in tumor progression and metastasis.

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0.1 mg

$1,050.00

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Cat. No.

A84618

CAS No.

2568277-76-7

PROTAC SMARCA2/4-degrader-2

PROTAC SMARCA2/4-degrader-2 is a molecular degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively induces degradation of these proteins in A549 cell lines with degradation concentrations (DC50s) less than 100 nM, achieving a maximum degradation rate (Dmax%) exceeding 90% after 24 hours of exposure. This compound is valuable for investigating the roles of SMARCA2 and SMARCA4 in various biological processes and may have applications in cancer research and therapeutic development.

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Cat. No.

A84619

CAS No.

2568276-72-0

PROTAC SMARCA2 degrader-13

PROTAC SMARCA2 degrader-13 is a novel PROTAC targeted at the degradation of SMARCA2 proteins. This compound effectively induces the degradation of SMARCA2 in A549 cells with a DC50 of less than 100 nM, achieving over 90% degradation after 24 hours of treatment. It serves as a valuable tool for studying the functional role of SMARCA2 in cancer biology and other cellular processes.

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Cat. No.

A84621

CAS No.

2703021-51-4

PROTAC AR Degrader-5

PROTAC AR Degrader-5 is a potent androgen receptor (AR) PROTAC degrader, exhibiting an IC50 value of 49 nM. This compound facilitates the targeted degradation of AR, demonstrating significant potential in inhibiting sebaceous plaque formation and promoting hair regeneration. Its mechanism utilizes a bifunctional ligand to recruit an E3 ligase, making it a valuable tool for research in androgen signaling and related therapeutic applications.

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Cat. No.

A84623

CAS No.

2568276-36-6

PROTAC SMARCA2/4-degrader-33

PROTAC SMARCA2/4-degrader-33 (compound I-277) is a targeted protein degradation compound that engages and induces degradation of SMARCA2 and SMARCA4. It demonstrates effective biological activity in A549 cells, with degradation concentrations (DC50s) below 100 nM, achieving over 90% protein degradation (Dmax%) after 24 hours of treatment. This reagent is suitable for research applications involving epigenetic regulation and cancer biology.

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Cat. No.

A84625

CAS No.

2568276-39-9

PROTAC SMARCA2 degrader-9

PROTAC SMARCA2 degrader-9 (compound I-285) is an innovative PROTAC agent designed to selectively degrade SMARCA2 proteins. It demonstrates potent biological activity with a DC50 value of less than 100 nM, achieving over 90% degradation of SMARCA2 in A549 cell lines after 24 hours of treatment. This compound serves as a valuable tool for research applications aimed at elucidating the role of SMARCA2 in cancer biology and exploring targeted protein degradation strategies.

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Cat. No.

A84626

CAS No.

3053689-54-3

YN14 (mixture of diastereomers)

YN14 is a mixture of diastereomers that functions as a proteolysis targeting chimera (PROTAC) specifically targeting KRASG12C. This compound exhibits high potency and selectivity in degrading KRASG12C by forming a stable ternary complex with VHL, characterized by low binding free energy (ΔG). YN14 demonstrates significant antiproliferative activity, effectively inhibiting the growth of KRASG12C-mutant cancer cells, making it a valuable tool for cancer research and drug development.

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Cat. No.

A84627

CAS No.

3023568-80-8

PRT3789 epimer

PRT3789 epimer is an epimer of PRT3789, a selective degrader targeting SMARCA2 through the PROTAC approach. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby providing a valuable tool for studying the role of this protein in cancer and other diseases. It is essential for research applications focused on targeted protein degradation mechanisms and their therapeutic implications.

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1 mg

$590.00

5 mg

$1,510.00

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Cat. No.

A84628

CAS No.

3093563-31-3

SNIPER(ABL)-020

SNIPER(ABL)-020 is a PROTAC compound designed to selectively degrade the BCR-ABL fusion protein through targeted ubiquitin-proteasome pathway engagement. By conjugating Dasatinib, an ABL inhibitor, with Bestatin, an IAP ligand, SNIPER(ABL)-020 effectively promotes the protein's ubiquitination and subsequent degradation. This reagent is valuable for research focused on chronic myeloid leukemia and BCR-ABL related signaling pathways, offering insights into targeted protein degradation mechanisms in cancer therapeutics.

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5 mg

$695.00

10 mg

$1,220.00

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Cat. No.

A84629

CAS No.

2222354-91-6

SNIPER(ER)-87

SNIPER(ER)-87 is a PROTAC compound designed to efficiently degrade estrogen receptor α (ERα) through targeted ubiquitination. It consists of an IAP ligand (LCL161 derivative) linked to the ERα ligand (4-hydroxytamoxifen) via a PEG linker, resulting in an IC50 of 0.097 μM for ERα degradation. This compound preferentially recruits XIAP, the primary E3 ubiquitin ligase, to facilitate the selective degradation of ERα in cellular contexts. SNIPER(ER)-87 is valuable for research on hormone receptor regulation, breast cancer studies, and the development of targeted protein degradation strategies.

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5 mg

$850.00

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Cat. No.

A84631

CAS No.

2241690-03-7

SNIPER(ER)-110

SNIPER(ER)-110 is a PROTAC compound designed for targeted degradation of the estrogen receptor (ER). Comprising an IAP ligand and an estrogen ligand linked together, SNIPER(ER)-110 effectively induces ER protein degradation, exhibiting DC50 values of less than 3 nM at 4 hours and approximately 7.7 nM at 48 hours. This reagent is valuable for studies investigating ER-related signaling pathways and therapeutic strategies in hormone-dependent cancers.

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Cat. No.

A84660

CAS No.

2892523-73-6

PROTAC SMARCA2 degrader-1

PROTAC SMARCA2 degrader-1 is a targeted degrader designed to selectively degrade BRM2 (SMARCA2) with a DC50 value of less than 0.1 μM. This compound functions as an E3 ubiquitin ligase binding linker, facilitating the targeted degradation of specific proteins. Its application in cancer research makes it a valuable tool for elucidating the role of BRM2 in tumor biology and developing potential therapeutic strategies.

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