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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.

A26633

CAS No.

2839552-68-8

WIZ degrader 1

WIZ Degrader 1 is a selective degrader targeting widely interspaced zinc finger motifs (WIZ) with an AC50 of 2 nM. This compound induces the expression of fetal hemoglobin (HbF) with an EC50 of 6 mM, providing a valuable tool for research into inherited blood disorders. Its capability to modulate HbF levels highlights its potential applications in therapeutic strategies for conditions such as sickle cell disease and beta-thalassemia.

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25 mg

$1,655.00

50 mg

$2,115.00

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Cat. No.

A26665

CAS No.

3032785-00-2

CARM1 degrader-1

CARM1 degrader-1 is a selective PROTAC degrader targeting CARM1, exhibiting a DC50 value of 8.1 nM. It effectively degrades CARM1 through a VHL- and proteasome-mediated mechanism, leading to a reduction in the methylation levels of CARM1 substrates in various cell-based assays. Additionally, CARM1 degrader-1 demonstrates the ability to inhibit cancer cell migration, making it a valuable tool for investigating mechanisms in breast cancer research.

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Cat. No.

A26675

CAS No.

2839552-69-9

WIZ degrader 2

WIZ Degrader 2 is an efficient degrader targeting widely interspaced zinc finger motifs, with an AC50 of 0.011 μM. This compound enhances the expression of fetal hemoglobin (HbF) with an EC50 of 0.038 μM. WIZ Degrader 2 is a valuable tool for research into inherited blood disorders, facilitating studies aimed at understanding and potentially treating these conditions.

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25 mg

$1,780.00

50 mg

$2,280.00

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Cat. No.

A26801

CAS No.

2929304-06-1

UNC8732 TFA

UNC8732 (TFA) is a potent inhibitor of NSD2, functioning as a protein degrader. This compound promotes cellular degradation of NSD2, which plays a critical role in various cellular processes, including gene expression and chromatin regulation. UNC8732 (TFA) is utilized in research related to cancer biology and epigenetic regulation, providing insights into NSD2's role in disease mechanisms and potential therapeutic strategies.

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1 mg

$220.00

5 mg

$560.00

All 2 sizes
Cat. No.

A26831

CAS No.

2929304-61-8

UNC8153 TFA

UNC8153 TFA is a potent degrader targeting nuclear receptor-binding SET domain-containing 2 (NSD2) with a Kd of 24 nM. This compound effectively decreases cellular levels of NSD2 protein, exhibiting a DC50 of 0.35 μM in U2OS cells, and diminishes the H3K36me2 chromatin modification. With its streamlined warhead, UNC8153 TFA facilitates proteasome-dependent degradation of NSD2, making it a valuable tool for investigating the role of NSD2 in various biological processes and disease mechanisms.

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1 mg

$55.00

5 mg

$130.00

All 6 sizes
Cat. No.

A26849

CAS No.

3049087-34-2

NC-R17

NC-R17 is a non-covalent degrader targeting Glutathione Peroxidase 4 (GPX4) through the PROTAC mechanism, designed to induce ferroptosis in cancer cells. Exhibiting significant antitumor activity, NC-R17 facilitates the targeted degradation of GPX4, contributing to research in cancer biology and therapeutic strategies. The compound combines a Demethyl-RSL3 ligand for GPX4 with an E3 ubiquitin ligase ligand derived from Lenalidomide, connected by a specific PROTAC linker to enhance its biological activity.

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Cat. No.

A26890

CAS No.

3096510-51-6

PROTAC FSP1 degrader 1

PROTAC FSP1 Degrader 1 is a potent PROTAC compound designed to selectively degrade FSP1, leading to an increase in intracellular lipid peroxides. This reagent effectively promotes ferroptosis in conjunction with GPX4 inhibitors and significantly elevates reactive oxygen species (ROS) production. Additionally, PROTAC FSP1 Degrader 1 upregulates the mRNA expression of several ferroptosis-related proteins, including GPX4, FTH1, ACSL4, TfR1, and FSP1. This compound is particularly suitable for research focused on triple-negative breast cancer.

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Cat. No.

A26947

CAS No.

3071165-43-7

PROTAC GPX4 degrader-4

PROTAC GPX4 degrader-4 selectively targets GPX4, functioning as a PROTAC degrader with a DC50 of 5.32 nM. This compound effectively inhibits the proliferation of RT4, T24, and J82 bladder cancer cell lines, exhibiting IC50 values of 0.09, 2.97, and 7.58 μM, respectively. PROTAC GPX4 degrader-4 promotes the accumulation of lipid reactive oxygen species (ROS) and triggers ferroptosis in T24 and RT4 cells. Additionally, it demonstrates significant antitumor efficacy in a T24 tumor-bearing BALB/c nude mouse model, making it a valuable tool for bladder cancer research.

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Cat. No.

A28547

CAS No.

1323151-45-6

HyT36

HyT36 is a low molecular weight hydrophobic tag that facilitates the targeted degradation of fusion proteins by leveraging the cellular ubiquitin-proteasome pathway. This compound is particularly effective for studies involving pseudokinase Her3, enabling researchers to investigate its functional roles and regulatory mechanisms. HyT36 serves as a valuable tool in protein degradation research and the exploration of protein interactions within cellular environments.

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1 mg

$40.00

5 mg

$100.00

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Cat. No.

A28613

CAS No.

3057939-66-6

Gly-PEG3-BA

Gly-PEG3-BA is an EML4-ALK PROTAC degrader that targets the EML4-ALK fusion protein. This compound exhibits a DC50 of 0.50 μM for EML4-ALK in H3122 cells and a DC50 of 20.15 μM for EGFR mutant (L858R/T790M) levels in H1975 cells. Gly-PEG3-BA demonstrates notable antiproliferative effects, with IC50 values of 0.84 μM against H3122 cells and 20.74 μM against H1975 cells. It is a valuable tool for research in non-small cell lung cancer.

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Cat. No.

A28645

CAS No.

3057939-67-7

Lys-PEG3-BA

Lys-PEG3-BA is a novel EML4-ALK/EGFR PROTAC degrader that influences target proteins through the ubiquitin-proteasome pathway. With DC50 values of 1.32 μM against H3122 (EML4-ALK) cells and 19.66 μM for H1975 (EGFR-L858R/T790M) cells, it effectively inhibits cell proliferation. This compound serves as a valuable tool for research into non-small cell lung cancer and the mechanisms underlying targeted protein degradation.

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Cat. No.

A28652

CAS No.

3065209-64-2

PROTAC EGFR degrader 17

PROTAC EGFR degrader 17 is a potent EGFR-targeted PROTAC degrader with a DC50 value of 0.49 nM. This reagent facilitates the ubiquitination and subsequent degradation of the epidermal growth factor receptor (EGFR). It is particularly useful for research applications related to various forms of cancer, including non-small cell lung cancer, providing a valuable tool for investigating targeted degradation pathways in oncogenesis.

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Cat. No.

A28665

CAS No.

2654821-05-1

PROTAC EGFR degrader 12

PROTAC EGFR degrader 12 is a PROTAC designed to selectively target and degrade mutant forms of epidermal growth factor receptor (EGFR). It demonstrates potent biological activity with IC50 values under 50 nM against EGFRL858R-T790M (NCI-H1975 cells), EGFRL858R (NCI-H3255 cells), and EGFRL858R-T790M-L797S (NCI-H1975+CS cells). This reagent is valuable for research applications focused on understanding and treating EGFR-driven cancers, particularly those with resistant mutations.

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Cat. No.

A28732

CAS No.

2654821-07-3

PROTAC EGFR degrader 16

PROTAC EGFR degrader 16 is a selective degrader designed to target the epidermal growth factor receptor (EGFR). It exhibits DC50 values of less than 50 nM in various cell lines, including NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R), and NCI-H1976 + CS (EGFR L858R-T970M-L797S). This compound is valuable for investigating EGFR-driven cancers, particularly non-small cell lung cancer, facilitating research into targeted degradation therapies.

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Cat. No.

A28741

CAS No.

1603845-45-9

TX2-120-1

TX2-120-1 is a potent Her3 degrader, exhibiting an IC50 value of 56 nM for Her3 binding. This compound facilitates the degradation of the Her3 protein, making it a valuable tool for investigating Her3-related pathways and therapeutic applications. Additionally, TX2-120-1 can be utilized in the synthesis of TX2-121-1, further expanding research possibilities in targeted protein degradation.

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Cat. No.

A28753

CAS No.

3034244-56-6

PROTAC EGFR degrader 10

PROTAC EGFR Degrader 10 is an advanced PROTAC agent targeting the epidermal growth factor receptor (EGFR) with a DC50 of less than 100 nM. It effectively binds to CRBN-DDB1 with a Ki of 37 nM, facilitating the degradation of EGFR as well as focal adhesion kinase (FAK) and RSK1. This compound demonstrates potent inhibitory effects on the proliferation of BaF3 cells, including those with EGFR mutations, with an IC50 of less than 150 nM. PROTAC EGFR Degrader 10 is suitable for studies focused on targeted protein degradation and cancer research.

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Cat. No.

A28883

CAS No.

3034244-71-5

PROTAC EGFR degrader 11

PROTAC EGFR Degrader 11 is a targeted degrader specifically designed to modulate the epidermal growth factor receptor (EGFR) through the PROTAC mechanism. It effectively binds to the CRBN-DDB1 complex with a Ki value of 36 nM and has a DC50 of less than 100 nM for EGFR degradation. This compound demonstrates significant biological activity by degrading not only EGFR but also focal adhesion kinase (FAK) and RSK1. Additionally, it inhibits the proliferation of BaF3 cells with both wild-type and mutant EGFR variants, achieving an IC50 of less than 100 nM, making it a valuable tool for cancer research focused on EGFR-related pathways.

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1 mg

$385.00

5 mg

$1,000.00

All 4 sizes
Cat. No.

A28887

CAS No.

2103331-95-7

PROTAC Her3 Degrader-8

PROTAC Her3 Degrader-8 is a potent Her3 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of the Her3 protein. This compound is particularly relevant for studies focused on lung adenocarcinoma and ovarian cancer, enabling researchers to investigate the role of Her3 in these malignancies. The design incorporates a specific Her3 ligand, an E3 ligase ligand, and a linker, which optimizes its efficacy as a targeted degradation tool in research applications.

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1 mg

$350.00

5 mg

$1,085.00

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Cat. No.

A28911

CAS No.

2230821-38-0

SJF-1528

SJF-1528 is a potent EGFR PROTAC degrader that selectively targets wild-type EGFR and Exon 20 Ins mutant EGFR, exhibiting DC50 values of 39.2 nM and 736.2 nM, respectively, in OVCAR8 and HeLa cells. This compound facilitates the ubiquitination and subsequent degradation of EGFR and also affects HER2 levels. SJF-1528 is valuable for breast cancer research, providing insights into targeted degradation mechanisms and alterations in growth factor signaling pathways.

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1 mg

$135.00

5 mg

$345.00

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Cat. No.

A28959

CAS No.

2923686-62-6

PROTAC PARP1 degrader-2

PROTAC PARP1 degrader-2 is a targeted protein degradation compound designed to specifically degrade PARP1. With a DC50 of less than 10 nM in MDA-MB-231 cells, it demonstrates potent efficacy in inducing degradation. Additionally, this compound inhibits cell viability in MDA-MB-436 cells with an IC50 of less than 100 nM, making it a valuable tool for research in cancer therapeutics and the mechanistic study of PARP1 function.

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Cat. No.

A29009

CAS No.

3093642-25-9

PROTAC EZH2 Degrader-44

PROTAC EZH2 Degrader-44 is a selective degrader targeting the EZH2-PRC2 complex through the recruitment of the CRBN E3 ligase, facilitating proteasome-mediated degradation of EZH2, SUZ12, and EED. This process leads to a marked reduction in H3K27me3 and CARM1 levels, resulting in potent antiproliferative effects. It induces mitochondrial dysfunction and promotes apoptosis by modulating Bcl-2 family proteins, demonstrating minimal cytotoxicity in normal human mammary epithelial, liver, and kidney cells. PROTAC EZH2 Degrader-44 serves as an effective research tool for investigating targeted therapies in triple-negative breast cancer.

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Cat. No.

A29123

CAS No.

2569517-30-0

RBN012811

RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections.

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5 mg

$965.00

10 mg

$1,640.00

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Cat. No.

A29140

CAS No.

2966791-41-1

NP1192

NP1192 is a selective PROTAC degrader targeting NAT10, effectively depleting NAT10 protein levels and inhibiting ac4C modification in cancer cells. This compound disrupts the NAT10/HIF-1α/PD-L1 signaling axis, resulting in dual inhibition of hypoxia-driven glycolysis and immunosuppression, thus enhancing antitumor efficacy. NP1192 is valuable for research applications in ovarian, cervical, and glioblastoma cancers, providing insights into therapeutic strategies involving NAT10 modulation.

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Cat. No.

A29147

CAS No.

3031606-85-3

PROTAC KAT2A/B degrader-1

PROTAC KAT2A/B degrader-1 is a targeted degrader that selectively induces the degradation of histone acetyltransferases KAT2A and KAT2B. This compound demonstrates significant inhibition of proliferation in acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 is a valuable tool for studying the roles of KAT2A and KAT2B in cancer biology and may facilitate the development of novel therapeutic strategies for these malignancies.

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Cat. No.

A29148

CAS No.

2260944-69-0

GSK702

GSK702 is a PROTAC that targets the P300/CBP-associated factor (PCAF) with a focus on the less active cis-(S,S)-enantiomer of GSK983. This compound exhibits a modest ability to reduce PCAF protein levels and effectively binds to Cereblon (CRBN), leading to decreased interleukin-1 beta (IL-1β) levels in macrophages. GSK702 serves as a valuable tool for investigating the role of inflammatory mediators in cellular processes.

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