PROTAC Degrader

Cat. No.

A24841

CAS No.

2416130-57-7

NRX-0492

NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.

Cat. No.

A24842

CAS No.

2759351-69-2

Dovitinib-RIBOTAC TFA

Dovitinib-RIBOTAC TFA is a targeted RNA RIBOTAC degrader that specifically binds to and degrades pre-miR-21. This compound demonstrates significant anti-tumor activity and effectively inhibits breast cancer metastasis. It serves as a valuable tool for research involving RNA-targeted degradation and its implications in cancer biology.

Cat. No.

A24843

CAS No.

2573298-36-7

KTX-951

KTX-951 is a selective IRAK4 degrader that employs a PROTAC mechanism to facilitate targeted degradation of IRAK4 and IMiD substrates, including Ikaros and Aiolos. With a Kd of 3.5 nM and DC50 values of 13 nM for IRAK4, Ikaros, and Aiolos, KTX-951 demonstrates potent biological activity. It also exhibits an IC50 of 35 nM against OCl-Ly10 CTG, indicating its potential use in antitumor research applications.

Cat. No.

A24844

CAS No.

3052553-20-2

PROTAC JAK1 degrader 1

PROTAC JAK1 Degrader 1 is a selective PROTAC agent targeting JAK1, exhibiting a DC50 of 214 nM. This compound initiates rapid degradation of JAK1, leading to significant antitumor activity. It serves as a valuable tool for investigating JAK1-related signaling pathways and developing therapeutic strategies for malignancies driven by JAK1 dysregulation.

Cat. No.

A24846

CAS No.

2550393-21-8

MS154

MS154 is a novel E3 ligase cereblon-recruited degrader specifically targeting epidermal growth factor receptor (EGFR). It has demonstrated potent degradation of the EGFR L858R mutant in cancer cell lines with Kd values of 1.8 nM and 3.8 nM for wild-type and mutant EGFR, respectively. This selective degradation mechanism highlights its potential as an anticancer agent, particularly in lung cancer treatment. MS154 operates through an E3 ligase-dependent pathway, representing a promising therapeutic strategy for treating EGFR-driven malignancies.

Cat. No.

A24847

CAS No.

2089205-64-9

PROTAC RIPK degrader-6

PROTAC RIPK degrader-6 is a Cereblon-based protein-targeting chimeric molecule designed for the degradation of RIP Kinase. This compound employs a RIP2 kinase inhibitor linked through a suitable spacer to a cereblon ligand, facilitating targeted proteolysis of RIPK. Prominent applications include investigations into kinase-related signaling pathways and the development of innovative therapeutic strategies for diseases associated with RIPK dysregulation.

Cat. No.

A24848

CAS No.

2133360-00-4

PROTAC BRD4 Degrader-1

PROTAC BRD4 Degrader-1 is a novel PROTAC that utilizes ligands for both Cereblon and BRD4, exhibiting an IC50 of 41.8 nM against the BRD4 bromodomain 1 (BD1). This compound promotes the degradation of BRD4 protein, leading to a significant decrease in c-Myc expression. It is designed for research applications aimed at understanding the role of BRD4 in transcriptional regulation and its implications in various cancers.

Cat. No.

A24849

CAS No.

2306388-65-6

PROTAC ERRα Degrader-3

PROTAC ERRα Degrader-3 is a selective degrader targeting estrogen-related receptor alpha (ERRα) through a von Hippel-Lindau-based mechanism. This compound effectively induces the degradation of ERRα protein by over 80% at a concentration of 30 nM, while showing no activity against ERRβ and ERRγ. It serves as a valuable tool for researchers investigating the role of ERRα in various biological processes and disease states.

Cat. No.

A24851

CAS No.

2639882-69-0

PROTAC EED degrader-2

PROTAC EED Degrader-2 is a von Hippel-Lindau-based PROTAC that selectively targets the embryonic ectoderm development (EED) subunit of the polycomb repressive complex 2 (PRC2), exhibiting a pKD of 9.27. This compound acts as an effective inhibitor, demonstrating a pIC50 of 8.11, facilitating the degradation of EED and providing valuable insights for research on PRC2-related epigenetic regulation and its implications in various biological processes. Applications include studies on gene expression regulation and potential therapeutic targets in cancer and developmental biology.

Cat. No.

A24852

CAS No.

2488851-89-2

PROTAC IDO1 Degrader-1

PROTAC IDO1 Degrader-1 is a novel compound targeting indoleamine 2,3-dioxygenase 1 (IDO1) through the engagement of Cereblon E3 ligase, facilitating its ubiquitination and subsequent degradation. With a reported DC50 of 2.84 μM, this degrader enhances the anti-tumor efficacy of HER2 CAR-T cells, making it a valuable tool for research in cancer immunotherapy and targeted degradation methods. Its ability to modulate IDO1 levels opens avenues for investigations into metabolic regulation and tumor microenvironment interactions.

Cat. No.

A24853

CAS No.

2316837-10-0

ARD-69

ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand.

Cat. No.

A24854

CAS No.

2384184-44-3

KB02-JQ1

KB02-JQ1 is a selective PROTAC BRD4 degrader that functions as a molecular glue, specifically targeting BRD4 while sparing BRD2 and BRD3. This compound induces BRD4 degradation by covalently modifying the E3 ligase DCAF16, thereby enhancing the stability and duration of protein degradation in biological systems. Its unique design, which incorporates JQ1 linked to the ubiquitin E3 ligase ligand KB02, facilitates targeted modulation of gene expression, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A24855

CAS No.

2921556-14-9

PROTAC TYK2 degradation agent1

PROTAC TYK2 degradation agent1 is a selective degrader targeting TYK2, effectively facilitating its degradation with a DC50 value of 14 nM. This compound highlights significant biological activity in modulating TYK2 levels, making it a useful tool for investigating autoimmune diseases. Research applications include studying the role of TYK2 in inflammatory pathways and evaluating potential therapeutic strategies.

Cat. No.

A24856

CAS No.

2139329-47-6

BSJ-02-162

Synonyms: CDK4/6-IN-11

BSJ-02-162 is a potent PROTAC degrader targeting CDK4/6 through the utilization of a thalidomide-based E3 ligase ligand and a selective CDK4/6 inhibitor. This compound effectively recruits ubiquitin ligases to facilitate the targeted degradation of CDK4/6, thereby modulating cellular responses to cell cycle regulation. BSJ-02-162 is designed for research applications exploring cancer therapies and the mechanisms of protein homeostasis within tumor cells.

Cat. No.

A24857

CAS No.

2655638-07-4

PROTAC PTPN2 degrader-1

PROTAC PTPN2 degrader-1 is an effective degrader of the protein tyrosine phosphatase PTPN2. This compound facilitates target protein degradation through the proteasome pathway, enabling the modulation of cellular signaling related to cancer and metabolic diseases. Its application in research may provide insights into the therapeutic potential of targeting PTPN2 in various disease contexts.

Cat. No.

A24859

CAS No.

2639882-72-5

PROTAC EED degrader-1

PROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC that selectively targets EED with a pKD of 9.02. This compound functions as a polycomb repressive complex 2 (PRC2) inhibitor, exhibiting an inhibitory potency characterized by a pIC50 of 8.17. It serves as a valuable tool for researching the modulation of PRC2 activity and its implications in cancer biology and epigenetic regulation.

Cat. No.

A25074

CAS No.

2782022-40-4

LD4172

LD4172 is a selective RIPK1 PROTAC degrader that exhibits a Ki of 4.8 nM. It facilitates RIPK1 protein degradation through the formation of a ternary complex with RIPK1 and VHL E3 ligase, leading to ubiquitination and proteasomal degradation. LD4172 effectively inhibits TNF-induced classical NF-κB signaling in TRAF2-deficient cells, significantly reducing IκBα phosphorylation and IL-8 production. Additionally, it promotes apoptosis and immunogenic cell death in tumor cells, enhances tumor-infiltrating lymphocyte responses, and sensitizes tumors to anti-PD1 therapy, making it a valuable chemical probe for studying RIPK1-related functions in melanoma and colon cancer research.

Cat. No.

A25107

CAS No.

2541626-49-5

PROTAC CDK2/4/6 Degrader-2

PROTAC CDK2/4/6 Degrader-2 is a targeted protein degradator specifically designed to degrade cyclin-dependent kinases CDK2, CDK4, and CDK6. This compound effectively inhibits cell proliferation and induces cell cycle arrest and apoptosis in malignant melanoma cells. Its application extends to cancer research, particularly in investigating the role of CDK2/4/6 in tumor biology. The compound can also be converted into its prodrug form, enabling versatile utilization in various assays related to cancer therapeutics.

Cat. No.

A25149

CAS No.

2410947-56-5

PROTAC BRD4 Degrader-6

PROTAC BRD4 Degrader-6 is a potent small-molecule degrader that targets BRD4, exhibiting an IC50 value of 2.7 nM for the BRD4 BD1 domain. This compound effectively degrades BRD4 protein and leads to the downregulation of c-Myc expression. In vitro studies demonstrate its capacity to inhibit proliferation and induce apoptosis in the pancreatic cancer cell line BxPC3, making it a valuable tool for research in human pancreatic cancer biology.

Cat. No.

A25213

CAS No.

3058911-16-0

DeFer-2

DeFer-2 is a PROTAC degrader targeting ferritin, with a Kd of 17.1 μM. By inducing ferritin degradation, DeFer-2 leads to caspase 3-GSDME-mediated pyroptosis in cancer cells, driven by an accumulation of free iron and elevated reactive oxygen species (ROS). This compound demonstrates significant tumor growth inhibition and extends survival in mouse models bearing B16F10 subcutaneous tumors, making it a valuable tool for research in melanoma.

Cat. No.

A25411

CAS No.

1182011-65-9

AR Degrader-3

AR Degrader-3 is an orally active molecular glue that targets the Androgen Receptor (AR) and its variant ARV7, inducing their degradation through the ubiquitin-proteasome pathway. By directly interacting with both the ligand-binding domain and the N-terminal domain of AR, it effectively suppresses the transcriptional activity of wild-type AR, AR mutants, and ARV7. This compound downregulates mRNA and protein levels of downstream AR target genes, providing a mechanism to overcome antiandrogen resistance associated with ARV7 and point mutations. Additionally, AR Degrader-3 promotes apoptosis in Enzalutamide-resistant cells through the elevation of cleaved caspase-3, making it a valuable tool in the research of castration-resistant prostate cancer.

Cat. No.

A25508

CAS No.

3038446-94-2

SK2188

Synonyms: JB325

SK2188 is a potent and selective PROTAC degrader that targets Aurora Kinase A (AURKA) with a DC50 of 3.9 nM. It induces DNA damage and promotes apoptosis in cancer cells, effectively leading to the degradation of MYCN. SK2188 serves as a valuable tool for investigating tumor cell proliferation and exploring therapeutic strategies in MYCN-amplified neuroblastoma.

Cat. No.

A25759

CAS No.

1603845-42-6

TX2-121-1

TX2-121-1 is a selective degrader of Her3 (ErbB3), featuring a hydrophobic adamantane moiety. With an IC50 of 49 nM, TX2-121-1 effectively inhibits Her3-dependent signaling as well as heterodimerization, leading to reduced cell proliferation. This reagent is valuable for research applications focused on tumor biology and the elucidation of Her3-related pathways.

Cat. No.

A25830

CAS No.

3035638-40-2

MS15

MS15 is a selective AKT PROTAC degrader that demonstrates potent inhibition of AKT isoforms 1, 2, and 3, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively. This compound facilitates the targeted degradation of AKT, making it a valuable tool for investigating AKT-related signaling pathways. Its applications include studying cellular processes like metabolism, growth, and survival in various cancer models.

Cat. No.

A25891

CAS No.

2897640-93-4

PROTAC HER2 degrader-1

PROTAC HER2 degrader-1 is a selective PROTAC that targets the HER2 receptor, exhibiting a DC50 value of 69 nM with a Dmax of 96%. By inducing persistent HER2 degradation, it effectively inhibits cell proliferation and tumor growth in HER2-positive cancer models, while also suppressing critical downstream signaling pathways such as AKT and ERK. Additionally, PROTAC HER2 degrader-1 promotes apoptosis in BT-474 cells, making it a valuable tool for the study of HER2-positive malignancies.