PROTAC Degrader

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.

Cat. No.

A26034

CAS No.

3087311-36-9

PROTAC PDE4 degrader-1

PROTAC PDE4 degrader-1 is a selective and orally active degrader targeting phosphodiesterase 4 (PDE4). It exhibits a DC50 of 41.98 μM and effectively inhibits the secretion of pro-inflammatory cytokines such as TNF-α and IL-6. This compound demonstrates significant potential in alleviating pulmonary inflammation in LPS-induced acute lung injury models, making it a valuable tool for studying inflammatory diseases and therapeutic interventions.

Cat. No.

A26156

CAS No.

3091132-73-6

FIP22

FIP22 is a potent and selective degrader of IRAK4 utilizing the PROTAC technology. It functions by inducing degradation through the formation of a ternary complex consisting of IRAK4, FIP22, and CRBN, with an EC50 of 12.63 nM. This mechanism effectively inhibits IRAK4-mediated signaling pathways, including NF-κB and MAPK pathways, making FIP22 valuable for research into conditions such as atopic dermatitis, where IRAK4 plays a critical role.

Cat. No.

A26221

CAS No.

3070346-91-4

R1-ICR-5

R1-ICR-5 is a selective RIPK1 PROTAC degrader designed to mediate protein degradation via the VHL pathway. This compound promotes the degradation of RIPK1, subsequently dysregulating TNFR1 and TLR3/4 signaling pathways, enhancing the activity of NF-κB, MAPK, and IFN signaling. Additionally, R1-ICR-5 facilitates RIPK3 activation, leading to necroptosis. This reagent is applicable in research focused on triple-negative breast cancer and skin inflammation.

Cat. No.

A26348

CAS No.

2669785-76-4

JPS014

JPS014 is a benzamide-based HDAC degrader designed to engage the Von Hippel-Lindau (VHL) E3 ligase for targeted proteolysis. It effectively degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression profiles and promoting apoptotic pathways in HCT116 cancer cells. This compound is particularly useful for studying the role of HDAC inhibition in cancer biology and elucidating mechanisms of resistance to therapies.

Cat. No.

A26404

CAS No.

3036245-14-1

PROTAC HDAC4 Degrader-1

PROTAC HDAC4 Degrader-1 is a selective PROTAC that targets and promotes the degradation of HDAC4, a histone deacetylase involved in regulating gene expression. This compound effectively decreases HDAC4 protein levels, leading to S phase cell cycle arrest and reduced tumor cell proliferation, as evidenced by its impact on colony formation. Additionally, PROTAC HDAC4 Degrader-1 demonstrates efficacy in vivo in H460 mouse models, making it a valuable tool for cancer research, particularly in studies related to lung cancer.

Cat. No.

A26423

CAS No.

3092219-09-2

YX862

YX862 is a selective PROTAC degrader targeting HDAC8, designed to induce robust degradation of this histone deacetylase. It achieves over 95% degradation of HDAC8 at a concentration of 250 nM in MDA-MB-231 cells. This compound serves as a valuable tool for investigating the role of HDAC8 in various biological processes and provides insights into potential therapeutic strategies for HDAC8-related diseases.

Cat. No.

A26482

CAS No.

2669785-84-4

JPS035

JPS035 is a benzamide-derived HDAC degrader that utilizes the Von Hippel-Lindau (VHL) E3 ligase-mediated PROTAC technology. It specifically targets and degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression and promoting apoptosis in HCT116 colorectal cancer cells. This compound serves as a valuable tool for studies focused on epigenetic modulation and therapeutic strategies against HDAC-related diseases.

Cat. No.

A26487

CAS No.

2669785-77-5

JPS016

JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor that targets HDAC1, HDAC2, and HDAC3 for ubiquitination and proteasomal degradation via VHL E3 ligase recruitment. This compound demonstrates significant anticancer activity by reducing the viability of colon cancer cells and inducing apoptosis. Additionally, JPS016 activates the PINK1/Parkin-mediated mitochondrial autophagy pathway, enhancing cardiomyocyte viability, alleviating mitochondrial damage, and decreasing mitochondrial ROS production. It is valuable for research into colon cancer and sepsis-related cardiac dysfunction.

Cat. No.

A26536

CAS No.

2785404-83-1

HDAC6 degrader-3

HDAC6 Degrader-3 is a selective inhibitor that promotes the degradation of histone deacetylase 6 (HDAC6) through ternary complex formation and the ubiquitin-proteasome pathway, exhibiting a DC50 value of 19.4 nM. With IC50 values of 4.54 nM for HDAC6 and 0.647 μM for HDAC1, it effectively induces significant hyperacetylation of α-tubulin. This compound is valuable for research applications focused on neurodegenerative diseases and cancer, where modulation of HDAC6 activity may play a critical role.

Cat. No.

A26537

CAS No.

2978763-95-8

HD-TAC7

HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD).

Cat. No.

A26550

CAS No.

2669785-85-5

JPS036

JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models.

Cat. No.

A26609

CAS No.

3098718-46-5

PROTAC EZH2 Degrader-3

PROTAC EZH2 Degrader-3 (compound ZJ-20) specifically targets and degrades the EZH2 protein through a proteolysis-targeting chimera (PROTAC) mechanism. This compound demonstrates potent inhibition of EZH2 expression as well as a significant reduction in other PRC2 subunits and H3K27me3 levels. Additionally, PROTAC EZH2 Degrader-3 exhibits anti-proliferative effects, inducing cell cycle arrest in the G0-G1 phase and promoting apoptosis in cancer cells, making it valuable for research in cancer therapeutics and epigenetic regulation.

Cat. No.

A26611

CAS No.

2978620-84-5

PROTAC EZH2 Degrader-9

PROTAC EZH2 Degrader-9 is an orally active PROTAC that selectively degrades EZH2 via the ubiquitin-proteasome pathway. By downregulating PRC2 core subunits and inhibiting H3K27me3, it effectively reverses PRC2-mediated gene silencing and disrupts EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 demonstrates potent antiproliferative effects on various cancer cell lines, inducing cell cycle arrest and apoptosis. This reagent is valuable for research focused on leukemia, lymphoma, and non-small cell lung cancer.