PROTAC Degrader

Cat. No.

A65764

CAS No.

2893885-31-7

PROTAC HPK1 Degrader-2

PROTAC HPK1 Degrader-2 targets HPK1 for degradation via a proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 23 nM in human peripheral blood mononuclear cells (PBMC), this compound is instrumental in elucidating HPK1's functions in cancer biology. The selectivity and potency of PROTAC HPK1 Degrader-2 make it a valuable tool for cancer research applications, enabling the study of targeted protein degradation and its implications in therapeutic strategies.

Cat. No.

A65774

CAS No.

2893885-42-0

HPK1-IN-47

HPK1-IN-47 is a selective HPK1 ligand designed for the synthesis of PROTACs, specifically serving as a precursor for PROTAC HPK1 Degrader-2. It exhibits potential in targeting HPK1, which plays a significant role in various HPK1-mediated diseases, particularly cancer. This compound is valuable for research applications focused on elucidating the therapeutic potential of HPK1 degradation in cancer treatment.

Cat. No.

A65775

CAS No.

3099168-12-1

PROTAC HPK1 Degrader-6

PROTAC HPK1 Degrader-6 is a potent PROTAC compound designed to selectively target and degrade the HPK1 protein, exhibiting an IC50 of less than 50 nM. This compound facilitates the investigation of HPK1's role in leukemia and other related disorders. By employing the dual binding mechanism to HPK1 and the E3 ligase CRBN, it serves as a valuable tool for researchers exploring targeted protein degradation as a therapeutic strategy.

Cat. No.

A65783

CAS No.

3047066-15-6

DD205-291

DD205-291 is an orally active PROTAC HPK1 degrader that exhibits a DC50 value of 5.3 nM. Its primary mechanism involves the targeted degradation of HPK1, leading to the inhibition of SLP-76 phosphorylation. This modulation subsequently results in the enhanced expression of key cytokines such as IL-2 and IFN-γ, making DD205-291 a valuable reagent for studies in immune signaling and related therapeutic applications.

Cat. No.

A65816

CAS No.

2756323-28-9

MS910

MS910 is a potent and selective PROTAC degrader targeting MEK1 and MEK2 kinases. It demonstrates effective degradation of MEK1 and MEK2 in various cancer cell lines, with reported DC50 values of 118 nM for MEK1 and 55 nM for MEK2 in HT-29 cells, and 94 nM for MEK1 and 38 nM for MEK2 in SK-MEL-28 cells. MS910 is primarily utilized in cancer research to explore the therapeutic potential of targeted protein degradation.

Cat. No.

A65826

CAS No.

3032600-90-8

PROTAC MLKL Degrader-1

PROTAC MLKL Degrader-1 selectively targets and degrades MLKL, achieving a maximum efficacy (Dmax) greater than 90%. This compound incorporates modified CRBN ligands and linker components, functioning effectively in cellular models. PROTAC MLKL Degrader-1 effectively inhibits cell death in a TNF-α, Smac, and zVAD (TSZ) model of necroptosis, making it a valuable tool for investigating necroptosis pathways and their implications in various diseases.

Cat. No.

A65835

CAS No.

3103327-20-1

PROTAC MLKL Degrader-2

PROTAC MLKL Degrader-2 is a novel PROTAC designed to specifically target MLKL (Mixed Lineage Kinase) for degradation. This compound utilizes a bifunctional approach, combining an E3 ligase ligand, Thalidomide, with a linker, N-Methylpiperazine, to facilitate the ubiquitination and subsequent proteasomal degradation of MLKL. By effectively modulating MLKL levels, this reagent serves as a powerful tool for investigating the role of MLKL in various biological processes, including cell death and inflammatory responses, thus enabling insights into therapeutic interventions for related diseases.

Cat. No.

A66587

CAS No.

1628323-80-7

Rusfertide

Synonyms: PTG-300

Rusfertide is a peptide mimetic of natural hepcidin that functions as a ferroportin degrader. By promoting the degradation of ferroportin, Rusfertide effectively reduces serum iron levels and transferrin saturation, thereby influencing red blood cell production. This compound shows potential for therapeutic applications in conditions such as polycythemia vera, β-thalassemia, and hereditary hemochromatosis.

Cat. No.

A69079

CAS No.

3046195-01-8

PTOTAC HSD17B13 degrader 1

PTOTAC HSD17B13 degrader 1 is a PROTAC designed to selectively target and promote the degradation of 17β-Hydroxysteroid dehydrogenase 13 (HSD17B13). This compound consists of a specific ligand for HSD17B13, a linker based on tert-Butyl 5-bromoisoindoline-2-carboxylate, and a ligand for an E3 ubiquitin ligase, enabling effective ubiquitination and subsequent proteasomal degradation of the target protein. PTOTAC HSD17B13 degrader 1 is a valuable tool for studying HSD17B13 functions and has potential applications in therapeutic development and protein regulation research.

Cat. No.

A69764

CAS No.

2411389-67-6

PROTAC CYP1B1 degrader-1

PROTAC CYP1B1 Degrader-1 is a targeted degrader designed to selectively eliminate cytochrome P450 1B1 (CYP1B1), utilizing a α-naphthoflavone chimera derivative. This compound exhibits IC50 values of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2, demonstrating its specificity in degrading CYP1B1. It serves as a valuable tool for investigating the role of CYP1B1 in prostate cancer and may aid in overcoming CYP1B1-mediated drug resistance in therapeutic applications.

Cat. No.

A69932

CAS No.

2836297-26-6

PROTAC CYP1B1 degrader-2

PROTAC CYP1B1 degrader-2 is a VHL E3 ligase-based degrader targeting CYP1B1, exhibiting a DC50 of 1.0 nM in A549/Taxol cells after 24 hours. This compound effectively inhibits the growth, migration, and invasion of cancer cells, making it a valuable tool for research into the therapeutic potential of targeting CYP1B1 in cancer treatment. Its unique mechanism of action offers insights into the modulation of protein levels in various biological contexts.

Cat. No.

A74601

CAS No.

3093413-94-3

PROTAC sEH-degrader-3

PROTAC sEH-degrader-3 is a selective sEH PROTAC degrader that specifically targets soluble epoxide hydrolase (sEH) in the cytosol, sparing its activity in peroxisomes. This compound induces degradation of sEH via a CRBN-mediated lysosomal pathway, exhibiting an IC50 of 0.8 nM against human sEH. PROTAC sEH-degrader-3 is valuable for research focusing on endoplasmic reticulum stress, inflammation, and metabolic diseases, offering insights into therapeutic strategies targeting these pathways.

Cat. No.

A74971

CAS No.

3033465-51-6

PROTAC TG2 degrader-2

PROTAC TG2 Degrader-2 is a selective degrader that targets Transglutaminase 2 (TG2). This compound effectively inhibits cell migration and reduces TG2 levels in ovarian cancer cells, making it a valuable tool for research into ovarian cancer biology. Its ability to modulate TG2 offers insights into potential therapeutic strategies against this malignancy.

Cat. No.

A74987

CAS No.

3033465-55-0

PROTAC TG2 degrader-1

PROTAC TG2 degrader-1 is a von Hippel-Lindau (VHL)-based PROTAC designed to specifically target tissue transglutaminase (TG2) with a dissociation constant (KD) of 68.9 μM. This compound effectively induces the degradation of TG2 in ovarian cancer cells through a proteasome-dependent mechanism. It serves as a valuable tool for research investigating the role of TG2 in cancer biology and potential therapeutic applications.

Cat. No.

A75023

CAS No.

1354444-72-6

EA-B2L

EA-B2L is a potent glutathione S-transferase P (GSTP) degrader, exhibiting a DC50 value of 48 μM. This compound is a Boc2Lys-linked Ethacrynic acid derivative, making it a valuable tool for studying GSTP-related pathways. Its ability to selectively degrade GSTP contributes to advancements in cancer research, allowing for the exploration of therapeutic strategies targeting GSTP expression and function.

Cat. No.

A75648

CAS No.

2715104-45-1

PROTAC HMGCR Degrader-1

PROTAC HMGCR Degrader-1 is an orally active PROTAC targeting HMGCR, exhibiting an IC50 of 1.32 μM. This lactone prodrug effectively leads to significant degradation of HMGCR, resulting in substantial cholesterol-lowering effects observed in vivo. PROTAC HMGCR Degrader-1 is valuable for research applications focused on hyperlipidemia and lipid metabolism.

Cat. No.

A75732

CAS No.

3048196-52-4

NU227326

NU227326 is a potent IDO1 PROTAC degrader designed to penetrate the blood-brain barrier, exhibiting a DC50 of 4.5 nM in HiBiT degradation assays. It effectively degrades IDO1 in human glioblastoma cell lines U87 and GBM43, with DC50 values of 7.1 nM and 11.8 nM, respectively, as demonstrated in Western blot assays. This compound is valuable for research into various malignancies, including glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer.

Cat. No.

A75734

CAS No.

2759420-43-2

NU223612

NU223612 is a selective PROTAC designed to target and degrade indoleamine 2,3-dioxygenase 1 (IDO1) through CRBN-mediated proteasomal degradation, exhibiting a Kd of 640 nM. With a binding affinity for CRBN of 290 nM, NU223612 effectively reduces IDO1 protein levels, making it a valuable tool in the study of immune modulation and tumor microenvironments. Additionally, NU223612 demonstrates the ability to cross the blood-brain barrier, enhancing its potential utility in neurobiological research.

Cat. No.

A76594

CAS No.

2975664-37-8

PROTAC MALT1 Degrader-1

PROTAC MALT1 Degrader-1 is a selective degrader targeting MALT1 through the use of the PROTAC (proteolysis targeting chimera) technology. This compound facilitates the ubiquitination and subsequent proteasomal degradation of MALT1, making it a valuable tool for studies focused on lymphoma and related malignancies. Its mechanism of action enables the investigation of MALT1's role in cellular processes and therapeutic strategies for lymphoma treatment.

Cat. No.

A76719

CAS No.

2241669-05-4

Mitochondria degrader-1

Mitochondria Degrader-1 is a potent compound that targets the degradation of damaged mitochondria through an autophagy-mediated mechanism. This reagent induces the selective removal of dysfunctional mitochondria, making it highly relevant for studying neurodegenerative diseases, cancer, inflammatory diseases, age-related conditions, metabolic disorders, mitochondrial pathologies, and Down syndrome. Mitochondria Degrader-1 serves as a valuable tool in research focused on enhancing mitochondrial quality control and exploring therapeutic strategies for mitochondrial dysfunction-related diseases.

Cat. No.

A77255

CAS No.

3063346-83-5

LRK-4189

LRK-4189 is an orally active degrader of the lipid kinase PIP4K2C, primarily targeting type 1 immune activation. This compound effectively induces degradation of PIP4K2C, thereby triggering the interferon signaling pathway in microsatellite-stable colorectal cancer cells. LRK-4189 enhances immunogenic tumor cell death and sensitizes tumors to natural killer (NK) cell-mediated cytotoxicity and dendritic cell phagocytosis. This reagent is valuable for research focused on therapies for microsatellite-stable colorectal cancer.

Cat. No.

A77626

CAS No.

3093767-34-8

CQ627

CQ627 is a molecular glue that specifically targets the degradation of RIOK2 through the ubiquitin-proteasome system (UPS). It efficiently recruits the E3 ubiquitin ligase RNF126, resulting in a DC50 value of 410 nM for RIOK2 degradation in the MOLT4 leukemia cell line. CQ627 induces apoptosis and causes cell cycle arrest in the G2/M phase, exhibiting antiproliferative effects across various cancer cell lines. Additionally, it demonstrates significant in vivo anticancer activity in a MOLT4 xenograft mouse model, highlighting its potential for cancer research applications.

Cat. No.

A78951

CAS No.

2919475-43-5

PROTAC mHTT Degrader-1

PROTAC mHTT Degrader-1 targets mutant huntingtin (mHTT) through a PROTAC mechanism, effectively penetrating the blood-brain barrier. This compound selectively binds to pathogenic mHTT aggregates and recruits Cereblon (CRBN), leading to the ubiquitination and subsequent proteasomal degradation of mHTT. Research indicates that PROTAC mHTT Degrader-1 mitigates mHTT-induced cytotoxicity and neuroinflammation. In preclinical studies involving the R6/2 Huntington's disease mouse model, it has demonstrated the ability to decrease cerebral protein aggregation, enhance body weight, improve motor coordination, and increase survival rates. This reagent is pivotal for investigating PROTAC therapies in Huntington's disease and other neurodegenerative conditions.

Cat. No.

A79156

CAS No.

3068938-30-4

NEURL1B-IN-1

NEURL1B-IN-1 is a potent NEURL1B degrader with a Kd value of 46.2 nM. By specifically binding to Arg422 in the NHR2 domain of NEURL1B, this compound promotes autoubiquitination and subsequent proteasomal degradation of NEURL1B, effectively disrupting its interaction with DLL1 and inhibiting the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis while also inhibiting the migration of hepatocellular carcinoma cells, making it a valuable tool for research in hepatocellular carcinoma.

Cat. No.

A79172

CAS No.

919023-94-2

SM875

SM875 is a potent degrader of the cellular prion protein (PrP), exhibiting an IC50 of 7.87 μM. It selectively targets PrP folding intermediates and facilitates their degradation via the autophagy-lysosomal pathway. Notably, SM875 acts exclusively on nascent, immature PrP molecules, showing no impact on the mature form. This compound holds promise for inhibiting prion replication and is valuable for research into neurodegenerative diseases, particularly prion disorders.