PROTAC Degrader

Cat. No.

A24712

CAS No.

2719051-84-8

SIM1

SIM1 is a highly potent von Hippel-Lindau (VHL)-based trivalent PROTAC that specifically targets the degradation of BET family proteins, with a notable preference for BRD2 (IC50=1.1 nM; Kd=186 nM). This compound has demonstrated sustained anti-cancer activity, making it a valuable tool for researchers investigating the roles of BET proteins in oncogenesis and other related biological pathways. Its application in PROTAC-mediated protein degradation provides unique avenues for therapeutic intervention in cancers driven by BET overexpression.

Cat. No.

A24713

CAS No.

2375555-66-9

FKBP12 PROTAC RC32

Synonyms: RC32

FKBP12 PROTAC RC32 is a targeted protein degrader utilizing PROTAC technology to selectively degrade FKBP12. This compound combines Rapamycin, a well-characterized immunosuppressant, with a Cereblon E3 ubiquitin ligase ligand derived from Pomalidomide, facilitating the ubiquitination and subsequent proteasomal degradation of FKBP12. It serves as an important tool in research applications aimed at investigating the modulation of protein levels and the functional consequences of targeted degradation in various biological contexts.

Cat. No.

A24716

CAS No.

2458219-65-1

SHP2-D26

SHP2-D26 is a potent SHP2 degrader that functions as a PROTAC by facilitating the recruitment of the VHL-1 E3 ligase to the SHP2 protein. This dual-target mechanism efficiently induces the degradation of SHP2 in a neddylation- and proteasome-dependent manner. SHP2-D26 is valuable for research applications in understanding esophageal cancer and acute myeloid leukemia, providing insights into SHP2's role in these malignancies.

Cat. No.

A24717

CAS No.

2769753-23-1

SK-3-91

SK-3-91 is a multi-kinase degrader functioning through the ubiquitin biotinylation (E-STUB) pathway to induce the degradation of over 125 unique kinases. This PROTAC effectively reduces the levels of YTHDF2, contributing to the inhibition of cell proliferation and morphological alterations in treated cells. Its design facilitates the selective targeting and degradation of diverse kinases, making it a valuable tool for studying kinase function and exploring therapeutic applications in cancer research.

Cat. No.

A24718

CAS No.

2376137-05-0

MS21

MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A24719

CAS No.

2570251-68-0

HJM-561

HJM-561 is a selective EGFR PROTAC degrader that effectively targets and degrades EGFR mutations resistant to conventional therapies, such as Osimertinib. It demonstrates potent degradation activity against key triple mutations including Del19/T790M/C797S (DC50: 9.2 nM) and L858R/T790M/C797S (DC50: 5.8 nM). HJM-561's mechanism provides promising potential for anti-tumor applications in the treatment of EGFR-driven malignancies.

Cat. No.

A24720

CAS No.

2920415-08-1

PROTAC Bcl-xL degrader-2

PROTAC Bcl-xL Degrader-2 is a highly effective protein degrader targeting Bcl-xL, a member of the Bcl-2 family. Utilizing a von Hippel-Lindau ligand, this compound demonstrates a potent inhibition with an IC50 of 0.6 nM. It facilitates the selective degradation of Bcl-xL, making it a valuable tool for research in apoptotic processes and cancer therapy. Laboratory applications include studying the role of Bcl-xL in cell survival and investigating therapeutic strategies in Bcl-2-associated malignancies.

Cat. No.

A24722

CAS No.

2624313-16-0

dTAGV-1 hydrochloride

dTAGV-1 hydrochloride is a highly selective degrader targeting FKBP12F36V-tagged proteins through the PROTAC mechanism. This compound effectively induces the degradation of FKBP12F36V-Nluc in vivo, making it a valuable tool for studies involving targeted protein degradation. Its application in research facilitates the investigation of protein function, dynamics, and the development of therapies that exploit the proteolysis pathway.

Cat. No.

A24726

CAS No.

2916433-81-1

PROTAC GPX4 degrader-1

PROTAC GPX4 degrader-1 functions as a targeted protein degradation agent specifically for GPX4. It exhibits a DC50 of 0.03 μM in HT1080 cells, demonstrating potent activity in promoting the degradation of GPX4. This compound is applicable in research exploring the role of GPX4 in various cellular processes and the therapeutic potentials of targeting antioxidant defenses in disease models.

Cat. No.

A24727

CAS No.

2413035-41-1

SJF-0628

SJF-0628 is a RAF PROTAC degrader that facilitates the targeted degradation of BRAF protein in cancer cell lines, specifically in colorectal cancer models (Colo-205, LS-411N, HT-29, RKO) and the triple-negative breast cancer line DU-4475. This compound significantly reduces levels of phosphorylated MEK and ERK in DU-4475 cells, demonstrating notable anti-tumor activity. SJF-0628 is valuable for research studies focused on the mechanisms of colorectal cancer and triple-negative breast cancer.

Cat. No.

A24729

CAS No.

2439058-23-6

HDAC6 degrader-1

HDAC6 degrader-1 is a PROTAC degrader targeting HDAC6, exhibiting a DC50 value of 3.8 nM in MM.1S cells. This compound efficiently induces the degradation of HDAC6 through a bifunctional strategy, linking a ligand for the E3 ligase Pomalidomide with a ligand for the target protein Nexturastat A via a specialized linker. Its application is vital for investigating the role of HDAC6 in cellular processes and potential therapeutic effects in various diseases.

Cat. No.

A24730

CAS No.

2411085-89-5

MG-277

MG-277 is a PROTAC GSPT1 degrader that induces degradation of the translation termination factor GSPT1 via a Cereblon E3 ligase mechanism, with a DC50 of 1.3 nM. This compound exhibits potent anticancer activity, significantly inhibiting tumor cell growth in a p53-independent manner, demonstrating IC50 values of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells. MG-277 is a valuable tool for cancer research, particularly in studies involving protein degradation and cellular mechanisms of tumorigenesis.

Cat. No.

A24732

CAS No.

3004503-12-9

NUCC-0226272

NUCC-0226272 is a potent PROTAC that facilitates the targeted degradation of EZH2. This compound exhibits significant anti-proliferative effects, making it a valuable tool for investigating the role of EZH2 in cancer biology. Its application in cancer research provides insights into potential therapeutic strategies for malignancies associated with EZH2 dysregulation.

Cat. No.

A24733

CAS No.

2951015-29-3

YD23

YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 and H1975 cell lines, respectively. This reagent induces the degradation of SMARCA2, exhibiting synthetic lethality towards SMARCA4-deficient cells and selectively inhibiting growth in SMARCA4 mutant lung cancer cells. YD23 also reduces chromatin accessibility in SMARCA4 deficient cells, impacting genes associated with cell cycle and growth regulation. It is a valuable tool for researching non-small cell lung cancer (NSCLC) and evaluating tumor growth in SMARCA4-mutant xenograft models.

Cat. No.

A24734

CAS No.

2365172-19-4

XZ739

XZ739 is a Cereblon-dependent PROTAC degrader targeting BCL-XL, a member of the Bcl-2 protein family. Demonstrating a DC50 value of 2.5 nM in MOLT-4 cells after 16 hours of treatment, XZ739 effectively induces cell death through caspase-mediated apoptosis. This compound is valuable for research applications focused on studying apoptosis, cancer therapeutics, and the modulation of protein degradation pathways.

Cat. No.

A24735

CAS No.

2384184-40-9

KB02-SLF

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader designed to facilitate targeted protein degradation. It achieves this by covalently modifying DCAF16, an E3 ligase, thereby enhancing the stability of FKBP12 degradation within biological systems. The compound consists of a molecular glue linking the ubiquitin E3 ligase ligand KB02 with SLF, enabling efficient degradation of FKBP12 for various research applications in protein regulation and degradation pathways.

Cat. No.

A24820

CAS No.

3026420-38-9

PROTAC BRD4 Degrader-8

PROTAC BRD4 Degrader-8 is a proteolysis-targeting chimera (PROTAC) that engages both von Hippel-Lindau (VHL) and BRD4, exhibiting IC50 values of 1.1 nM for BRD4 BD1 and 1.4 nM for BRD4 BD2. This compound effectively promotes the degradation of BRD4 protein in PC3 prostate cancer cells, making it a valuable tool for research into BRD4-related signaling pathways and cancer therapeutics. Its high potency highlights its potential use in studying mechanisms of protein regulation and developing novel cancer treatments.

Cat. No.

A24821

CAS No.

2380000-55-3

β-NF-JQ1

β-NF-JQ1 is a PROTAC that targets bromodomain-containing (BRD) proteins by leveraging β-NF as a ligand for the Aryl Hydrocarbon Receptor (AhR) E3 ligase. This compound facilitates the degradation of BRD proteins through the recruitment of AhR, leading to effective protein knockdown. β-NF-JQ1 demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and the development of targeted therapeutic strategies.

Cat. No.

A24822

CAS No.

2832961-58-5

CBPD-268

CBPD-268 is a highly potent CBP/p300 PROTAC degrader, exhibiting a DC50 value of ≤ 0.03 nM. This compound effectively induces degradation of CBP/p300 and demonstrates significant inhibition of cell growth, showcasing its antitumor potential. CBPD-268 is particularly relevant for research into androgen receptor-positive prostate cancer, facilitating studies on novel therapeutic strategies.

Cat. No.

A24824

CAS No.

2451573-87-6

dTAGV-1-NEG

dTAGV-1-NEG is a diastereomer that acts as a heterobifunctional negative control for dTAGV-1, specifically targeted at FKBP12(F36V). This compound is utilized in research to study the selectivity and efficacy of FKBP12(F36V) degraders, helping to elucidate cellular mechanisms and pathways influenced by FKBP12 modulation. Its role as a control reagent makes it essential for validating experimental results in protein degradation studies.

Cat. No.

A24825

CAS No.

2740582-16-3

SHP2-D26 isomer-1

SHP2-D26 isomer-1 is an isoform of the SHP2-D26 degrader, designed specifically for targeted protein degradation applications. This compound does not induce degradation of SHP2 at concentrations ranging from 3 to 1000 nM. As a component of PROTAC technology, SHP2-D26 isomer-1 serves as a valuable tool for studying SHP2's role in signaling pathways and assessing the therapeutic potential of SHP2 modulation in various diseases.

Cat. No.

A24826

CAS No.

2924557-42-4

SNX7886

SNX7886 is a potent PROTAC degrader targeting CDK8 and CDK19. It effectively induces degradation of CDK8 and CDK19, achieving up to 90% and 80% degradation, respectively, in 293 cells. This compound is valuable for research applications in understanding the role of CDK8/19 in various biological processes and cancer pathways.

Cat. No.

A24827

CAS No.

2052306-13-3

PROTAC TBK1 degrader-2

PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases.

Cat. No.

A24828

CAS No.

3050872-59-5

MS8847

MS8847 is a powerful EZH2 PROTAC degrader that utilizes the E3 ligase von Hippel-Lindau (VHL) to promote the degradation of EZH2 through the ubiquitin-proteasome system. This compound demonstrates robust anti-proliferative effects in acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cell lines. MS8847 serves as a valuable tool for investigating the role of EZH2 in oncogenic signaling pathways and developing targeted therapies for EZH2-dependent malignancies.

Cat. No.

A24829

CAS No.

2769753-64-0

DB-3-291

DB-3-291 is a potent and selective PROTAC degrader targeting the protein CSK, exhibiting a Kd of 1 nM. This compound facilitates the degradation of CSK through its specific interaction with the E3 ligase, enabling in-depth studies of CSK-related biological pathways and providing insights into potential therapeutic strategies. It is valuable for researchers investigating targeted protein degradation and cancer biology.