PROTAC Degrader

Cat. No.

A23907

CAS No.

1973403-00-7

ARCC-4

ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research.

Cat. No.

A23908

CAS No.

2064175-41-1

FKBP12 PROTAC dTAG-13

dTAG-13 is a PROTAC-based heterobifunctional degrader that selectively targets FKBP12^F36V fused in-frame to a protein of interest. By engaging both FKBP12^F36V and the cereblon (CRBN) E3 ligase, dTAG-13 induces efficient and selective degradation of FKBP12^F36V-tagged proteins, making it a valuable tool for conditional protein knockdown studies.

Cat. No.

A23909

CAS No.

2222112-77-6

Bavdegalutamide (ARV-110)

Synonyms: ARV-110

Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer.

Cat. No.

A23910

CAS No.

2225938-17-8

MS1943

MS1943 is an orally active, PROTAC-based selective degrader of EZH2 that effectively reduces cellular EZH2 levels. It exhibits strong anticancer activity, showing cytotoxic effects in various triple-negative breast cancer (TNBC) cell lines while sparing normal cells. MS1943 maintains high potency in inhibiting EZH2 methyltransferase activity (IC₅₀ = 120 nM) and demonstrates high selectivity for EZH2, making it a promising candidate for epigenetic and cancer research.

Cat. No.

A23911

CAS No.

2225938-86-1

MS177

MS177 is a fast-acting and effective PROTAC degrader targeting EZH2. It comprises a cereblon (CRBN) ligand, a linker, and the potent EZH2 enzymatic inhibitor C24 (IC₅₀: 12 nM). MS177 efficiently depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes, leading to inhibition of leukemia cell proliferation, induction of apoptosis, and cell cycle arrest. It is a valuable tool for epigenetic and cancer research.

Cat. No.

A23912

CAS No.

2229711-68-4

Vepdegestrant (ARV471)

Synonyms: ARV471

Vepdegestrant (ARV-471) is an orally bioavailable PROTAC designed to target and degrade the estrogen receptor (ER). It is being developed for the treatment of patients with locally advanced or metastatic ER+/HER2− breast cancer, offering a novel approach to overcome endocrine resistance through targeted ER degradation.

Cat. No.

A23913

CAS No.

2229974-83-6

XY028-140 (MS140)

Synonyms: MS140

XY028-140 (MS140) is a highly potent and selective dual-function compound that acts as both a CDK4/6 kinase inhibitor and a PROTAC degrader. By combining kinase inhibition with targeted protein degradation, MS140 provides an effective approach for disrupting CDK4/6-mediated cell cycle regulation, making it a valuable tool for cancer research.

Cat. No.

A23914

CAS No.

2250025-88-6

TL12-186

TL12-186 is a cereblon-dependent PROTAC degrader with broad-spectrum activity against multiple kinases, including CDKs, BTK, FLT3, Aurora kinases, TEC, ULK, and ITK. It inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC₅₀ values of 73 nM and 55 nM, respectively, making it a valuable tool for studying kinase-driven signaling pathways and cancer biology.

Cat. No.

A23915

CAS No.

2271035-37-9

FC-11

FC-11 is a highly potent PROTAC degrader targeting focal adhesion kinase (FAK), with a DC₉₀ of 1 nM. It offers a powerful tool for investigating FAK-mediated signaling pathways and holds potential for cancer research and therapeutic development.

Cat. No.

A23916

CAS No.

2349356-09-6

BSJ-03-204

BSJ-03-204 is a potent and selective PROTAC degrader targeting CDK4 and CDK6, constructed by linking Palbociclib to a cereblon ligand. It exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, without inducing degradation of IKZF1 or IKZF3. BSJ-03-204 demonstrates strong anti-cancer activity and is a valuable tool for cell cycle and oncology research.

Cat. No.

A23917

CAS No.

2349356-39-2

BSJ-04-132

BSJ-04-132 is a potent and selective Ribociclib-based PROTAC degrader targeting CDK4, constructed using ligands for cereblon and CDK. It exhibits IC₅₀ values of 50.6 nM for CDK4/D1 and 30 nM for CDK6/D1, while sparing CDK6 and IKZF1/3 from degradation. BSJ-04-132 demonstrates anti-cancer activity and is a valuable tool for cell cycle and oncology research.

Cat. No.

A23918

CAS No.

2365478-58-4

HaloPROTAC-E

HaloPROTAC-E is a potent and selective PROTAC designed to degrade Halo-tagged endoplasmic reticulum-localized proteins, including SGK3 and VPS34, with a DC₅₀ of 3–10 nM. It effectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) when Halo-tagged, leading to inhibition of autophagy. HaloPROTAC-E is a valuable tool for conditional protein degradation and autophagy research.

Cat. No.

A23919

CAS No.

2375564-55-7

ACBI1

ACBI1 is a potent and cooperative PROTAC degrader targeting SMARCA2, SMARCA4, and PBRM1, with DC₅₀ values of 6 nM, 11 nM, and 32 nM, respectively. It exhibits strong anti-proliferative activity and induces apoptosis, making it a valuable tool for studying chromatin remodeling and cancer therapeutics.

Cat. No.

A23920

CAS No.

2378258-52-5

PROTAC K-Ras Degrader-1

PROTAC K-Ras Degrader-1 (Compound 518) is a cereblon-based PROTAC that selectively degrades K-Ras, achieving ≥70% degradation efficiency in SW1573 cells. It serves as a valuable tool for studying K-Ras-driven signaling pathways and potential therapeutic strategies in cancer research.

Cat. No.

A23921

CAS No.

2380274-50-8

AU-15330

AU-15330 is a PROTAC degrader targeting the SWI/SNF chromatin remodeling ATPase subunits SMARCA2 and SMARCA4. It effectively suppresses tumor growth in prostate cancer xenograft models and enhances the therapeutic efficacy of the AR antagonist enzalutamide. AU-15330 also induces remission in castration-resistant prostate cancer models, demonstrating strong antitumor activity with a favorable safety profile.

Cat. No.

A23922

CAS No.

2381320-35-8

PROTAC SGK3 degrader-1 (SGK3-PROTAC1)

Synonyms: SGK3-PROTAC1

SGK3-PROTAC1 is a PROTAC molecule designed to selectively degrade SGK3 by linking the 308-R SGK inhibitor to the VHL-binding ligand VH032. Through recruitment of the VHL E3 ligase, SGK3-PROTAC1 induces proteasomal degradation of SGK3, providing a targeted approach for studying SGK3 function in cellular signaling and disease.

Cat. No.

A23923

CAS No.

2407452-77-9

MS67

MS67 is a highly potent and selective PROTAC degrader of WD40 repeat domain protein 5 (WDR5), exhibiting minimal activity against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. Its strong anticancer activity highlights its utility as a targeted tool for studying WDR5-related epigenetic regulation and cancer therapy.

Cat. No.

A23924

CAS No.

2408641-24-5

PROTAC CDK2/9 Degrader-1

PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual PROTAC degrader targeting CDK2 (DC₅₀ = 62 nM) and CDK9 (DC₅₀ = 33 nM), constructed by linking a CDK inhibitor to a cereblon ligand. It effectively inhibits PC-3 prostate cancer cell proliferation (IC₅₀ = 0.12 µM) by inducing cell cycle arrest in the S and G2/M phases, making it a valuable tool for cancer and cell cycle research.

Cat. No.

A23925

CAS No.

2416131-46-7

Zelebrudomide (NX-2127)

Synonyms: NX-2127

Zelebrudomide (NX-2127) is a novel, potent BTK degrader that induces proteasomal degradation through targeted ubiquitination, rather than direct inhibition. In addition to degrading BTK, Zelebrudomide (NX-2127) enhances immune responses by stimulating T cell activation and increasing IL-2 production in primary human T cells, supporting its potential in cancer and immunotherapy research.

Cat. No.

A23926

CAS No.

2417097-18-6

JQAD1

JQAD1 is a CRBN-dependent PROTAC selectively targeting EP300 for degradation. It effectively reduces EP300 protein levels and H3K27ac histone acetylation, resulting in apoptosis. JQAD1 is a valuable tool for investigating EP300 function and epigenetic regulation in cellular processes.

Cat. No.

A23927

CAS No.

2417371-71-0

GNE-987

GNE-987 is a highly potent PROTAC degrader of BRD4, composed of a BET inhibitor, a von Hippel-Lindau (VHL) ligand, and a ten-methylene linker. It binds both BD1 and BD2 bromodomains of BRD4 with low nanomolar affinity (IC₅₀ = 4.7 and 4.4 nM) and induces BRD4 degradation with a DC₅₀ of 0.03 nM in EOL-1 AML cells. GNE-987 is also suitable for use in PROTAC–Antibody Conjugates (PAC), making it a valuable tool for targeted protein degradation and epigenetic cancer research.

Cat. No.

A23928

CAS No.

2429877-44-9

SD-36

SD-36 is a selective PROTAC degrader of STAT3 that induces potent degradation of STAT3 protein both in vitro and in vivo, with minimal impact on other STAT family members. By suppressing STAT3-driven transcriptional programs, SD-36 inhibits the proliferation of acute myeloid leukemia and anaplastic large-cell lymphoma cells through cell cycle arrest and apoptosis. In xenograft mouse models, SD-36 achieves complete and sustained tumor regression at well-tolerated doses, making it a promising tool for cancer research and targeted therapy development.

Cat. No.

A23929

CAS No.

2432994-31-3

KT-474

Synonyms: PROTAC IRAK4 degrader-7; KYM-001

KT-474 (SAR444656) is a selective small-molecule PROTAC degrader of IRAK4, under development for the treatment of TLR/IL-1R–mediated autoimmune diseases. It effectively suppresses R848 (TLR7/8)- and LPS-induced IL-6 and IL-8 production in peripheral blood mononuclear cells (PBMCs), highlighting its potential as an anti-inflammatory therapeutic.

Cat. No.

A23930

CAS No.

2446928-30-7

Gridegalutamide (BMS-986365)

Synonyms: CC-94676

BMS-986365 (CC-94676) is an orally active, selective PROTAC degrader targeting the androgen receptor (AR), including AR mutants. It functions via cereblon (CRBN)-mediated ubiquitination and proteasomal degradation of AR. BMS-986365 exhibits strong in vivo efficacy by suppressing AR signaling and inhibiting tumor growth in advanced prostate cancer models, making it a promising candidate for therapeutic development.

Cat. No.

A23931

CAS No.

2484739-25-3

dCBP-1

dCBP-1 is a potent and selective heterobifunctional PROTAC degrader of p300/CBP, utilizing a cereblon ligand for E3 ligase recruitment. It effectively eliminates oncogenic enhancer activity driving MYC expression and demonstrates strong cytotoxicity against multiple myeloma cells, making it a valuable tool for epigenetic and cancer research.