PROTAC Degrader

Cat. No.

A24420

CAS No.

2768610-97-3

MS41

MS41 is a selective PROTAC degrader of eleven-nineteen leukemia (ENL), with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). MS41 effectively inhibits the proliferation of ENL-dependent leukemia cells, induces G1 phase cell cycle arrest, and promotes apoptosis. It reduces chromatin occupancy of the ENL-associated transcription elongation complex, thereby suppressing oncogenic gene expression and leukemia progression.

Cat. No.

A24447

CAS No.

2769753-47-9

DB0614

DB0614 is a PROTAC molecule utilizing a cereblon ligand, designed as a selective and potent degrader of NEK9 and other kinases. It induces the degradation of multiple kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1–3, MAP4K5, MAPK14, MAPK7–9, MAPKAPK2/3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1/3, SIK2/3, STK35, TNK2, and ULK1. DB0614 is suitable for research involving diseases or disorders driven by aberrant kinase activity.

Cat. No.

A24451

CAS No.

2769141-82-2

SR-1114

SR-1114 is a first-in-class PROTAC degrader targeting ENL. It induces rapid, cereblon (CRBN)-dependent degradation of ENL with DC₅₀ values of 150 nM in MV4;11 cells, 311 nM in MOLM-13 cells, and 1.65 μM in OCI/AML-2 cells.

Cat. No.

A24452

CAS No.

2757422-79-8

ARD-2585

ARD-2585 is an exceptionally potent, orally active PROTAC degrader of the androgen receptor (AR), designed to selectively and efficiently induce AR degradation for potential therapeutic applications.

Cat. No.

A24453

CAS No.

2414418-49-6

Pomalidomide-C3-adavosertib

Pomalidomide-C3-adavosertib is a rapid and selective PROTAC degrader of Wee1, with an IC₅₀ of 3.58 nM. It exhibits anti-proliferative activity against cancer cells and induces apoptosis.

Cat. No.

A24495

CAS No.

2984505-88-4

AK-1690

AK-1690 is a potent and selective PROTAC degrader of STAT6. It reduces STAT6 protein levels in cells with a DC₅₀ of 1 nM and effectively depletes STAT6 in mouse tissues. AK-1690 is suitable for cancer research involving STAT6-driven pathways.

Cat. No.

A24496

CAS No.

2769753-69-5

DD-03-156

Synonyms: (S,R,S)-AHPC-Me-PEG2-dabrafenib

DD-03-156 is a potent and selective degrader of CDK17 and LIMK2. It exhibits high selectivity and potency, making it a strong candidate for the development of a chemical probe targeting CDK17 degradation.

Cat. No.

A24498

CAS No.

3033993-13-1

CST626

CST626 (Compound 9) is a pan-IAP degrader PROTAC that targets and degrades inhibitor of apoptosis proteins XIAP, cIAP1, and cIAP2 in MM.1S cells, with DC₅₀ values of 0.7 nM, 2.4 nM, and 6.2 nM, respectively.

Cat. No.

A24499

CAS No.

2769753-59-3

DB-0646

DB-0646 is a PROTAC-based multi-kinase degrader designed to target and degrade multiple kinase proteins. It is suitable for research involving kinase signaling pathways and related disease models.

Cat. No.

A24501

CAS No.

2828438-38-4

LC-MB12

LC-MB12 is an orally active PROTAC compound that targets FGFR2 degradation, with a DC₅₀ of 11.8 nM. It consists of the FGFR2 inhibitor BGJ398, a PROTAC linker, and a cereblon (CRBN) ligand. LC-MB12 effectively inhibits FGFR2 signaling in gastric cancer cells and exhibits antitumor activity.

Cat. No.

A24502

CAS No.

2864408-92-2

GBD-9

GBD-9 is a dual-action degrader that targets both BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). It acts as a PROTAC to promote BTK degradation and functions as a molecular glue to induce GSPT1 degradation. GBD-9 exhibits significant antiproliferative activity in cancer cells, making it a promising candidate for cancer research.

Cat. No.

A24577

CAS No.

2750830-09-0

Luxdegalutamide (ARV-766)

Synonyms: ARV-766

Luxdegalutamide (ARV-766) is an orally active proteolysis-targeting chimera (PROTAC) designed to selectively degrade the androgen receptor (AR), including clinically relevant resistance-associated mutants such as T878A, H875Y, and L702H. By inducing AR ubiquitination and proteasomal degradation, Luxdegalutamide effectively suppresses AR signaling and exhibits potent antitumor activity. It is a promising therapeutic agent and research tool for studying castration-resistant prostate cancer (CRPC) and mechanisms of AR-driven oncogenesis.

Cat. No.

A24607

CAS No.

2704617-96-7

CFT8634

CFT8634 is an orally bioavailable PROTAC that targets the E3 ubiquitin ligase CRBN to degrade BRD9. This heterobifunctional molecule effectively inhibits the growth of tumor cells reliant on BRD9, making it a valuable tool for researching synovial sarcoma and SMARCB1-deficient solid tumors. CFT8634 facilitates targeted degradation through its unique binding properties, offering a strategic approach to investigate the role of BRD9 in SMARCB1-related cancers, including malignant rhabdoid tumors.

Cat. No.

A24661

CAS No.

2364367-27-9

PROTAC B-Raf degrader 1

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) that facilitates the degradation of B-Raf through a Cereblon ligand. This compound demonstrates significant anti-cancer activity, making it a valuable tool for cancer research. It is particularly useful in studies investigating B-Raf-mediated signaling pathways and therapeutic strategies targeting oncogenic mutations in B-Raf.

Cat. No.

A24684

CAS No.

2938169-99-2

PROTAC K-Ras Degrader-4

PROTAC K-Ras Degrader-4 specifically targets and degrades mutant KRAS proteins, including KRASG12D and KRASG12V, with DC50 values of 1 nM and 13 nM, respectively. By inhibiting the MAPK signaling pathway, this compound serves as a powerful tool for studying the functional implications of KRAS mutations in cancer biology. Research applications include elucidating the role of KRAS in tumorigenesis and evaluating the therapeutic potential of targeting this oncogene in various malignancies.

Cat. No.

A24686

CAS No.

2785323-62-6

PROTAC-O4I2

PROTAC-O4I2 is a targeted protein degraders (PROTAC) that specifically degrades splicing factor 3B1 (SF3B1). It demonstrates an IC50 value of 0.244 μM for inducing FLAG-SF3B1 degradation in K562 cells. Additionally, PROTAC-O4I2 promotes cellular apoptosis in K562 wild-type cells, making it a valuable tool for studying the functional role of SF3B1 in various biological contexts. This compound is suitable for investigating the therapeutic potential of SF3B1 modulation in cancer research.

Cat. No.

A24688

CAS No.

2913161-19-8

ACBI2

ACBI2 is a potent VHL PROTAC designed for the targeted degradation of SMARCA2. With an EC50 of 7 nM and a DC50 of 1 nM in RKO cells, ACBI2 selectively modulates SMARCA2 levels, making it a valuable tool for studying SMARCA2-related pathways. This compound is particularly relevant in lung cancer research, facilitating investigations into therapeutic strategies targeting SMARCA2 degradation.

Cat. No.

A24691

CAS No.

2767440-24-2

PROTAC AR-V7 degrader-1

PROTAC AR-V7 degrader-1 is a selective degrader targeting the androgen receptor variant 7 (AR-V7) through the PROTAC mechanism. With a DC50 of 0.32 μM in 22Rv1 cells, this compound demonstrates potent inhibition of tumor cell proliferation and exhibits significant anti-tumor activity. It is particularly relevant for research applications focusing on prostate cancer and can aid in the development of targeted therapeutic strategies.

Cat. No.

A24692

CAS No.

2855085-25-3

MS8815

MS8815 is a selective enhancer of the enhancer of zeste homolog 2 (EZH2) and functions as a PROTAC degrader. With an IC50 value of 8.6 nM, MS8815 demonstrates potent inhibitory activity against EZH2. This compound is valuable for research applications focused on triple-negative breast cancer (TNBC) and other conditions influenced by EZH2 activity.

Cat. No.

A24693

CAS No.

2821793-99-9

Setidegrasib

Synonyms: ASP-3082; KRAS G12D inhibitor 17

Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors.

Cat. No.

A24694

CAS No.

2851885-95-3

ARV-393

ARV-393 is a potent BCL6 PROTAC degrader that facilitates the ubiquitination and subsequent proteasomal degradation of BCL6. This compound exhibits significant biological activity and is particularly relevant for research focused on advanced non-Hodgkin lymphoma. Its ability to modulate protein levels through targeted degradation makes it a valuable tool for elucidating BCL6-related pathways in cancer biology.

Cat. No.

A24701

CAS No.

2509359-75-3

CP5V

CP5V is a PROTAC that targets Cdc20 for degradation through the recruitment of the von Hippel-Lindau (VHL) complex. By facilitating the ubiquitination of Cdc20, CP5V promotes proteasomal degradation, leading to mitotic inhibition. This compound has significant applications in research focused on cancer cell proliferation and cell cycle regulation.

Cat. No.

A24702

CAS No.

2789678-92-6

SJ10542

SJ10542 is a potent and selective PROTAC degrader targeting JAK2 and JAK3. With DC50 values of 14 nM for JAK2 and 11 nM for JAK3 in patient-derived xenograft cells (PDX), SJ10542 demonstrates significant antitumor activity. This compound is valuable for research in hematological malignancies and autoimmune diseases, facilitating the exploration of targeted degradation mechanisms in these therapeutic areas.

Cat. No.

A24707

CAS No.

2409538-70-9

GAL-02-221

Synonyms: PROTAC BRD4 Degrader-5

GAL-02-221 is a PROTAC designed to target and degrade BRD4 through ligands that recruit von Hippel-Lindau (VHL) E3 ligase. This compound effectively promotes the degradation of BRD4 in both HER2-positive and negative breast cancer cell lines, demonstrating potential utility in the study of tumor biology and therapeutic approaches. Its ability to selectively eliminate BRD4 highlights its relevance in cancer research and provides a valuable tool for investigating mechanisms of oncogenesis and treatment resistance.

Cat. No.

A24709

CAS No.

3031353-59-7

MS159

MS159 is a potent PROTAC degrader targeting nuclear receptor binding SET domain protein 2 (NSD2). It effectively inhibits tumor cell growth, making it a valuable tool for investigating the biological functions of NSD2 in various health and disease contexts. This compound serves as an important resource for researchers studying the therapeutic potential of NSD2 modulation.