PROTAC Degrader

Cat. No.

A24006

CAS No.

2222635-92-7

MI-389

MI-389 is a PROTAC degrader targeting the translation termination factor GSPT1. Its activity relies on recruitment of the CRL4^CRBN E3 ubiquitin ligase complex to induce selective degradation of GSPT1. MI-389 effectively disrupts a critical dependency shared across multiple acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cell lines, making it a promising therapeutic candidate for hematologic malignancies characterized by GSPT1 dependence.

Cat. No.

A24007

CAS No.

2632305-36-1

ARD-1676

ARD-1676 is an orally bioavailable PROTAC degrader of the androgen receptor (AR), composed of an AR-binding ligand and a cereblon-recruiting moiety. It effectively induces AR degradation both in vitro and in vivo, and demonstrates significant antitumor activity by inhibiting VCaP prostate cancer xenograft growth in mouse models. ARD-1676 represents a promising therapeutic strategy for targeting AR-driven malignancies.

Cat. No.

A24008

CAS No.

2742732-92-7

YX968

YX968 is a potent and selective PROTAC degrader targeting histone deacetylases HDAC3 and HDAC8, with DC₅₀ values of 1.7 nM and 6.8 nM, respectively. By inducing degradation of these epigenetic regulators, YX968 promotes apoptosis and exhibits significant antitumor activity, representing a promising therapeutic strategy for cancers driven by aberrant HDAC3/8 activity.

Cat. No.

A24091

CAS No.

3058483-58-9

PROTAC YAP degrader-1

PROTAC YAP degrader-1 (compound YZ-6) is a bifunctional molecule designed to selectively degrade Yes-associated protein (YAP), a key effector of the Hippo signaling pathway involved in cell proliferation, survival, and tumorigenesis. In addition to promoting proteasomal degradation of YAP, it also inhibits YAP's nuclear localization, thereby impairing its transcriptional co-activator functions.YZ-6 is composed of two main components:Target protein ligand: NSC682769 and E3 ubiquitin ligase recruiter with linker: (R,S,R)-AHPC-PEG2-C2-Boc which recruits the VHL E3 ligase complex. The linker used in the PROTAC design is Acid-PEG2-C2-Boc, facilitating optimal spatial orientation for ternary complex formation. The demethylated analog Demethyl-NSC682769 serves as a target ligand activity control. PROTAC YAP degrader-1 represents a novel tool for functional YAP inhibition and offers potential therapeutic applications in YAP-driven cancers and fibrotic diseases.

Cat. No.

A24092

CAS No.

2417370-90-0

PROTAC BRD4 Degrader-12

PROTAC BRD4 Degrader-12 (compound 9c) is a bifunctional molecule designed to target and degrade the bromodomain-containing protein BRD4 by recruiting the von Hippel–Lindau (VHL) E3 ubiquitin ligase. It functions as a highly potent degrader, with a DC₅₀ of 0.39 nM and 0.24 nM when conjugated to STEAP1 and CLL1 antibodies, respectively, enabling targeted delivery and degradation of BRD4 in PC3 prostate cancer cells.

Cat. No.

A24093

CAS No.

2772612-96-9

MS9449

MS9449 is a potent PROTAC-based degrader of the epidermal growth factor receptor (EGFR), exhibiting strong binding affinities with K\_d values of 17 nM for wild-type EGFR and 10 nM for the L858R mutant. It effectively induces degradation of mutant EGFR proteins via both the ubiquitin–proteasome system (UPS) and the autophagy–lysosome pathway, enabling dual-pathway clearance. MS9449 shows strong antiproliferative activity in non-small cell lung cancer (NSCLC) cells, making it a valuable compound for anticancer research, particularly in EGFR-driven tumors.

Cat. No.

A24094

CAS No.

2767427-87-0

Anti-inflammatory agent 70

Synonyms: N-Me-SP23

Anti-inflammatory agent 70 (N-Me-SP23) is a PROTAC-based degrader targeting the STING (stimulator of interferon genes) protein, a key regulator of innate immune and inflammatory responses. By promoting STING degradation, N-Me-SP23 effectively inhibits the STING signaling pathway, leading to reduced downstream inflammatory cytokine production. This compound exhibits notable anti-inflammatory activity and holds potential for therapeutic research in STING-associated autoimmune and inflammatory disorders.

Cat. No.

A24095

CAS No.

2573298-13-0

KTX-582

KTX-582 is a potent heterobifunctional PROTAC degrader that targets interleukin-1 receptor–associated kinase 4 (IRAK4) and the transcription factor Ikaros, with DC₅₀ values of 4 nM and 5 nM, respectively. It induces apoptosis in MYD88^L265P-mutant diffuse large B-cell lymphoma (DLBCL) cells, a subtype characterized by constitutive IRAK4 signaling. In preclinical lymphoma models, KTX-582 effectively drives in vivo tumor regression, highlighting its therapeutic potential for MYD88-mutant hematologic malignancies.

Cat. No.

A24096

CAS No.

2230821-68-6

SJF-8240

SJF-8240 (PROTAC 7) is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade the receptor tyrosine kinase c-Met. It induces polyubiquitination and subsequent proteasomal degradation of c-Met, leading to effective inhibition of downstream signaling. SJF-8240 exhibits potent antiproliferative activity in GTL16 gastric cancer cells, with an IC₅₀ of 66.7 nM, making it a promising tool for targeted cancer therapy and c-Met–driven tumor research.

Cat. No.

A24097

CAS No.

2863634-97-1

SJ1008030 TFA

SJ1008030 (compound 8) TFA is a selective JAK2-targeting PROTAC that promotes proteasomal degradation of Janus kinase 2 (JAK2). It exhibits potent antiproliferative activity in MHH–CALL-4 leukemia cells, with an IC₅₀ of 5.4 nM. By effectively eliminating JAK2 protein rather than merely inhibiting its activity, SJ1008030 TFA represents a promising therapeutic strategy for JAK2-driven hematologic malignancies, particularly in leukemia research.

Cat. No.

A24098

CAS No.

2769753-18-4

SB1-G-187

SB1-G-187 is a multifunctional PROTAC designed as a multi-kinase degrader, capable of inducing the selective degradation of multiple kinase targets through the ubiquitin–proteasome system. In addition to its targeted degradation activity, SB1-G-187 features an alkyne functional group, enabling its use as a click chemistry reagent. It can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, allowing for versatile applications in chemical biology, such as probe development, conjugation, and target identification.

Cat. No.

A24099

CAS No.

2675490-92-1

MS39

MS-39 is a highly potent and selective PROTAC degrader specifically engineered to target mutant forms of the epidermal growth factor receptor (EGFR). It is constructed by conjugating the EGFR inhibitor gefitinib to a von Hippel–Lindau (VHL) E3 ligase ligand via a tailored linker. MS-39 exhibits strong binding affinity and efficient degradation of mutant EGFR proteins, offering a promising strategy for overcoming resistance in EGFR-driven cancers. Its design enables targeted proteasomal degradation rather than mere kinase inhibition, providing a novel approach to cancer therapy.

Cat. No.

A24100

CAS No.

2841308-96-9

PROTAC AR/AR-V7 degrader-1

PROTAC AR/AR-V7 Degrader-1 (27c) is a PROTAC-based dual degrader targeting both full-length androgen receptor (AR) and its splice variant AR-V7, which is implicated in resistance to androgen deprivation therapies. It exhibits DC₅₀ values of 2.67 μM for AR and 2.64 μM for AR-V7, effectively promoting their proteasomal degradation. By eliminating both isoforms, compound 27c induces apoptosis in AR-driven cancer cells, making it a promising therapeutic candidate for castration-resistant prostate cancer (CRPC) and other AR/AR-V7–dependent malignancies.

Cat. No.

A24101

CAS No.

2503018-29-7

INY-05-040

INY-05-040 is a potent and selective PROTAC degrader targeting all three isoforms of AKT (AKT1, AKT2, and AKT3). It induces rapid proteasomal degradation of AKT, effectively inhibiting downstream signaling pathways such as PI3K/AKT/mTOR, which are critical for cancer cell survival and proliferation. INY-05-040 demonstrates broad antiproliferative activity across 288 cancer cell lines, highlighting its potential as a powerful therapeutic agent for targeting AKT-driven malignancies.

Cat. No.

A24281

CAS No.

3053716-98-3

YJ1206

YJ1206 is an orally active and selective PROTAC degrader targeting CDK12 and CDK13, with an IC50 of 12.55 nM in VCaP cells. It induces DNA damage, promotes apoptosis, and leads to tumor regression in orthotopic WA74 patient-derived xenograft (PDX) models of resistant prostate cancer. Additionally, YJ1206 enhances antitumor efficacy when used in combination with AKT pathway inhibitors, highlighting its potential for combination therapy in advanced prostate cancer.

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.