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PROTAC Degrader

PROTAC degraders recruit an E3 ubiquitin ligase to a target protein so that the proteasome degrades it. Each proteolysis-targeting chimera (PROTAC) links a target-binding ligand to an E3 ligase ligand through a chemical linker. The approach was first described in 2001, and later work showed that small-molecule PROTACs can act catalytically, removing several target copies per molecule. Examples include the bromodomain and extra-terminal (BET) degraders dBET1, MZ1 and ARV-771, and the estrogen receptor degrader ERD-308. Degraders of anti-apoptotic proteins, such as PROTAC Mcl1 degrader-1, are also listed.

Cat. No.

A32566

CAS No.

3099825-86-9

PROTAC KSP degrader 1

PROTAC KSP Degrader 1 is a targeted protein degrader designed to selectively deplete kinesin spindle protein (KSP). This compound achieves a DC50 value of 114.8 nM for KSP degradation in HCT-116 cells and demonstrates a potent anti-proliferative effect with an IC50 of 10 nM. It effectively induces G2/M cell cycle arrest and triggers apoptosis in HCT-116 cells, exhibiting notable anti-tumor efficacy in relevant mouse models. This reagent serves as a valuable tool for investigating KSP's role in cancer biology and therapeutic approaches.

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Cat. No.

A32667

CAS No.

3064994-97-1

PROTAC CDK4/6/9 degrader 1

PROTAC CDK4/6/9 Degrader 1 is a targeted protein degradation agent that specifically degrades cyclin-dependent kinases CDK4, CDK6, and CDK9. This compound effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells by inducing G1 phase arrest, promoting apoptosis, and suppressing cellular migration and invasion. PROTAC CDK4/6/9 Degrader 1 serves as a valuable tool for studying the role of these kinases in TNBC and may support the development of novel therapeutic strategies aimed at this aggressive cancer subtype.

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Cat. No.

A32676

CAS No.

3055593-64-8

Gal-ARV-771

Gal-ARV-771 is a galactose-modified PROTAC prodrug designed to target SA-β-Gal-expressed cancer senescent cells for activation. Upon activation, Gal-ARV-771 releases ARV-771, which facilitates the selective degradation of the BRD4 protein via the ubiquitin-proteasome pathway in senescent cells. This compound has demonstrated the capability to induce apoptosis in senescent cancer cells, making it a valuable tool for cancer research focused on cellular senescence and therapeutic strategies targeting BRD4.

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Cat. No.

A32746

CAS No.

3098519-83-3

XM-U-14

XM-U-14 is a selective PROTAC degrader targeting USP7, demonstrating a DC50 of 0.74 nM for inducing USP7 degradation in the RS4;11 cell line. This compound effectively upregulates p53 and p21 levels and exhibits significant inhibition of acute lymphoblastic leukemia (ALL) cell proliferation, with IC50 values of 0.5 nM and 8.3 nM for RS4;11 and Reh cells, respectively. Additionally, XM-U-14 induces apoptosis and cell cycle arrest, ultimately inhibiting tumor growth, making it a valuable tool for cancer research and therapeutic exploration.

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Cat. No.

A32774

CAS No.

3095277-20-3

WRN-IN-20

WRN-IN-20 is a targeted WRN degrader known for its effective degradation of the Werner syndrome protein (WRN). This compound demonstrates significant degradation activity in various cell lines, including HCT-116 (DC50 = 1.7 µM), SW-48 (DC50 = 3.0 µM), and SW-480 (DC50 = 5.9 µM). WRN-IN-20 exhibits potent anti-proliferative, pro-apoptotic, migration-inhibiting, and DNA damage-inducing effects, particularly in MSI-H cancer cells. This reagent is suitable for research applications focused on cancer biology and therapeutic strategies involving WRN modulation.

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Cat. No.

A32863

CAS No.

3053537-06-4

RD-23

RD-23 is a selective RET PROTAC degrader that functions through the promotion of ubiquitination and subsequent degradation of the RETG810C mutation, exhibiting a DC50 value of 11.7 nM. This compound effectively inhibits downstream Shc signaling pathways and induces apoptosis in RET-related cancer models. RD-23 is a valuable tool for investigating the biological roles and therapeutic targeting of RET in oncology research.

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Cat. No.

A33243

CAS No.

2770470-20-5

PROTAC TYK2 degrader-1

PROTAC TYK2 degrader-1 (CPD-155) is a proteolysis-targeting chimera (PROTAC) that effectively degrades TYK2, achieving a degradation efficiency (Dmax) exceeding 60%. This compound utilizes a selective TYK2 ligand combined with a Cereblon ligand, linked through a proprietary structure. It is poised for applications in research focusing on autoimmune diseases and inflammatory disorders where TYK2 modulation is of interest.

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5 mg

$535.00

10 mg

$875.00

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Cat. No.

A33311

CAS No.

2863634-96-0

SJ1008030

SJ1008030 is a PROTAC compound designed to selectively degrade Janus kinase 2 (JAK2). This compound exhibits potent inhibitory activity against MHH–CALL-4 cell growth, with an IC50 of 5.4 nM. SJ1008030 is valuable for research applications focusing on leukemia, facilitating the study of JAK2-related pathways and therapeutic interventions.

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Cat. No.

A33334

CAS No.

3067695-20-6

PROTAC FLT3/JAK2/BRD4 Degrader-1

PROTAC FLT3/JAK2/BRD4 Degrader-1 is a potent PROTAC degrader that simultaneously targets FLT3, JAK2, and BRD4, exhibiting DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It demonstrates significant antiproliferative activity against MV4;11 cells with an IC50 of 0.79 nM, inducing apoptosis in these cells. Additionally, PROTAC FLT3/JAK2/BRD4 Degrader-1 shows marked anti-tumor efficacy in MV4;11 xenograft models in NOD SCID mice. This compound is valuable for research into acute myeloid leukemia (AML).

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Cat. No.

A33495

CAS No.

2504949-52-2

DGY-09-192

DGY-09-192 is a PROTAC degrader targeting FGFR1 and FGFR2, demonstrating DC50 values of 4.35 nM and 70 nM, respectively. This compound selectively degrades both wild-type FGFR1/2 and various FGFR2 fusion proteins, such as FGFR2-PHGDH and FGFR2-OPTN. By suppressing downstream FGFR signaling, DGY-09-192 effectively reduces the phosphorylation of key targets including FRS2 Y196 and ERK1/2 T202/Y204, making it a valuable tool for investigating FGFR-driven malignancies in both in vitro and in vivo studies.

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1 mg

$800.00

5 mg

$2,190.00

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Cat. No.

A33591

CAS No.

3037776-72-7

Leu-PEG1-Dasa

Leu-PEG1-Dasa is an efficient BCR-ABL PROTAC degrader that operates through the N-terminal canonical pathway, demonstrating a DC50 of 0.48 nM. This compound utilizes a single amino acid as the E3 ligase ligand and exhibits significant anti-proliferative effects on K562 cells. Leu-PEG1-Dasa is applicable in the research of chronic myeloid leukemia (CML) and provides insights into targeted degradation mechanisms in cancer therapy.

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Cat. No.

A33626

CAS No.

2489876-41-5

GMB-805

GMB-805 is a potent BCR-Abl PROTAC degrader, demonstrating a DC50 of 30 nM in K562 cells. It effectively induces antiproliferative activity, making it a valuable tool for studying chronic myeloid leukemia. Additionally, GMB-805 exhibits significant anti-tumor efficacy in vivo, coupled with a favorable safety profile, highlighting its potential for therapeutic development.

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Cat. No.

A33630

CAS No.

3037776-67-0

Arg-PEG1-Dasa

Arg-PEG1-Dasa is a mini-PROTAC designed to selectively degrade BCR-ABL, a key oncogenic driver in chronic myeloid leukemia. It demonstrates potent degradation efficacy with an EC50 of 0.85 nM, and exhibits significant antiproliferative activity in K562 cells, with an IC50 of 0.36 nM. This reagent is valuable for research applications focused on targeted therapies for BCR-ABL-driven malignancies.

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Cat. No.

A33633

CAS No.

2635386-55-7

P19As

P19As is a PROTAC degrader that targets the BCR-ABL fusion protein, exhibiting a DC50 value of approximately 200 nM for wild-type BCR-ABL. This compound effectively degrades the T315I mutant variant and demonstrates potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cell lines. P19As serves as a valuable tool for investigating therapeutic strategies in chronic myeloid leukemia and acute lymphoblastic leukemia.

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Cat. No.

A33635

CAS No.

2512843-74-0

P19P

P19P is a BCR-ABL PROTAC degrader that demonstrates a DC50 value of approximately 20 nM for wild-type BCR-ABL protein. It effectively degrades various drug-resistant mutants, including T315I, E255K, H396R, and V468F, and exhibits significant anti-proliferative activity in BaF3-BCR-ABL (T315I) cells, with an IC50 of 13.1 nM against ABL (T315I). P19P is suitable for research applications related to chronic myeloid leukemia and acute lymphoblastic leukemia while showing no inhibition of vascular lumen formation in HUVEC cells.

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Cat. No.

A33636

CAS No.

3033463-06-5

SIAIS100

SIAIS100 is a potent BCR-ABL PROTAC degrader, exhibiting a DC50 value of 2.7 nM. This compound facilitates the targeted degradation of the BCR-ABL fusion protein, making it an important tool in the study of chronic myeloid leukemia (CML). Its ability to induce proteolytic degradation offers valuable insights for therapeutic development and understanding disease mechanisms associated with CML.

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Cat. No.

A33640

CAS No.

2378581-37-2

SIAIS056

SIAIS056 is a BCR-ABL PROTAC degrader that effectively targets and degrades BCR-ABL fusion proteins, displaying a potent DC50 value of 0.18 nM. It inhibits the BCR-ABL signaling pathway in a time-dependent manner, leading to reduced phosphorylation of BCR-ABL as well as downstream effectors like STAT5 and CRKL in K562 cells. Additionally, SIAIS056 demonstrates the ability to degrade various BCR-ABL resistance mutations and exhibits significant anti-proliferative effects, resulting in marked tumor regression in K562 xenograft models. This compound is valuable for research in leukemia.

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Cat. No.

A33641

CAS No.

2635386-51-3

P22D

P22D is a BCR-ABL PROTAC degrader designed for targeted protein degradation, exhibiting a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. This compound effectively inhibits the proliferation of K562 cells harboring the wild-type BCR-ABL, but does not exhibit activity against BaF3-BCR-ABL (T315I) cells. P22D is valuable for research on chronic myeloid leukemia and acute lymphocytic leukemia, offering insights into the mechanisms of resistance and targeted therapies.

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Cat. No.

A33649

CAS No.

3037776-73-8

Phe-PEG1-Dasa

Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, demonstrating a DC50 value of 1.56 nM. This compound utilizes phenylalanine as the E3 ligase ligand and triggers the N-end rule pathway to facilitate the degradation of target proteins. Phe-PEG1-Dasa effectively suppresses the proliferation of K562 leukemia cells, making it a valuable tool for research into leukemia treatment strategies.

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Cat. No.

A33690

CAS No.

2892631-70-6

PF15

PF15 is a PROTAC designed to target FLT3 kinase through its ligands linked with CRBN. This highly selective FLT3-ITD degrader exhibits a DC50 of 76.7 nM, effectively inhibiting the proliferation of FLT3-ITD-positive cells. PF15 down-regulates the phosphorylation of FLT3 and STAT5, demonstrating significant anti-tumor activity in mouse models, making it a valuable tool for leukemia research.

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Cat. No.

A34249

CAS No.

3115765-45-9

dAurAB5

dAurAB5 is a dual PROTAC degrader targeting Aurora-A (DC50 = 8.8 nM) and Aurora-B (DC50 = 6.1 nM). It effectively induces the degradation of these kinases, leading to reduced N-Myc levels and decreased viability in IMR32 neuroblastoma cells. dAurAB5 also downregulates AAK1, PTK2, GAK, and TTK, making it a valuable tool for investigating the molecular mechanisms in neuroblastoma and related cancers.

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1 mg

$545.00

5 mg

$1,395.00

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Cat. No.

A34268

CAS No.

2471525-44-5

FAK PROTAC B5

FAK PROTAC B5 is a potent degrader targeting focal adhesion kinase (FAK) with an IC50 of 14.9 nM. This compound exhibits significant FAK degradation capabilities along with antiproliferative effects. Furthermore, it demonstrates notable plasma stability and moderate membrane permeability, effectively inhibiting cell migration and invasion. FAK PROTAC B5 is suitable for research applications focused on cancer biology and cellular signaling pathways.

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Cat. No.

A34271

CAS No.

2414478-45-6

BSJ-04-146

BSJ-04-146 is a selective PROTAC that targets focal adhesion kinase (FAK) for degradation, exhibiting an IC50 of 26 nM. It demonstrates rapid and robust degradation of FAK in cancer cells while maintaining high specificity across the proteome, and it induces prolonged degradation in murine models. The activity of BSJ-04-146 relies on the ubiquitin-proteasome system, making it a valuable tool for investigating pathways associated with pancreatic cancer and triple-negative breast cancer.

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Cat. No.

A34283

CAS No.

3054388-18-7

PROTAC TG2 Degrader-3

PROTAC TG2 Degrader-3 functions as a targeted protein degrader specifically for transglutaminase 2 (TG2). This compound effectively inhibits the adhesion and migration of ovarian cancer cells, making it a valuable tool for research focused on ovarian cancer biology and therapeutics. By facilitating the degradation of TG2, it provides insights into the modulation of cancer cell behavior and the potential development of novel treatments.

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Cat. No.

A34289

CAS No.

2341740-85-8

BI-0319

BI-0319 is a selective PROTAC degrader targeting PTK2/FAK, effectively promoting the degradation of these proteins. This compound has demonstrated the ability to reduce cancer cell viability, inhibit cellular proliferation, and curtail invasion, making it a valuable tool for cancer research, particularly in studies related to liver cancer. BI-0319 provides insights into therapeutic strategies focused on protein degradation in oncology.

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