PROTAC Degrader

Cat. No.

A30885

CAS No.

3105680-00-7

PROTAC XPO1 degrader-1

PROTAC XPO1 degrader-1 is a targeted protein degrader designed to selectively promote the degradation of XPO1. This compound demonstrates significant anti-proliferative effects, induces apoptosis, inhibits NF-κB signaling, and causes cell cycle arrest at the G1 phase. It is an important tool for researching hematological malignancies, offering insights into therapeutic strategies by modulating XPO1 levels.

Cat. No.

A30886

CAS No.

3081688-77-6

PROTAC SMARCA2/4 degrader-38

PROTAC SMARCA2/4 degrader-38 is a dual-targeted PROTAC degrader designed to promote the ubiquitination and subsequent degradation of the SMARCA2 and SMARCA4 proteins. With DC50 values of 3.0 nM and 4.0 nM for SMARCA2 and SMARCA4 respectively, this compound effectively blocks the G0/G1 cell cycle phase and induces apoptosis in cancer cells. It has significant potential for use in research focused on acute myeloid leukemia (AML) and other malignancies involving these chromatin remodeling factors.

Cat. No.

A30914

CAS No.

3010273-12-5

PROTAC ATR degrader-2

PROTAC ATR degrader-2 is a selective degrader targeting the ATR protein. It effectively induces degradation of ATR in acute myeloid leukemia (AML) cell lines MV-4-11 and MOLM-13, demonstrating DC50 values of 22.9 nM and 34.5 nM, respectively. This compound has an IC50 of 29.6 nM against ATR, while exhibiting minimal activity against ATM and PI3K. PROTAC ATR degrader-2 promotes apoptosis, causes DNA damage, and upregulates p53 expression, thereby inhibiting cancer cell proliferation. This reagent is suitable for research applications focused on understanding mechanisms in acute myeloid leukemia.

Cat. No.

A30993

CAS No.

3059333-98-8

SZU-B6

SZU-B6 is a SIRT6-protein-targeting chimeric degrader that achieves a DC50 of 45 nM and 154 nM in SK-HEP-1 and Huh-7 cell lines, respectively. It effectively inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cells. Additionally, SZU-B6 induces apoptosis and causes a cell cycle arrest in the G2/M phase in SK-HEP-1 cells, demonstrating notable antitumor efficacy in mouse models. This compound serves as a valuable tool for studying the functional roles of SIRT6 in cancer research.

Cat. No.

A31204

CAS No.

2378056-80-3

A947

A947 is a selective SMARCA2 proteolysis-targeting chimera (PROTAC) that functions as a potent degrader of SMARCA2. It exhibits a binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM, establishing its effectiveness in mediating targeted protein degradation. This compound has significant applications in cancer research, facilitating studies on the role of SMARCA2 in tumorigenesis and potential therapeutic interventions.

Cat. No.

A31312

CAS No.

491586-42-6

AN5777

AN5777 is a GSPT1 degrader that targets the ubiquitin-proteasome system to facilitate the degradation of GSPT1 protein. This compound has been shown to induce a G1 phase cell cycle arrest and promote apoptosis in cancer cells. AN5777 exhibits significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A31585

CAS No.

3092208-36-8

DFCI-002-06

DFCI-002-06 is an orally active PROTAC degrader targeting both HCK and BTK, demonstrating DC₅₀ values of 1.3 nM and 4.5 nM, respectively. This compound exhibits superior anti-tumor activity compared to a dual-target inhibitor, promoting apoptosis in cancer cells, particularly in MYD88 mutant B-cell malignancies. DFCI-002-06 serves as a valuable tool for researching mechanisms underlying these specific cancer types.

Cat. No.

A31690

CAS No.

2585561-49-3

PROTAC BRD4 Degrader-17

PROTAC BRD4 Degrader-17 is a potent protein degrader targeting bromodomain-containing protein 4 (BRD4). It exhibits IC50 values of 29.54 nM for BRD4 (BD1) and 3.82 nM for BRD4 (BD2). This compound effectively inhibits G2/M cell cycle progression, leading to decreased expression of Cyclin B1, and significantly induces apoptosis in MV-4-11 cells. PROTAC BRD4 Degrader-17 is valuable for research applications focused on cancer cell biology and the development of targeted degraders in therapeutic strategies.

Cat. No.

A31789

CAS No.

2409793-36-6

PROTAC EGFR degrader 5

PROTAC EGFR Degrader 5 is a targeted protein degradation agent that effectively degrades the EGFRDel19 variant in HCC827 cells, exhibiting a DC50 of 34.8 nM. This compound significantly induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells, making it a valuable tool for studying EGFR-related signaling pathways and potential therapeutic interventions in lung cancer research.

Cat. No.

A31796

CAS No.

2956722-48-6

PROTAC FLT-3 degrader 4

PROTAC FLT-3 degrader 4 is a CRBN-based degrader that selectively targets FLT3-ITD mutants by harnessing the ubiquitin-proteasome system for degradation. This compound demonstrates potent activity against FLT3-ITD mutant acute myeloid leukemia (AML) cells, offering a focused approach for research applications in cancer therapeutics. Its oral bioavailability positions it as a valuable tool for investigating FLT3-related signaling pathways and potential treatment strategies in AML.

Cat. No.

A31851

CAS No.

3057939-64-4

Pro-PEG3-BA

Pro-PEG3-BA is a targeted PROTAC degrader that specifically degrades EML4-ALK and EGFR mutants, with DC50 values of 0.42 μM and 13.50 μM, respectively. It effectively inhibits proliferation and induces cell cycle arrest and apoptosis in non-small cell lung cancer (NSCLC) cell lines in vitro. In vivo studies reveal that Pro-PEG3-BA rewires the ubiquitin-proteasome system, leading to a reduction in EML4-ALK protein levels while demonstrating a favorable safety profile. This reagent is suitable for research focused on non-small cell lung cancer treatments.

Cat. No.

A31880

CAS No.

3023189-40-1

(R)-SL18

(R)-SL18 is an ANXA3 degrader that facilitates the degradation of ANXA3 protein via the ubiquitination pathway. It exhibits significant anti-cancer activity by inhibiting the proliferation, migration, invasion, and colony formation of breast cancer cells while inducing apoptosis. This compound is valuable for research focused on triple-negative breast cancer.

Cat. No.

A31896

CAS No.

2798907-16-9

ITRI-90

ITRI-90 is an orally bioavailable androgen receptor (AR) PROTAC degrader that facilitates the degradation of both full-length AR (AR-FL) and the splice variant AR-V7 through the ubiquitin-proteasome pathway. This mechanism effectively reduces AR transcriptional activity and downregulates target gene expression. ITRI-90 has shown significant antitumor effects by inhibiting the proliferation of prostate cancer cells, including those resistant to Enzalutamide, and promoting apoptosis. Additionally, it possesses favorable pharmacokinetic properties, making it a valuable tool for research in prostate cancer.

Cat. No.

A31972

CAS No.

3031840-36-2

NEP162

NEP162 is a potent BRD4 PROTAC degrader, demonstrating DC50 values of 1.2 and 1.6 μM in SW480 and U2OS cell lines, respectively. It exhibits significant antiproliferative activity, effectively inhibiting tumor growth and promoting apoptosis in various cancer models. NEP162 is particularly relevant for research applications in osteosarcoma, colorectal cancer, and non-small cell lung cancer.

Cat. No.

A31999

CAS No.

3032601-92-3

PROTAC AR-NTD degrader 1

PROTAC AR-NTD degrader 1 is a protein-targeting chimera designed to selectively target and degrade the N-terminal domain of the Androgen Receptor (AR-V7). This small molecule exhibits significant efficacy in inducing apoptosis in prostate cancer cells, demonstrating a degradation efficiency of 62.2% at 1 μM and 71.1% at 5 μM in VCaP cells. PROTAC AR-NTD degrader 1 is a valuable tool for research focused on androgen receptor signaling and its implications in prostate cancer therapy.

Cat. No.

A32016

CAS No.

2751703-31-6

KT-474 hydrochloride

Synonyms: KYM-001 hydrochloride; PROTAC IRAK4 degrader-7 hydrochloride

KT-474 hydrochloride is a potent PROTAC degrader targeting IRAK4, exhibiting significant anti-tumor properties. This compound inhibits the cell cycle and induces apoptosis in affected cells, demonstrating tumor regression in xenograft models of MYD88-mutated ABC DLBCL. Additionally, KT-474 features an alkyne group facilitating click chemistry, allowing for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for chemical biology research.

Cat. No.

A32036

CAS No.

2559747-12-3

JPS004

JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications.

Cat. No.

A32046

CAS No.

2585561-36-8

PROTAC BRD4 Degrader-16

PROTAC BRD4 Degrader-16 is an effective degrader specifically targeting BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). This compound is known to significantly reduce Cyclin B1 expression, which is associated with G2/M cell cycle progression. Additionally, PROTAC BRD4 Degrader-16 effectively induces apoptosis in MV-4-11 cells, contributing to its potential utility in cancer research and therapeutic applications.

Cat. No.

A32121

CAS No.

2703834-25-5

PROTAC BCR-ABL Degrader-2

PROTAC BCR-ABL Degrader-2 is a selective degrader targeting the Bcr-AblT315 mutant, with a DC50 of 108.7 nM in Ba/F3 Bcr-AblT315I cells. This compound demonstrates a notable degradation efficacy, achieving degradation rates of 69.89% and 94.23% at concentrations of 100 nM and 300 nM, respectively. Additionally, it shows promising in vivo anti-tumor effects including significant tumor regression and induction of apoptosis in tumor cells, while maintaining a favorable safety profile. PROTAC BCR-ABL Degrader-2 is suitable for research focused on chronic myeloid leukemia (CML).

Cat. No.

A32145

CAS No.

2409793-28-6

PROTAC EGFR degrader 6

PROTAC EGFR Degrader 6 is a selective degrader targeting the EGFRDel19 mutant, exhibiting a DC50 value of 45.2 nM in HCC827 cells. This compound effectively induces apoptosis and leads to G1 phase cell cycle arrest in HCC827 cells. Its unique mechanism of action makes it a valuable tool for research focused on EGFR-related pathways and the development of targeted cancer therapies.

Cat. No.

A32174

CAS No.

2785404-76-2

PROTAC HDAC6 degrader 1

PROTAC HDAC6 Degrader 1 is a selective compound designed to target and degrade histone deacetylase 6 (HDAC6) through the proteolysis-targeting chimera (PROTAC) mechanism. With a DC50 of 3.5 nM, this degrader exhibits significant antiproliferative effects, particularly by inducing apoptosis in myeloid leukemia cell lines. It serves as a valuable tool for research on cancer therapies and the modulation of histone deacetylation pathways.

Cat. No.

A32285

CAS No.

2959535-15-8

PROTAC c-Met Degrader-4

PROTAC c-Met Degrader-4 is a potent orally active PROTAC designed to target c-MET for degradation. It exhibits remarkable intracellular degradation potency with a DC50 value of less than 0.5 nM and effectively induces cell cycle arrest and apoptosis while inhibiting cell invasion and migration. This compound is particularly useful in cancer research, demonstrating the ability to suppress proliferation and inhibit the growth of various cancers, including non-small cell lung cancer and gastric cancer. In vivo studies also highlight its effectiveness in reducing tumor growth in Hs746T xenograft models.

Cat. No.

A32386

CAS No.

3100306-42-8

PROTAC TRIB2 degrader-1

PROTAC TRIB2 degrader-1 selectively targets TRIB2 for degradation through the CRBN-dependent ubiquitin-proteasome pathway. This compound effectively inhibits cell proliferation and induces apoptosis, making it a valuable tool in cancer research. Its unique mechanism allows for targeted protein degradation, facilitating studies on TRIB2's role in various cellular processes.

Cat. No.

A32503

CAS No.

3102423-10-6

PROTAC KDM4 degrader-1

PROTAC KDM4 Degrader-1 is a potent proteolysis targeting chimera (PROTAC) designed to selectively degrade KDM4A-C while sparing KDM4D. This compound demonstrates significant antiproliferative effects in esophageal cancer cells, inducing apoptosis and cell cycle arrest. Additionally, PROTAC KDM4 Degrader-1 effectively inhibits histone H3 lysine demethylation, making it a valuable tool for research into cancer biology and epigenetic regulation.

Cat. No.

A32518

CAS No.

2933135-82-9

SJ11646

SJ11646 is a LCK-targeting PROTAC degrader based on Dasatinib, exhibiting a DC50 of 0.00838 pM. This compound demonstrates potent cytotoxic effects against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, effectively prolonging LCK signaling suppression and inducing apoptosis in T-ALL. Additionally, SJ11646 binds with high affinity to 51 human kinases, including ABL1, KIT, and DDR1, and shows enhanced antileukemic efficacy in T-ALL mouse models, making it a valuable tool for research into novel therapeutic strategies for leukemia.