PROTAC Degrader

Cat. No.

A30647

CAS No.

3044108-04-2

PROTAC AR Degrader-8

PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer.

Cat. No.

A30747

CAS No.

2821803-61-4

HEMTAC CDK4/6 degrader 1

HEMTAC CDK4/6 degrader 1 is a PROTAC designed to target CDK4 and CDK6 through a dual-ligand approach involving HSP90. This compound effectively induces the degradation of CDK4/6 in B16F10 melanoma cells, leading to cell cycle arrest at the G0/G1 phase and subsequent apoptosis. It serves as a vital tool for cancer research, particularly in elucidating mechanisms of CDK4/6 regulation and their role in tumor progression. Additionally, HEMTAC CDK4/6 degrader 1 features an alkyne functional group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing compounds for advanced applications in chemical biology.

Cat. No.

A30751

CAS No.

2521299-80-7

PROTAC ERα Degrader-4

PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies.

Cat. No.

A30794

CAS No.

2570251-69-1

SIAIS039

SIAIS039 is an orally active PROTAC targeting the c-ros oncogene 1 (ROS1), exhibiting DC50 values of 154.46 nM, 126.47 nM, and 143.69 nM in HCC78 cells, and Ba/F3 cells expressing the CD74-ROS1 and SDC4-ROS1 fusions, respectively. This compound effectively suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity in ROS1-positive cells. Additionally, SIAIS039 demonstrates significant anti-tumor effects in vivo against ROS1-driven tumor growth, making it a valuable tool for research in targeted cancer therapy.

Cat. No.

A30796

CAS No.

2770263-77-7

SZUH280

SZUH280 is a selective PROTAC degrader targeting HDAC8, demonstrating a DC50 of 0.58 μM in A549 cells. It effectively induces apoptosis in cancer cells and disrupts DNA repair mechanisms, thereby enhancing cellular radiosensitivity. This compound is particularly useful for research related to cancer therapeutics and the study of epigenetic regulation.

Cat. No.

A30822

CAS No.

2408339-39-7

MS105

Synonyms: YX39-105

MS105 is a selective degrader of protein tyrosine kinase 6 (PTK6), functioning through the PROTAC mechanism. By recruiting the VHL E3 ligase, MS105 facilitates the ubiquitination and subsequent proteasomal degradation of PTK6. It demonstrates notable biological activity by inhibiting the proliferation and migration of breast cancer cells while also inducing apoptosis. This compound is valuable for research applications focused on breast cancer mechanisms and therapeutic strategies.

Cat. No.

A30842

CAS No.

2458170-54-0

PROTAC eEF2K degrader-1

PROTAC eEF2K degrader-1 is a small molecule designed to target and induce degradation of the elongation factor 2 kinase (eEF2K). This compound has been shown to effectively promote apoptosis in MDA-MB-231 cancer cells, demonstrating its potential in cancer research. The mechanism of action involves the targeted elimination of eEF2K, providing a valuable tool for studying the role of this kinase in cellular processes and therapeutic applications.

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.