PROTAC Degraders: dBET1, MZ1 & ARV-771

Cat. No.: A28753

CAS No.: 3034244-56-6

PROTAC EGFR degrader 10

PROTAC EGFR Degrader 10 is an advanced PROTAC agent targeting the epidermal growth factor receptor (EGFR) with a DC50 of less than 100 nM. It effectively binds to CRBN-DDB1 with a Ki of 37 nM, facilitating the degradation of EGFR as well as focal adhesion kinase (FAK) and RSK1. This compound demonstrates potent inhibitory effects on the proliferation of BaF3 cells, including those with EGFR mutations, with an IC50 of less than 150 nM. PROTAC EGFR Degrader 10 is suitable for studies focused on targeted protein degradation and cancer research.

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Cat. No.: A28883

CAS No.: 3034244-71-5

PROTAC EGFR degrader 11

PROTAC EGFR Degrader 11 is a targeted degrader specifically designed to modulate the epidermal growth factor receptor (EGFR) through the PROTAC mechanism. It effectively binds to the CRBN-DDB1 complex with a Ki value of 36 nM and has a DC50 of less than 100 nM for EGFR degradation. This compound demonstrates significant biological activity by degrading not only EGFR but also focal adhesion kinase (FAK) and RSK1. Additionally, it inhibits the proliferation of BaF3 cells with both wild-type and mutant EGFR variants, achieving an IC50 of less than 100 nM, making it a valuable tool for cancer research focused on EGFR-related pathways.

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Cat. No.: A28887

CAS No.: 2103331-95-7

PROTAC Her3 Degrader-8

PROTAC Her3 Degrader-8 is a potent Her3 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of the Her3 protein. This compound is particularly relevant for studies focused on lung adenocarcinoma and ovarian cancer, enabling researchers to investigate the role of Her3 in these malignancies. The design incorporates a specific Her3 ligand, an E3 ligase ligand, and a linker, which optimizes its efficacy as a targeted degradation tool in research applications.

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1 mg

$350.00

5 mg

$1,085.00

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Cat. No.: A28911

CAS No.: 2230821-38-0

SJF-1528

SJF-1528 is a potent EGFR PROTAC degrader that selectively targets wild-type EGFR and Exon 20 Ins mutant EGFR, exhibiting DC50 values of 39.2 nM and 736.2 nM, respectively, in OVCAR8 and HeLa cells. This compound facilitates the ubiquitination and subsequent degradation of EGFR and also affects HER2 levels. SJF-1528 is valuable for breast cancer research, providing insights into targeted degradation mechanisms and alterations in growth factor signaling pathways.

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1 mg

$135.00

5 mg

$345.00

All 6 sizes

Cat. No.: A28959

CAS No.: 2923686-62-6

PROTAC PARP1 degrader-2

PROTAC PARP1 degrader-2 is a targeted protein degradation compound designed to specifically degrade PARP1. With a DC50 of less than 10 nM in MDA-MB-231 cells, it demonstrates potent efficacy in inducing degradation. Additionally, this compound inhibits cell viability in MDA-MB-436 cells with an IC50 of less than 100 nM, making it a valuable tool for research in cancer therapeutics and the mechanistic study of PARP1 function.

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Cat. No.: A29009

CAS No.: 3093642-25-9

PROTAC EZH2 Degrader-44

PROTAC EZH2 Degrader-44 is a selective degrader targeting the EZH2-PRC2 complex through the recruitment of the CRBN E3 ligase, facilitating proteasome-mediated degradation of EZH2, SUZ12, and EED. This process leads to a marked reduction in H3K27me3 and CARM1 levels, resulting in potent antiproliferative effects. It induces mitochondrial dysfunction and promotes apoptosis by modulating Bcl-2 family proteins, demonstrating minimal cytotoxicity in normal human mammary epithelial, liver, and kidney cells. PROTAC EZH2 Degrader-44 serves as an effective research tool for investigating targeted therapies in triple-negative breast cancer.

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Cat. No.: A29123

CAS No.: 2569517-30-0

RBN012811

RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections.

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5 mg

$965.00

10 mg

$1,640.00

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Cat. No.: A29140

CAS No.: 2966791-41-1

NP1192

NP1192 is a selective PROTAC degrader targeting NAT10, effectively depleting NAT10 protein levels and inhibiting ac4C modification in cancer cells. This compound disrupts the NAT10/HIF-1α/PD-L1 signaling axis, resulting in dual inhibition of hypoxia-driven glycolysis and immunosuppression, thus enhancing antitumor efficacy. NP1192 is valuable for research applications in ovarian, cervical, and glioblastoma cancers, providing insights into therapeutic strategies involving NAT10 modulation.

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Cat. No.: A29147

CAS No.: 3031606-85-3

PROTAC KAT2A/B degrader-1

PROTAC KAT2A/B degrader-1 is a targeted degrader that selectively induces the degradation of histone acetyltransferases KAT2A and KAT2B. This compound demonstrates significant inhibition of proliferation in acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 is a valuable tool for studying the roles of KAT2A and KAT2B in cancer biology and may facilitate the development of novel therapeutic strategies for these malignancies.

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Cat. No.: A29148

CAS No.: 2260944-69-0

GSK702

GSK702 is a PROTAC that targets the P300/CBP-associated factor (PCAF) with a focus on the less active cis-(S,S)-enantiomer of GSK983. This compound exhibits a modest ability to reduce PCAF protein levels and effectively binds to Cereblon (CRBN), leading to decreased interleukin-1 beta (IL-1β) levels in macrophages. GSK702 serves as a valuable tool for investigating the role of inflammatory mediators in cellular processes.

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Cat. No.: A29158

CAS No.: 2839637-72-6

WIZ degrader 3

WIZ Degrader 3 (Compound 29) is a selective degrader targeting widely interspaced zinc finger motifs (WIZ), exhibiting an AC50 of 6.4 nM. This compound effectively induces the expression of fetal hemoglobin (HbF) with an EC50 of 45 nM. WIZ Degrader 3 is valuable for research in blood disorders, including sickle cell disease and β-thalassemia, facilitating studies on therapeutic strategies for these conditions.

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Cat. No.: A29167

CAS No.: 3036553-83-7

WIZ degrader 7

WIZ Degrader 7 is a potent WIZ degrader with an IC50 value of less than 0.01 μM. It is designed for the targeted degradation of WIZ proteins, making it a valuable tool in the study of sickle cell disease (SCD) and thalassemia. This compound enables researchers to explore the mechanistic pathways involved in these hemoglobin disorders and assess potential therapeutic interventions.

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Cat. No.: A29170

CAS No.: 3036553-87-1

WIZ degrader 6

WIZ Degrader 6 is a potent WIZ degrader with an EC50 of less than 0.01 μM, effectively targeting the WIZ protein. This compound plays a critical role in cellular pathways associated with sickle cell disease, providing a valuable tool for investigating disease mechanisms and potential therapeutic approaches. Its high specificity and efficacy make it suitable for research applications focused on cellular degradation processes.

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Cat. No.: A29171

CAS No.: 2879250-73-2

WIZ degrader 5

WIZ Degrader 5 is a selective degrader targeting the WIZ protein, facilitating efficient degradation with a maximum efficacy of 88.6% observed in 293T cells. This reagent is particularly valuable for investigating the biological mechanisms underlying sickle cell disease, enabling researchers to explore novel therapeutic approaches.

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Cat. No.: A29179

CAS No.: 3031593-79-7

AUR1545

AUR1545 is a selective degrader of KAT2A and KAT2B, which plays a crucial role in the modulation of monocyte differentiation and the inhibition of acute myeloid leukemia cell proliferation. This compound has demonstrated efficacy in inducing epithelial differentiation and suppressing tumor growth in small cell lung cancer models. Additionally, AUR1545 promotes differentiation and inhibits growth in neuroendocrine prostate cancer cells, including primary patient-derived organoids. Its application extends to critical research in acute myeloid leukemia, small cell lung cancer, and neuroendocrine prostate cancer.

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1 mg

$170.00

5 mg

$440.00

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Cat. No.: A29211

CAS No.: 3055107-34-8

BT-O2C

BT-O2C is a selective p300 PROTAC degrader that effectively reduces p300 levels in HAP1 cells. It exhibits significant cytotoxicity in CIC:DUX4 sarcoma cell lines, with IC50 values ranging from 152 to 221 nM, and notably decreases the expression of target genes associated with CDS, such as ETV1, ETV4, and ETV5. This compound serves as a valuable tool for research in cancer biology, facilitating studies on p300's role in oncogenic processes.

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Cat. No.: A29217

CAS No.: 2879250-22-1

WIZ degrader 4

WIZ Degrader 4 is a WIZ degrader that exhibits an AC50 value of 160 nM. This compound plays a critical role in targeted protein degradation, facilitating the investigation of underlying mechanisms in sickle cell disease (SCD) and thalassemia. Its application in research aids in understanding disease pathology and therapeutic development.

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5 mg

$215.00

10 mg

$355.00

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Cat. No.: A29231

CAS No.: 2260944-68-9

GSK699

GSK699 is a PROTAC degrader targeting PCAF/GCN5, promoting their ubiquitination and subsequent proteasomal degradation. This compound effectively inhibits the production of key cytokines and chemokines, such as interleukin-6 (IL-6) and CXCL1/GROα, thus demonstrating significant anti-inflammatory properties. GSK699 is suitable for investigations related to inflammatory diseases and other conditions modulated by these target proteins.

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1 mg

$290.00

5 mg

$750.00

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Cat. No.: A29232

CAS No.: 3109024-12-3

PROTAC CBP/p300/BRD4 Degrader-1

PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader that specifically targets BRD4, CBP, and p300, achieving DC50 values of 8.8 pM, 6.55 nM, and 1.05 nM, respectively. This compound promotes CRBN- and proteasome-mediated degradation of BRD4 and CBP/p300, leading to the downregulation of c-Myc and acetyl-H3K27, and inducing apoptosis. It exhibits significant antiproliferative and antitumor effects, demonstrated by tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 is a valuable tool for research focused on prostate and colorectal cancer.

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Cat. No.: A29233

CAS No.: 3102127-45-4

PROTAC CBP/P300 Degrader-2

PROTAC CBP/P300 Degrader-2 is a PROTAC that targets the CBP and p300 proteins, promoting their degradation via the ubiquitin-proteasome system. This compound is effective in modulating gene transcription and can be utilized in research studies focused on cancer, autoimmune disorders, inflammatory conditions, and neurodegenerative diseases. Its potential to selectively degrade these co-activators makes it a valuable tool for investigating the therapeutic implications of targeting transcriptional regulation in various disease contexts.

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Cat. No.: A30020

CAS No.: 2803881-11-8

MRT-2359

MRT-2359 is a selective degrader of GSPT1, exhibiting potent inhibition with an IC50 between 30 and 300 nM. This compound induces apoptosis through mechanisms that depend on protein translation, demonstrating significant anti-proliferative effects, particularly in MYC-driven cancer cell lines, including non-small cell and small cell lung cancers with elevated N-Myc or L-Myc expression. Additionally, MRT-2359 effectively targets drug-resistant NSCLC and SCLC cells, making it a valuable tool for cancer research applications.

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1 mg

$40.00

5 mg

$90.00

All 7 sizes

Cat. No.: A30229

CAS No.: 3042820-12-9

BWA-522

BWA-522 is an orally active PROTAC degrader that targets the full-length androgen receptor (AR-FL) and its splice variant AR-V7. By antagonizing the N-terminal domain of the androgen receptor, BWA-522 effectively suppresses downstream signaling pathways and induces apoptosis in cancer cells. Furthermore, this compound has demonstrated significant inhibition of tumor growth in LNCaP xenograft mouse models, making it a valuable tool for prostate cancer research.

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1 mg

$300.00

5 mg

$615.00

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Cat. No.: A30477

CAS No.: 3025082-14-5

PROTAC CDK4/6 degrader 1

PROTAC CDK4/6 degrader 1 is a dual-targeted degrader designed to selectively degrade cyclin-dependent kinases CDK4 and CDK6. With DC50 values of 10.5 nM and 2.5 nM, this compound effectively inhibits cell proliferation in Jurkat cells, demonstrating an IC50 of 0.18 μM. The compound promotes G1 phase cell cycle arrest and triggers apoptosis, making it a valuable tool for studying cancer biology and potential therapeutic applications in CDK-related malignancies.

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Cat. No.: A30620

CAS No.: 3055471-57-0

CPD-10

CPD-10 is a targeted CCND1 and CDK4 PROTAC degrader that effectively promotes the degradation of these proteins. Exhibiting significant anti-proliferative activity, CPD-10 induces apoptosis in cancer cell lines. It decreases the expression levels of cyclin D1, cyclin D3, CDK4, and phosphorylated Rb at serines 5807 and 811 in a dose-dependent manner, making it a valuable tool for research in cancer biology and therapeutic applications targeting cell cycle regulation.

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1 mg

$480.00

5 mg

$1,230.00

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Cat. No.: A30635

CAS No.: 2992670-33-2

PROTAC EGFR degrader 9

PROTAC EGFR Degrader 9 is a CRBN-based PROTAC designed to specifically target and degrade the mutant forms of the epidermal growth factor receptor (EGFR), particularly EGFRL858R/T790M/C797S. It demonstrates potent degradation activity with a DC50 of 10.2 nM and a Kd of 240.2 nM, effectively eliminating EGFR mutants while leaving wild-type EGFR unaffected. This compound serves as a valuable tool in cancer research, particularly in studies focused on targeted therapies for EGFR-driven malignancies.

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5 mg

$415.00

10 mg

$680.00

All 5 sizes