PROTAC Degraders: dBET1, MZ1 & ARV-771

Cat. No.: A34541

CAS No.: 2379672-57-6

PROTAC ALK degrader-5

PROTAC ALK degrader-5 is a targeted degrader composed of a small molecule that selectively degrades anaplastic lymphoma kinase (ALK). It demonstrates potent inhibitory activity against EML4-ALK and NPM-ALK, with IC50 values of 27.4 nM and 116.5 nM, respectively. This compound exhibits significant anti-proliferative effects against ALK-driven cancer cell lines, including H3122 and Karpas 299, and effectively inhibits ALK and STAT3 phosphorylation. PROTAC ALK degrader-5 is a valuable tool for investigating ALK-driven malignancies, particularly in the context of human non-small cell lung cancer and anaplastic large cell lymphoma research.

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Cat. No.: A34543

CAS No.: 2162120-55-8

TD-004

TD-004 is a highly effective ALK PROTAC degrader, demonstrating potent anti-ALK inhibitory activity with an IC50 of 0.11 µM. This compound selectively hampers the proliferation of ALK-positive cancer cell lines, SU-DHL-1 and H3122, with IC50 values of 0.058 µM and 0.28 µM, respectively. TD-004 induces the degradation of ALK fusion proteins, including NPM-ALK and EML4-ALK, through the recruitment of the VHL E3 ligase and the proteasome pathway. Its significant tumor growth inhibition and favorable safety profile in vivo make TD-004 a valuable tool for researching anaplastic large cell lymphoma and non-small cell lung cancer.

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Cat. No.: A34841

CAS No.: 2601594-19-6

PROTAC VEGFR-2 degrader-1

PROTAC VEGFR-2 Degrader-1 is a targeted protein degradation compound designed to selectively degrade VEGFR-2. It demonstrates minimal VEGFR-2 inhibition with an IC50 exceeding 1 μM, and exhibits limited anti-proliferative activity against EA.hy926 cells, with an IC50 greater than 100 μM. This reagent is valuable for research applications focused on the regulation of VEGFR-2 and its role in vascular biology and related disease mechanisms.

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Cat. No.: A34847

CAS No.: 2353417-85-1

PROTAC VEGFR-2 degrader-2

PROTAC VEGFR-2 Degrader-2 primarily targets the vascular endothelial growth factor receptor 2 (VEGFR-2) for degradation through the PROTAC mechanism. This compound displays minimal inhibition of VEGFR-2 activity with an IC50 exceeding 1 μM and demonstrates anti-proliferative effects in EA.hy926 cells, with an IC50 greater than 100 μM. It serves as a valuable tool for studies focused on targeted protein degradation and the modulation of signaling pathways related to angiogenesis.

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Cat. No.: A34909

CAS No.: 3049215-64-4

BLK degrader 1

BLK Degrader 1 is a selective degrader of B-lymphoid tyrosine kinase (BLK), a key regulator in B-cell signaling pathways. This compound exhibits significant anticancer activity across various B-lymphoid cell lines, making it a valuable tool for research into B-cell malignancies. Its targeted degradation of BLK offers potential insights into therapeutic strategies for treating cancers that involve B-lymphoid cells.

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$105.00

5 mg

$275.00

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Cat. No.: A34917

CAS No.: 3081937-95-0

SJ45566

SJ45566 is a potent PROTAC-based degrader targeting LCK with a DC50 of 1.21 nM. This compound is designed for the selective degradation of LCK, providing a valuable tool for investigating T-Cell Acute Lymphoblastic Leukemia. Its efficacy in modulating LCK levels makes it applicable in studies aimed at understanding T-cell signaling pathways and cancer biology.

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Cat. No.: A34927

CAS No.: 3095032-59-7

LCK degrader-3

LCK Degrader-3 is a CRBN-based molecular glue degrader targeting LCK (lymphocyte-specific protein tyrosine kinase). This compound facilitates the selective degradation of LCK, making it a valuable tool for investigating the role of LCK in acute lymphoblastic leukemia. Its application in research may provide insights into therapeutic mechanisms and potential treatment strategies for leukemia.

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Cat. No.: A34973

CAS No.: 2922274-35-7

NTRK degrader-1

NTRK Degrader-1 is a potent PROTAC degrader specifically targeting both wild-type and mutant NTRK1, with IC50 values of 4 nM for wild-type, 2 nM for G595R, 5 nM for G667C, and

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Cat. No.: A34980

CAS No.: 2412055-93-5

CG428

CG428 is a potent CRBN-dependent PROTAC degrader specifically targeting tropomyosin receptor kinase (TRK). It effectively reduces levels of the TPM3-TRKA fusion protein in KM12 colorectal carcinoma cells with a DC50 of 0.36 nM and inhibits downstream PLCγ1 phosphorylation with an IC50 of 0.33 nM. CG428 demonstrates higher binding affinity for TRKA (Kd = 1 nM) compared to TRKB and TRKC, making it a valuable tool for research into colorectal carcinoma.

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$140.00

5 mg

$365.00

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Cat. No.: A35144

CAS No.: 2760847-82-1

PROTAC RET Degrader 1

PROTAC RET Degrader 1 is an orally bioavailable RET PROTAC degrader that effectively crosses the blood-brain barrier. It demonstrates remarkable potency with DC50 values for various RET mutations, including 1.7 nM for RET (WT) and 3 nM for RET (G810S). PROTAC RET Degrader 1 exhibits strong anti-proliferative effects in cancer cell lines harboring oncogenic RET fusions and mutations, and shows significant anti-tumor efficacy in patient-derived xenograft mouse models. This reagent is valuable for investigating RET-positive cancers and their therapeutic targeting.

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Cat. No.: A35335

CAS No.: 2432992-21-5

PROTAC IRAK4 degrader-13

PROTAC IRAK4 degrader-13 is a selective IRAK4-directed PROTAC degrader that effectively targets IRAK4 with DC50 values of 0.86 nM and 1.1 nM in monocytes and lymphocytes, respectively. This compound significantly activates TIR signaling and reduces the expression of proinflammatory cytokines in an Imiquimod-induced psoriasis mouse model. PROTAC IRAK4 degrader-13 is applicable in research focused on TLR- and IL-1R-driven inflammatory diseases, including hidradenitis suppurativa and atopic dermatitis.

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Cat. No.: A35702

CAS No.: 2995357-09-8

PROTAC PD-L1 degrader-2

PROTAC PD-L1 degrader-2 is a selective degrader targeting PD-L1. It demonstrates a potent inhibitory effect with an IC50 of 197.4 nM and a binding affinity characterized by a Kd of 301 nM. This compound facilitates the internalization and subsequent degradation of PD-L1 through both proteasomal and lysosomal pathways, thereby enhancing immune system activation. Its efficacy has been validated in MC38 C57BL/6 mouse models, underscoring its potential for antitumor applications.

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Cat. No.: A36031

CAS No.: 3108744-13-1

PROTAC HPK1 Degrader-5

PROTAC HPK1 Degrader-5 is a highly potent and orally bioavailable PROTAC that targets HPK1 for degradation (DC50 = 5.0 nM; Dmax ≥ 99%). This compound effectively inhibits SLP76 phosphorylation and promotes ERK pathway activation, leading to increased release of IL-2 and IFN-γ. It demonstrates the capability to counteract immunosuppressive signals induced by PGE2, NECA, or TGF-β. Additionally, PROTAC HPK1 Degrader-5 has shown efficacy in inhibiting tumor growth in MC38 syngeneic mouse models, making it a valuable tool for research in tumor immunotherapy, particularly in colorectal cancer.

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Cat. No.: A36111

CAS No.: 3113890-51-7

PROTAC IRAK4 degrader-14

PROTAC IRAK4 degrader-14 is an orally active degrader targeting IRAK4 with a DC50 of 2.4 nM. It functions by selectively degrading IRAK4, thereby inhibiting pro-inflammatory responses in various cell types, including T cells, monocytes, and keratinocytes. This compound has significant relevance in research focused on inflammatory diseases, particularly psoriasis.

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Cat. No.: A36262

CAS No.: 3032975-48-4

PVD-06

PVD-06 is a selective PROTAC degrader targeting PTPN2, exhibiting a DC50 of 217 nM with a selectivity index greater than 60-fold over PTP1B. This compound facilitates the degradation of PTPN2 through a VHL-, ubiquitin-, and proteasome-dependent mechanism. It has been shown to enhance T cell activation and promote IFN-γ-mediated anticancer effects. PVD-06 is a valuable tool for exploring the role of PTPN2 in various diseases, including leukemia and melanoma.

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Cat. No.: A36306

CAS No.: 3093519-24-2

JCS-1

JCS-1 is a highly potent DcpS PROTAC degrader that facilitates the targeted degradation of the DcpS enzyme through non-covalent binding via a RG3039-based warhead, while recruiting the E3 ligase VHL. This compound effectively promotes ubiquitination and subsequent degradation of DcpS at nanomolar concentrations, demonstrating a DC50 value of 87 nM in MOLM-14 cells. JCS-1 is a valuable tool for investigating acute myeloid leukemia (AML) and other genetic disorders associated with DcpS dependency.

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Cat. No.: A36422

CAS No.: 2912307-39-0

PROTAC PTPN2 degrader-2 TFA

PROTAC PTPN2 degrader-2 TFA is a highly potent PTPN2 degrader with a DC50 of less than 50 nM. This compound facilitates targeted protein degradation, providing a valuable tool for investigating the role of PTPN2 in cancer and metabolic disorders, including colon cancer. Its application in research can enhance understanding of disease mechanisms and therapeutic interventions.

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Cat. No.: A36434

CAS No.: 2912307-38-9

PROTAC PTPN2 degrader-2

PROTAC PTPN2 Degrader-2 is a selective PTPN2 degrader that effectively induces targeted degradation of the PTPN2 protein, demonstrating a DC50 of less than 50 nM. This compound is instrumental for exploring cellular mechanisms within cancer and metabolic disorders, particularly in the context of colon cancer research. Its utility in protein knockdown enables innovative studies into therapeutic strategies for disease intervention.

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Cat. No.: A36475

CAS No.: 3077464-21-9

PROTAC STAT6 degrader-1

PROTAC STAT6 degrader-1 is a targeted protein degradative compound designed to modulate STAT6 activity through the recruitment of E3 ligase CRBN. With a DC50 of less than 1 nM, this PROTAC showcases potent efficacy in STAT6 degradation. It is particularly relevant for research on inflammation and various cancer types, providing a valuable tool for exploring STAT6's role in pathophysiology and therapeutic responses.

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Cat. No.: A36514

CAS No.: 2497585-50-7

SD-436

SD-436 is a selective and potent degrader of STAT3, functioning through the PROTAC mechanism with a DC50 of 0.5 μM and an IC50 of 19 nM for STAT3. It promotes the ubiquitination and subsequent degradation of STAT3, leading to significant tumor regression. This reagent is applicable in cancer research, including studies focused on leukemia and lymphoma.

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1 mg

$210.00

5 mg

$645.00

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Cat. No.: A36544

CAS No.: 3053413-58-1

DU-14 (PTP1B/TC-PTP PROTAC)

DU-14 is a potent dual degrader targeting PTP1B and TC-PTP via the PROTAC mechanism. It demonstrates remarkable selectivity with IC50 values of 24.2 nM and 30.1 nM for PTP1B and TC-PTP phosphatase activity, respectively. DU-14 enhances interferon-gamma signaling, promotes T cell activation, and exhibits anti-tumor properties, making it a valuable tool for cancer immunology research and the study of immune modulation.

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Cat. No.: A36554

CAS No.: 3077385-98-6

PROTAC STAT6 degrader-3

PROTAC STAT6 degrader-3 is a highly potent degrader targeting STAT6, exhibiting a DC50 of less than 1 nM. This compound facilitates the targeted degradation of STAT6, making it a valuable tool for investigating allergic and inflammatory diseases as well as various cancers. Its application in research can provide insights into the role of STAT6 in disease pathways and therapeutic interventions.

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$465.00

10 mg

$760.00

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Cat. No.: A36580

CAS No.: 3054116-24-1

SD-2301

SD-2301 is a selective STAT3 PROTAC degrader that targets and induces the degradation of STAT3 while preserving the expression of other STAT family members such as STAT1, STAT2, STAT4, STAT5, and STAT6. It has demonstrated anti-tumor efficacy in B16F10-bearing mouse models, making it a valuable tool for cancer research. This compound can be utilized in studies focused on the modulation of STAT3 pathways and the development of targeted therapies.

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Cat. No.: A36586

CAS No.: 3105288-31-8

PROTAC STAT6 degrader-2

PROTAC STAT6 Degrader-2 is a potent bifunctional degrader that specifically targets signal transducer and activator of transcription 6 (STAT6). It demonstrates high efficiency with a DC50 of 1-10 nM in human peripheral blood mononuclear cells (PBMC) and less than 100 nM in HEK293-HIBiT-STAT6 cells. This compound is ideal for research applications related to STAT6-mediated diseases, facilitating the study of its role in various biological processes.

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Cat. No.: A36589

CAS No.: 2710221-08-0

XD2-149

XD2-149 is a PROTAC designed to selectively target STAT3, employing a unique mechanism of action that promotes targeted protein degradation. This compound combines the STAT3 ligand Napabucasin with the E3 ligase Thalidomide via a specialized linker (NH2-C5-Azacyclohexane-N-Boc). XD2-149 offers significant potential for research applications involving cancer biology and the modulation of inflammatory responses, making it a valuable tool for the investigation of therapeutic strategies that manipulate protein levels within cells.

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