PROTAC Degrader

Cat. No.

A34321

CAS No.

3056647-52-7

PROTAC c-Met degrader-1

PROTAC c-Met degrader-1 is a selective and orally active degrader targeting c-Met, exhibiting a DC50 of 6.21 nM. This compound promotes CRBN-dependent ubiquitination and subsequent proteasomal degradation of c-Met, effectively inducing G0/G1 phase arrest in c-Met-dependent cancer cells. Furthermore, PROTAC c-Met degrader-1 demonstrates significant anticancer activity by killing c-Met-dependent cells and inhibiting tumor growth in animal models, making it a valuable tool for research in gastric cancer.

Cat. No.

A34342

CAS No.

3048497-38-4

OZD-MET 01

OZD-MET 01 is a PROTAC-type MET degrader that utilizes a chaperone-mediated mechanism to induce targeted degradation of the MET protein. It exhibits potent inhibition of cell proliferation in non-small cell lung cancer cell lines H596 and H1437, with IC50 values of 3.07 and 3.5 μM, respectively. This compound serves as a valuable tool for cancer research, particularly in studies investigating MET-targeted therapies and mechanisms of resistance in oncogenic signaling pathways.

Cat. No.

A34357

CAS No.

2254608-80-3

PROTAC c-Met degrader-2

PROTAC c-Met degrader-2 is a PROTAC-based degrader that selectively targets c-Met for degradation through the ubiquitin-proteasome pathway, exhibiting a DC50 of 50 nM. This compound employs a unique linkage incorporating a CRBN ligand derived from Thalidomide, facilitating targeted protein degradation. It serves as a valuable tool for researching c-Met-related pathways and their implications in various cancers, enhancing the understanding of therapeutic strategies involving c-Met modulation.

Cat. No.

A34387

CAS No.

2801715-13-7

PROTAC BTK Degrader-1

PROTAC BTK Degrader-1 is an innovative PROTAC-based compound designed for the selective degradation of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 34.51 nM for wild-type BTK and 64.56 nM for the BTK-481S mutant. This compound effectively lowers BTK protein levels, thereby inhibiting tumor growth. Additionally, PROTAC BTK Degrader-1 features an alkyne group facilitating its application in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for advanced chemical research and targeted therapies.

Cat. No.

A34392

CAS No.

2451070-32-7

L18I

L18I is a PROTAC designed to target Bruton’s tyrosine kinase (Btk), facilitating the degradation of this protein and thereby mitigating inflammation associated with autoimmune diseases, such as lupus erythematosus induced by BM12 splenocytes. This compound comprises the IBT6A ligand, a linker moiety (Propargyl-PEG3-alcohol), and an E3 ubiquitin ligase ligand (Lenalidomide-Br), effectively promoting the destruction of Btk. L18I serves as a valuable tool for investigating Btk's role in autoimmunity and offers potential pathways for therapeutic intervention.

Cat. No.

A34399

CAS No.

2366132-45-6

DD-03-171

DD-03-171 is a selective PROTAC BTK degrader that targets Bruton's tyrosine kinase (BTK) for degradation. This compound demonstrates significant anti-proliferative effects on mantle cell lymphoma (MCL) cells with an IC50 of 5.1 nM and enhances survival in murine models bearing patient-derived xenograft (PDX) lymphoma. Additionally, DD-03-171 inhibits platelet function and thrombosis, making it a valuable tool for research in cancer and hematological disorders.

Cat. No.

A34408

CAS No.

2767204-39-5

PROTAC BTK Degrader-6

PROTAC BTK Degrader-6 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 of 3.18 nM. This compound exhibits anti-inflammatory activity by inhibiting NF-κB activation and reducing the expression of pro-inflammatory cytokines, including IL-1β and IL-6. It serves as a valuable tool for research into the modulation of immune responses and the development of therapies for inflammatory diseases.

Cat. No.

A34409

CAS No.

2884554-45-2

UBX-382

UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM, specifically designed to target Bruton's tyrosine kinase (BTK). It effectively disrupts B-cell receptor signaling and demonstrates robust degradation of both wild-type and mutant BTK proteins, including the C481S mutation. UBX-382 has been shown to inhibit tumor growth in murine xenograft models with BTK-expressing TMD-8 cells, making it a valuable tool for investigating B-cell-related malignancies and therapeutic strategies.

Cat. No.

A34411

CAS No.

2250382-66-0

PROTAC BTK Degrader-2

PROTAC BTK Degrader-2 is a highly effective proteolysis-targeting chimera (PROTAC) that selectively degrades Bruton's tyrosine kinase (BTK). By recruiting the Cullin-RING E3 ubiquitin ligase complex, it mediates the ubiquitination and subsequent degradation of BTK protein, leading to a marked reduction in its cellular levels. This compound is valuable in research focused on B-cell malignancies and autoimmune diseases, providing insights into BTK's role in signaling pathways and therapeutic interventions.

Cat. No.

A34414

CAS No.

2988804-46-0

PROTAC BTK Degrader-10

PROTAC BTK Degrader-10 is a PROTAC agent that targets Bruton's Tyrosine Kinase (BTK) for selective degradation. This compound is particularly useful in the study of chronic lymphocytic leukemia (CLL) due to its ability to modulate BTK levels, thereby influencing malignant cell survival and proliferation. The degrader is designed with a specific ligand for BTK and a linker, enabling effective recruitment of the E3 ubiquitin ligase Cereblon for targeted degradation.

Cat. No.

A34418

CAS No.

2821938-05-8

SJF620 hydrochloride

SJF620 hydrochloride functions as a PROTAC designed for the degradation of Bruton's tyrosine kinase (Btk) via recruitment of the cereblon (CRBN) E3 ligase. With a DC50 value of 7.9 nM, SJF620 effectively mediates the targeted degradation of Btk, making it a valuable tool for research focused on Btk-related pathways. This compound is particularly relevant in studies of immune responses and various hematological malignancies.

Cat. No.

A34423

CAS No.

2642231-19-2

PTD10

PTD10 is a potent PROTAC degrader targeting Bruton's tyrosine kinase (BTK), exhibiting a DC50 of 0.5 nM and a KD of 2.28 nM. It effectively degrades BTK in Ramos and JeKo-1 cell lines, leading to the inhibition of cell growth and the induction of apoptosis through caspase activation and mitochondrial pathways. PTD10 is suitable for investigating mechanisms of B-cell dysregulation and related therapeutic strategies.

Cat. No.

A34448

CAS No.

3036944-98-3

DDa-1

DDa-1 is a potent BTK PROTAC degrader with a DC50 of 90 nM, designed to facilitate the targeted degradation of Bruton's Tyrosine Kinase (BTK) in cellular systems. This compound effectively utilizes a novel mechanism involving DCAF1 binding, a distinct linker, and a specific BTK ligand to enhance selectivity and efficacy. DDa-1 is primarily utilized in research applications focusing on BTK-related signaling pathways and therapeutic strategies against B-cell malignancies.

Cat. No.

A34453

CAS No.

2669844-82-8

BCPyr

BCPyr is a PROTAC-class degrader specifically targeting Bruton’s Tyrosine Kinase (BTK), exhibiting a DC50 of 800 nM. This compound integrates a BTK ligand (ligand 11) and an E3 ubiquitin ligase ligand (ligand 20) through a pyrazinyl methanol linker. BCPyr facilitates the targeted degradation of BTK, making it a valuable tool for studying diseases where BTK is implicated, such as certain hematological malignancies.

Cat. No.

A34467

CAS No.

2736508-65-7

PROTAC BTK Degrader-12

PROTAC BTK Degrader-12 is a PROTAC (Proteolysis Targeting Chimera) designed to selectively degrade Bruton's tyrosine kinase (BTK). It facilitates the targeted ubiquitination and subsequent proteasomal degradation of BTK, resulting in diminished signaling pathways associated with B-cell malignancies and autoimmune disorders. This compound serves as a valuable tool in research investigating BTK's role in disease mechanisms and therapeutic interventions.

Cat. No.

A34475

CAS No.

2926610-43-5

TQ-3959

TQ-3959 is an orally bioavailable BTK PROTAC degrader that demonstrates a DC50 of 14.6 nM. It exhibits potent antiproliferative effects on both wild-type BTK and the C481S mutant BTK cell lines. In vivo, TQ-3959 effectively inhibits tumor growth in female NOD-SCID mice bearing TMD-8 xenografts. This compound is valuable for investigating B-cell malignancies, including lymphoma.

Cat. No.

A34486

CAS No.

2416130-49-7

PROTAC BTK/IKZF1/3 Degrader-1

PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally bioavailable degrader targeting BTK, IKZF1, and IKZF3 through the PROTAC mechanism. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research, particularly in the context of lymphoma. Its unique mechanism of action allows for the targeted degradation of specific oncogenic proteins, facilitating studies in therapeutic strategies and disease mechanisms.

Cat. No.

A34487

CAS No.

2893795-12-3

PROTAC BTK Degrader-4

PROTAC BTK Degrader-4 is a highly effective PROTAC designed to selectively degrade Bruton's tyrosine kinase (BTK) with a DC50 of less than 100 nM. This compound demonstrates minimal immunomodulatory imide drug (IMiD) activity, with a DC50 of 0.345 μM and a maximum degradation rate of 27.4%. PROTAC BTK Degrader-4 is suitable for investigating various pathologies, including cancers, autoimmune disorders, and inflammatory diseases associated with BTK dysregulation.

Cat. No.

A34491

CAS No.

2563861-90-3

PROTAC BTK Degrader-3

PROTAC BTK Degrader-3 is a selective degrader targeting Bruton's tyrosine kinase (BTK) with a DC50 value of 10.9 nM for BTK degradation in Mino cells. This compound demonstrates significant biological activity and is applicable in research focusing on B-cell malignancies, particularly chronic lymphoid malignancies. Its mechanism of action offers potential pathways for therapeutic intervention in relevant disease models.

Cat. No.

A34493

CAS No.

3034024-77-3

PROTAC BTK Degrader-9

PROTAC BTK Degrader-9 functions as a targeted degrader of Bruton's tyrosine kinase (BTK), primarily inhibiting the NFAT signaling pathway. By downregulating the BTK-PLCγ2-Ca2+-NFATc1 cascade activated by RANKL, it demonstrates significant potential in inhibiting osteoclastogenesis and reducing alveolar bone loss. This compound is suitable for research applications related to bone resorption and inflammation in models of periodontitis.

Cat. No.

A34496

CAS No.

3114684-06-6

PROTAC BTK degrader-14

PROTAC BTK Degrader-14 is a targeted protein degrader that specifically degrades Bruton's tyrosine kinase (BTK) through the PROTAC mechanism of action. This compound is significant in cancer research, particularly for studies focused on malignancies where BTK plays a crucial role in signaling pathways. Its ability to effectively modulate BTK levels can provide insights into therapeutic strategies and disease mechanisms involving this key protein.

Cat. No.

A34501

CAS No.

2570251-63-5

SIAIS001

SIAIS001 is a potent PROTAC degrader targeting anaplastic lymphoma kinase (ALK) with a DC50 of 3.9 nM. This compound induces G1/S phase cell cycle arrest and effectively inhibits the proliferation of SR cells with an IC50 of 0.9 nM. SIAIS001 is suitable for research in non-small cell lung cancer (NSCLC) and anaplastic large-cell lymphomas (ALCLs).

Cat. No.

A34502

CAS No.

3055593-63-7

MS99-β-Gal

Synonyms: Gal-MS99

MS99-β-Gal is a galactose-modified PROTAC degrader targeting the NPM-ALK fusion protein. This compound is selectively hydrolyzed by SA-β-gal and esterase in senescent cancer cells, allowing the release of MS99, which effectively degrades the NPM-ALK protein. MS99-β-Gal demonstrates an IC50 of 454.8 nM in aging Karpas 299 cells, showing improved potency compared to normal Karpas 299 cells with an IC50 of 2.162 μM. This reagent is valuable for cancer research, particularly in studies focused on targeted protein degradation.

Cat. No.

A34528

CAS No.

2417174-28-6

PROTAC EML4-ALK Degrader-2

PROTAC EML4-ALK Degrader-2 is an advanced degrader specifically targeting the EML4-ALK fusion protein. With an IC50 of 1.6 nM, it exhibits potent selective inhibitory activity against ALK while maintaining selectivity over IGF1R, INSR, FLT3, and FGFR2. This compound demonstrates significant anti-cancer effects in both in vitro and in vivo models and is particularly relevant for research applications involving non-small cell lung cancer (NSCLC), as well as liver and cervical cancers.

Cat. No.

A34531

CAS No.

2353494-84-3

SIAIS117

SIAIS117 is a potent Brigatinib-PROTAC degrader that targets the ALK protein, specifically effective against the ALK G1202R point mutation. By utilizing a VHL-1 conjugation, SIAIS117 exhibits significant capability to induce protein degradation, leading to inhibited growth of SR and H2228 cancer cell lines. This compound holds potential for applications in anti-proliferative research, particularly in small cell lung cancer contexts.