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BTK

Bruton's tyrosine kinase (BTK) inhibitors act on a cytoplasmic kinase that relays signals from the B cell receptor. In 1993 two groups linked defects in the BTK gene to X-linked agammaglobulinemia, in which mature B cells fail to develop. BTK belongs to the Tec kinase family and is also expressed in myeloid cells such as macrophages and mast cells. Ibrutinib, first described as PCI-32765, binds covalently to a cysteine in the BTK active site and blocks B cell activation. Spebrutinib, listed as AVL-292 and as spebrutinib besylate, is another covalent inhibitor, while CGI1746 and RN486 bind reversibly. Ibrutinib-biotin and the fluorescent analog PCI-33380 serve as probes for BTK active-site occupancy.

Cat. No.

A34462

CAS No.

2922723-28-0

Topoisomerase I inhibitor 11

Topoisomerase I inhibitor 11 is a potent inhibitor of Topoisomerase I, a key enzyme involved in DNA replication and repair. This compound disrupts the enzyme's catalytic activity, leading to the accumulation of DNA damage and ultimately inducing apoptosis in cancer cells. Topoisomerase I inhibitor 11 is primarily utilized in cancer research, particularly for studying mechanisms of drug resistance and the therapeutic potential of targeting Topoisomerase I in various malignancies.

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Cat. No.

A34463

CAS No.

1791402-90-8

BTK/IKZF1/3 ligand 1

BTK/IKZF1/3 ligand 1 is a PROTAC ligand targeting Bruton's tyrosine kinase (BTK) and the Ikaros family zinc finger proteins (IKZF1/3). This compound can be conjugated with E3 ligase ligands and linkers to produce PROTAC BTK/IKZF1/3 Degrader-1, facilitating targeted protein degradation. It is valuable for cancer research, supporting investigations into therapeutic strategies aimed at modulating BTK and IKZF1/3 activity in malignant cells.

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Cat. No.

A34464

CAS No.

1609465-88-4

(Rac)-PF-06250112

(Rac)-PF-06250112 is a racemic mixture of PF-06250112, a highly selective and orally bioavailable inhibitor of Bruton's tyrosine kinase (BTK). This compound demonstrates potent inhibitory activity against BTK as well as BMX nonreceptor tyrosine kinase and TEC. Its selectivity and efficacy make it a valuable tool for research applications focused on B cell malignancies and other diseases associated with aberrant BTK signaling.

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$1,275.00

50 mg

$1,625.00

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Cat. No.

A34466

CAS No.

2824922-28-1

BTK-IN-8

BTK-IN-8 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK), exhibiting a binding affinity with an IC50 of 0.22 nM and a Kd of 0.91 nM. This compound demonstrates significant cellular activity against whole blood CD69, with an IC50 of 0.029 µM. BTK-IN-8 is primarily used in research focused on hematological malignancies and autoimmune disorders, providing insights into BTK-mediated signaling pathways.

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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.

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Cat. No.

A34468

CAS No.

1423129-83-2

RN983

RN983 is a highly selective inhibitor of Bruton's tyrosine kinase (Btk), demonstrating potent inhibition of immunoglobulin G (IgG) production in B-cells with an IC50 of 2.5 nM, and prostaglandin D2 (PGD2) production in mast cells with an IC50 of 8.3 nM. This compound serves as a valuable tool for investigating the roles of Btk in B-cell signaling and mast cell activation, making it relevant in the study of asthma and other allergic diseases.

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Cat. No.

A34469

CAS No.

2502301-31-5

BTK-IN-36

BTK-IN-36 is a potent Bruton’s Tyrosine Kinase (BTK) inhibitor, exhibiting an IC50 of 0.5 nM. This compound effectively inhibits BTK signaling pathways, which are crucial for B-cell receptor signaling and have implications in various cancers. BTK-IN-36 is applicable in cancer research, particularly in studies exploring targeted therapies for B-cell malignancies.

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Cat. No.

A34470

CAS No.

2755843-62-8

RET-IN-14

RET-IN-14 is a highly selective RET inhibitor that demonstrates potent inhibition with IC50 values of less than 0.51 nM for wild-type RET and varying nanomolar activity against RET mutations (G810R and V804M) as well as BTK and its C481S mutant. Its exceptional efficacy positions RET-IN-14 as a valuable tool for investigating RET-driven tumors and exploring therapeutic strategies in cancer research.

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25 mg

$1,800.00

50 mg

$2,285.00

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Cat. No.

A34471

CAS No.

2820426-92-2

BTK-IN-15

BTK-IN-15 is a highly potent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 value of 0.7 nM. This compound demonstrates exceptional selectivity for BTK and displays significant antitumor activity. Additionally, BTK-IN-15 is known to induce apoptosis, making it a valuable tool for research in cancer biology and the development of targeted therapies.

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Cat. No.

A34472

CAS No.

2088001-24-3

VA5

VA5 is a potent Bruton’s tyrosine kinase (BTK) inhibitor, designed to selectively inhibit BTK activity. This compound plays a crucial role in modulating B-cell signaling pathways and has potential applications in studying various diseases associated with dysregulated BTK activity, including certain hematological malignancies and autoimmune disorders. VA5 serves as a valuable tool in preclinical research to further investigate the therapeutic potential of targeting BTK.

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25 mg

$1,405.00

50 mg

$1,790.00

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Cat. No.

A34473

CAS No.

2736508-94-2

PROTAC BTK Degrader-11

PROTAC BTK Degrader-11 is a potent PROTAC designed to selectively degrade Bruton's tyrosine kinase (BTK), exhibiting a DC50 of 1.7 nM. This compound facilitates targeted protein degradation, offering significant potential in cancer research applications by modulating BTK-related pathways. The structure includes a target protein ligand, a linker, and an E3 ligase component, allowing for effective engagement of the ubiquitin-proteasome system.

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Cat. No.

A34474

CAS No.

2758410-51-2

BTK-IN-38

BTK-IN-38 is a potent inhibitor of Bruton's tyrosine kinase (BTK). It effectively inhibits the proliferation of DOHH2 and BT474 cancer cell lines, exhibiting IC50 values of 114 nM and 340 nM, respectively. This compound is of particular interest in research applications targeting B-cell malignancies and related signaling pathways.

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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.

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Cat. No.

A34476

CAS No.

2573048-11-8

BTK-IN-23

BTK-IN-23 is a selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 12.8 nM. This compound also exhibits inhibitory effects on BMX and BLK, with IC50 values of 5.7 nM and 35.6 nM, respectively. BTK-IN-23 demonstrates enhanced kinase selectivity compared to Ibrutinib, making it a valuable tool for research in cancer and autoimmune disease therapies, particularly in studies focusing on B-cell signaling pathways.

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25 mg

$1,275.00

50 mg

$1,625.00

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Cat. No.

A34477

CAS No.

3081685-04-0

BTK-IN-43

BTK-IN-43 is a selective inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 value of 21.6 nM. This compound is capable of oral administration and exhibits potent activity against BTK-mediated signaling pathways. It is primarily utilized in research applications focused on hematological malignancies and immune disorders driven by aberrant BTK activity.

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Cat. No.

A34478

CAS No.

2649400-05-3

BTK degrader-2

BTK Degrader-2 is a potent dual-functional agent designed to degrade Bruton's tyrosine kinase (BTK) via the ubiquitin-proteasome pathway. This compound is valuable for investigating B-cell-related disorders by providing insights into BTK's role in cellular processes and disease mechanisms. Its application in research can enhance the understanding of therapeutic strategies targeting B-cell malignancies and other related diseases.

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Cat. No.

A34479

CAS No.

2041789-14-2

HZ-A-005

HZ-A-005 is a potent and selective covalent inhibitor of Bruton’s tyrosine kinase (BTK), a critical regulator in B cell receptor signaling. This compound demonstrates significant anti-tumor activity, effectively reducing tumor growth in xenograft mouse models. HZ-A-005 is valuable for research applications focused on B cell malignancies and the study of BTK's role in various signaling pathways.

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25 mg

$1,275.00

50 mg

$1,625.00

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Cat. No.

A34480

CAS No.

1015441-29-8

BTK-IN-32

BTK-IN-32 is a selective Bruton’s tyrosine kinase (BTK) inhibitor that effectively modulates BTK activity. It uniquely activates both full-length BTK and smaller multidomain fragments, rather than solely targeting the isolated kinase domain. This compound is useful in research applications focused on B-cell signaling pathways and the development of therapies for related hematological malignancies.

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Cat. No.

A34481

CAS No.

330785-90-5

BTK ligand 1

BTK Ligand 1 is a selective ligand for Bruton’s tyrosine kinase (Btk) that facilitates targeted protein degradation via a PROTAC (proteolysis-targeting chimera) approach. By linking with an E3 ligase ligand through a PROTAC linker, this compound enables the targeted degradation of Btk. BTK Ligand 1 is valuable for researching chronic lymphocytic leukemia (CLL) and other B-cell malignancies, providing insights into the therapeutic potential of Btk inhibition in oncology.

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1 mg

$50.00

5 mg

$115.00

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Cat. No.

A34482

CAS No.

2696450-27-6

BTK inhibitor 20

BTK Inhibitor 20 is a highly selective inhibitor of Bruton’s Tyrosine Kinase (BTK), exhibiting an IC50 value of 8 nM. This compound effectively modulates the BTK signaling pathway, playing a critical role in B-cell receptor signaling and related processes. It is valuable for research focused on B-cell malignancies, autoimmune diseases, and other conditions where BTK activity is implicated.

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25 mg

$1,780.00

50 mg

$2,280.00

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Cat. No.

A34483

CAS No.

2562351-92-0

BTK-IN-25

BTK-IN-25 is a highly potent inhibitor of Bruton’s tyrosine kinase (BTK), demonstrating an IC50 of 0.77 nM against the BTK(C481S) mutant and 1 nM in DOHH2 cells. This compound is valuable for exploring BTK-related signaling pathways and potential therapeutic interventions in B-cell malignancies. Its selective inhibition of BTK makes it a useful tool for research applications focused on the modulation of immune responses and the development of targeted cancer therapies.

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Cat. No.

A34484

CAS No.

2762043-53-6

BTK-IN-12

BTK-IN-12 is a potent Bruton’s Tyrosine Kinase (BTK) inhibitor, with IC50 values of 1.2 nM for wild-type BTK and 0.8 nM for the mutated BTK (C481S). This compound selectively targets BTK, a key regulator in B-cell receptor signaling, making it valuable for research in hematological malignancies and autoimmune disorders. BTK-IN-12 can facilitate the study of therapeutic approaches for conditions associated with dysregulated B-cell activity.

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Cat. No.

A34485

CAS No.

2792171-84-5

ABBV-992

ABBV-992 is a potent and selective Bruton's Tyrosine Kinase (BTK) inhibitor. It demonstrates significant inhibitory activity, making it a valuable tool for studying various hematological malignancies. This compound is primarily utilized in cancer research to investigate BTK signaling pathways and their roles in tumor progression and survival.

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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.

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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.

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