BTK

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.

A34412

CAS No.

936563-91-6

(Rac)-Ibrutinib alkyne

(Rac)-Ibrutinib alkyne is a potent Bruton's tyrosine kinase (Btk) inhibitor with an IC50 of 0.72 nM. This compound effectively disrupts B-cell receptor signaling, demonstrated by an IC50 of 9 nM for inhibiting calcium flux in Ramos cells. (Rac)-Ibrutinib alkyne is suitable for investigating various Btk-related pathologies, including rheumatoid arthritis and other immune disorders.

Cat. No.

A34413

CAS No.

1654820-87-7

Dihydrodiol-Ibrutinib

Synonyms: PCI-45227

Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib, selectively targeting Bruton’s tyrosine kinase (BTK). This compound exhibits inhibitory activity towards BTK that is approximately 15 times lower than that of its parent compound, Ibrutinib. Dihydrodiol-Ibrutinib is utilized in research related to B-cell malignancies and other BTK-mediated pathways, providing insights into the modulation of immune responses and signaling pathways in cancer treatment.

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.

A34415

CAS No.

2241732-30-7

BTK inhibitor 10

BTK Inhibitor 10 is a potent and orally bioavailable inhibitor of Bruton’s tyrosine kinase (BTK), with potential applications in the treatment of rheumatoid arthritis. By selectively targeting BTK, this compound modulates B cell receptor signaling pathways, offering insights into therapeutic strategies for autoimmune diseases. Its efficacy in inhibiting BTK activity makes it a valuable tool for research in immunology and inflammation.

Cat. No.

A34416

CAS No.

1133432-50-4

GDC-0834 (S-enantiomer)

GDC-0834 (S-enantiomer) is a potent and selective Bruton’s tyrosine kinase (BTK) inhibitor. It demonstrates significant activity in disrupting B-cell receptor signaling, making it valuable for research focusing on B-cell malignancies and autoimmune diseases. This compound is particularly useful in studies evaluating the therapeutic potential of BTK inhibition in various hematological disorders.

Cat. No.

A34417

CAS No.

1858206-76-4

BTK inhibitor 17

BTK Inhibitor 17 is a potent, orally active irreversible inhibitor of Bruton's Tyrosine Kinase (BTK), exhibiting an IC50 value of 2.1 nM. This compound demonstrates significant inhibitory activity, making it a valuable tool in the study of rheumatoid arthritis and related inflammatory diseases. Its effectiveness in BTK-related signaling pathways provides insights into therapeutic approaches for conditions associated with B-cell malignancies and autoimmune disorders.

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.

A34419

CAS No.

2283349-24-4

BGB-8035

BGB-8035 is a highly selective bruton's tyrosine kinase (BTK) inhibitor, exhibiting an IC50 of 1.1 nM for BTK, while demonstrating lower activity against TEC and EGFR with IC50 values of 99 nM and 621 nM, respectively. This compound displays significant antitumor and anti-arthritis properties, making it a valuable tool for investigating B-cell malignancies and autoimmune diseases. BGB-8035 is ideal for research applications focused on targeted therapies in hematological tumors and related pathologies.

Cat. No.

A34420

CAS No.

1575591-66-0

(E/Z)-Rilzabrutinib

Synonyms: (E/Z)-PRN1008

(E/Z)-Rilzabrutinib is a cis-trans isomer of the Bruton's Tyrosine Kinase (BTK) inhibitor Rilzabrutinib. This compound targets BTK, a critical regulator of B-cell receptor signaling, and plays a significant role in immune response modulation. It is utilized in research applications focused on autoimmune disorders and certain types of hematological malignancies, contributing to the understanding of BTK's role in disease pathology.

Cat. No.

A34421

CAS No.

121-40-4

Terreic acid

Terreic acid, a quinone epoxide antibiotic, serves as a potent inhibitor of Bruton’s tyrosine kinase (Btk) by disrupting the interaction between protein kinase C (PKC) and the pleckstrin homology domain of Btk. This compound effectively inhibits the binding of GST-BtkPH to PKC in lysates of human mast cells (HMC-1), demonstrating an IC50 value of approximately 100 μM. Its ability to modulate Btk activity makes terreic acid a valuable reagent for research applications involving immune signaling and mast cell function.

Cat. No.

A34422

CAS No.

1579278-92-4

QL47B

QL47B is a biotinylated inhibitor of Bruton's tyrosine kinase (BTK), exhibiting a potent inhibitory effect with an IC50 value of 1.3 μM. This compound demonstrates significant anti-tumor activity, making it valuable for research in cancer therapeutics and cellular signaling pathways involving BTK modulation. Its biotinylation allows for easy detection in experimental settings, enhancing its utility in biochemical assays and studies of BTK-related mechanisms.

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.

A34424

CAS No.

2101700-14-3

(R)-Pirtobrutinib

Synonyms: (R)-LOXO-305

(R)-Pirtobrutinib ((R)-LOXO-305) is an enantiomer of the BTK inhibitor Pirtobrutinib, primarily targeting Bruton's Tyrosine Kinase (BTK), which plays a critical role in B-cell receptor signaling. While exhibiting reduced activity compared to its counterpart, this compound serves as a valuable tool for studying the impact of BTK inhibition on various B-cell malignancies. It is particularly useful in research exploring resistance mechanisms associated with BTK C481 substitution mutations.

Cat. No.

A34426

CAS No.

2068022-09-1

Dihydrodiol-Ibrutinib-d5

Synonyms: PCI-45227-d5

Dihydrodiol-Ibrutinib-d5 is a deuterium-labeled form of Dihydrodiol-Ibrutinib, a potent Bruton’s tyrosine kinase (BTK) inhibitor. This active metabolite exhibits inhibitory activity towards BTK that is approximately 15 times lower than that of its parent compound, ibrutinib. Dihydrodiol-Ibrutinib-d5 serves as a valuable tool for investigating the pharmacokinetics and metabolic pathways of BTK inhibition in various research applications, particularly within cancer therapeutics.

Cat. No.

A34427

CAS No.

1643570-23-3

(R)-Elsubrutinib

Synonyms: (R)-ABBV-105

(R)-Elsubrutinib is a potent Bruton tyrosine kinase (Btk) inhibitor. By selectively inhibiting Btk, this compound modulates B-cell signaling pathways, making it valuable for investigating immune disorders such as rheumatoid arthritis, psoriasis, and systemic lupus erythematosus, as well as certain malignancies. Its applications extend to preclinical research, providing insights into the therapeutic potential of targeting Btk in various disease contexts.

Cat. No.

A34428

CAS No.

1579278-89-9

QL47R

QL47R is an isosteric analogue of QL47, specifically designed for research involving BTK inhibition. At concentrations below 10 μM, QL47R does not exhibit significant biochemical kinase activity against BTK, nor does it demonstrate antiproliferative effects on B-Cell Lymphoma Cell Lines. This compound is useful for studies focused on the characterization of BTK-related pathways and the development of targeted therapies.

Cat. No.

A34429

CAS No.

2411771-95-2

JS25

JS25 is a selective covalent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting an IC50 value of 5.8 nM through chelation of Tyr551. This compound demonstrates potent anti-proliferative effects on cancer cells, induces apoptosis, and has shown efficacy in promoting tumor regression in murine xenograft models of Burkitt's lymphoma. Notably, JS25 effectively crosses the blood-brain barrier, making it a valuable tool for research in brain-related malignancies.

Cat. No.

A34430

CAS No.

2376726-26-8

BTK inhibitor 13

BTK inhibitor 13 is a highly potent and selective inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 value of 1.2 nM. This compound exhibits significant biological activity in modulating BTK pathways, making it a valuable tool for research in B-cell malignancies and autoimmune disorders. Its high selectivity and potency facilitate investigations into BTK's role in various signaling pathways and potential therapeutic applications.

Cat. No.

A34431

CAS No.

2145152-06-1

BTK-IN-5

BTK-IN-5 is a covalent Bruton’s tyrosine kinase (BTK) inhibitor that effectively targets the BTK signaling pathway. This compound is instrumental in studying various medical conditions, including cardiovascular diseases, respiratory disorders, inflammation, and diabetes. Its inhibitory action on BTK makes it a valuable tool for exploring the role of BTK in disease pathogenesis and therapeutic interventions.

Cat. No.

A34432

CAS No.

2941611-57-8

CFON-026

CFON-026 is a selective, orally active non-covalent inhibitor of Bruton’s tyrosine kinase (BTK), exhibiting an IC50 of 0.27 nM. This compound demonstrates substantial antitumor efficacy against both wild-type BTK and various clinically relevant BTK resistance mutations, including C481S, T474I, L528W, and V416L. In vivo studies have shown that CFON-026 induces complete tumor regression in TMD8 xenograft models, making it a valuable tool for investigating hematological malignancies such as chronic lymphocytic leukemia and Waldenström macroglobulinemia.

Cat. No.

A34433

CAS No.

1643372-83-1

BMS-986143

BMS-986143 is a potent, orally active inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.26 nM, demonstrating significant selectivity against a range of kinases. This compound also inhibits TEC, BLK, BMX, TXK, FGR, YES1, and ITK with varying IC50 values, establishing its broad-spectrum activity. BMS-986143 is valuable for research into autoimmune diseases, providing insights into the modulation of B cell signaling and function.

Cat. No.

A34434

CAS No.

2724962-58-5

Cinsebrutinib

Cinsebrutinib is a selective inhibitor of Bruton's tyrosine kinase (BTK), demonstrating significant activity in disrupting BTK-mediated signaling pathways. This compound exhibits potential in cancer research, particularly in hematological malignancies, by inhibiting cell proliferation and survival. Researchers can utilize Cinsebrutinib to investigate the role of BTK in tumor biology and to explore therapeutic strategies targeting BTK in oncology.

Cat. No.

A34435

CAS No.

2764674-60-2

BTK-IN-14

BTK-IN-14 is a potent Bruton tyrosine kinase (BTK) inhibitor, targeting the BTK signaling pathway involved in B cell antigen receptor (BCR) and Fcγ receptor (FcγR) signaling in B and myeloid cells. This compound is instrumental for the investigation of BTK's role in various pathological conditions, including autoimmune diseases, inflammatory disorders, and certain cancers. Its efficacy makes it a valuable tool for researchers exploring BTK-related therapeutic strategies.

Cat. No.

A34436

CAS No.

1581714-50-2

BTK-IN-20

BTK-IN-20 is a selective Bruton's tyrosine kinase (BTK) inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. This compound demonstrates significant anti-inflammatory and anticancer properties, making it a valuable tool for investigating BTK's role in B-cell signaling and associated malignancies. BTK-IN-20 is suitable for research applications focusing on cancer biology and inflammation pathways.