BTK

Cat. No.

A30952

CAS No.

2031152-08-4

XMU-MP-3

XMU-MP-3 is a potent non-covalent inhibitor of Bruton's tyrosine kinase (BTK), exhibiting IC50 values of 10.7 nM for wild-type BTK and 17.0 nM for the C481S mutation in the presence of 10 μM ATP. This compound is known to induce apoptosis in BTK-dependent cells, making it a valuable tool for investigating B-cell receptor signaling and related pathways. XMU-MP-3 is applicable in research focused on hematological malignancies and immune responses.

Cat. No.

A31568

CAS No.

2649008-95-5

TM471-1

TM471-1 is a potent and covalent inhibitor of Bruton's tyrosine kinase (BTK), demonstrating an IC50 of 1.3 nM against BTKWT and exhibiting selectivity with IC50 values of >40,000 nM for BTKC481S, 7.9 nM for TEC, and 12.4 nM for TXK. This compound effectively inhibits cell proliferation both in vivo and in vitro, induces apoptosis, and causes arrest in the G0/G1 phase of the cell cycle. TM471-1 is valuable for research into the roles of BTK in various cancer types and related signaling pathways.

Cat. No.

A32244

CAS No.

2952702-39-3

BTK-IN-7

BTK-IN-7 is a potent and selective Bruton’s Tyrosine Kinase (BTK) inhibitor, exhibiting an IC50 of 4.0 nM. This compound demonstrates exceptional selectivity in enzymatic assays, with over 250-fold selectivity for ITK and over 2500-fold for EGFR, as well as in cellular contexts with a 227-fold and 27-fold selectivity respectively. BTK-IN-7 exhibits significant antitumor activity, making it a valuable tool for research in cancer biology and the development of targeted therapies.

Cat. No.

A32299

CAS No.

2361192-21-2

BTK-IN-9

BTK-IN-9 is a reversible Bruton's tyrosine kinase (BTK) inhibitor known for its potent antiproliferative effects against mantle cell lymphoma. This compound disrupts mitochondrial membrane potential and elevates reactive oxygen species levels in Z138 cells, leading to increased apoptotic activity. BTK-IN-9 is valuable for research applications focusing on lymphoma biology and the mechanisms of apoptosis.

Cat. No.

A33280

CAS No.

62004-35-7

LFM-A13

LFM-A13 is a selective Bruton's tyrosine kinase (BTK) inhibitor known for its capacity to inhibit JAK2 and PLK. With IC50 values of 2.5 μM for recombinant BTK, 10 μM for JAK2, and 61 μM for PLK3, LFM-A13 exhibits significant antiproliferative and anticancer properties. This compound is valuable for research applications focused on cancer biology and therapeutic interventions targeting BTK and related signaling pathways.

Cat. No.

A33337

CAS No.

2674036-98-5

JAK3/BTK-IN-3

JAK3/BTK-IN-3 is a selective inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). Targeting both JAK3 and BTK can provide synergistic effects beneficial for the therapeutic intervention of autoimmune diseases. This compound is suitable for research applications focused on elucidating the roles of JAK3 and BTK in various disease mechanisms, facilitating the development of novel treatment strategies.

Cat. No.

A33341

CAS No.

2844387-16-0

JAK3/BTK-IN-7

JAK3/BTK-IN-7 is a potent inhibitor targeting Janus kinase 3 (JAK3) and Bruton’s tyrosine kinase (BTK), demonstrating IC50 values of 2 nM and 14 nM, respectively. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for investigating the underlying mechanisms of rheumatoid arthritis. Its efficacy in modulating inflammatory pathways highlights its potential in related therapeutic research applications.

Cat. No.

A33373

CAS No.

2674036-93-0

JAK3/BTK-IN-2

JAK3/BTK-IN-2 is a potent dual inhibitor of Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). By simultaneously targeting the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that may enhance therapeutic outcomes in autoimmune diseases. JAK3/BTK-IN-2 is suitable for research applications focused on JAK3 and BTK-related pathologies, facilitating studies on their roles in immune regulation and disease progression.

Cat. No.

A33401

CAS No.

2673196-75-1

JAK3/BTK-IN-5

JAK3/BTK-IN-5 is a potent dual inhibitor targeting Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK). This compound effectively disrupts the BTK/JAK3 signaling pathway, demonstrating potential synergistic effects advantageous for the treatment of autoimmune diseases. JAK3/BTK-IN-5 is valuable for research into conditions related to JAK3 kinase and BTK, making it a crucial tool for studying the pathophysiology of these targets.

Cat. No.

A33420

CAS No.

2243136-03-8

JAK3/BTK-IN-6

JAK3/BTK-IN-6 is a potent dual inhibitor targeting Bruton's Tyrosine Kinase (BTK) and Janus Kinase 3 (JAK3), exhibiting IC50 values of 0.6 nM and 0.4 nM, respectively. This compound demonstrates excellent metabolic stability in human liver microsomes, making it suitable for in vitro studies. JAK3/BTK-IN-6 is valuable in research applications related to hematological disorders and immune system dysfunctions.

Cat. No.

A33425

CAS No.

2673196-38-6

JAK3/BTK-IN-4

JAK3/BTK-IN-4 is a potent inhibitor targeting both JAK3 and BTK kinases, which are critical in the modulation of immune responses involved in autoimmune diseases. By simultaneously inhibiting the BTK/JAK3 signaling pathway, JAK3/BTK-IN-4 demonstrates synergistic effects, making it a valuable tool for studying JAK3 and BTK-related pathologies. This compound is particularly relevant for research applications focused on therapeutic strategies for autoimmune disorders.

Cat. No.

A33443

CAS No.

2674036-91-8

JAK3/BTK-IN-1

JAK3/BTK-IN-1 is a potent dual inhibitor targeting JAK3 and BTK, key proteins implicated in autoimmune diseases. By simultaneously blocking the BTK/JAK3 signaling pathway, this compound demonstrates synergistic effects that could enhance therapeutic outcomes. JAK3/BTK-IN-1 is suitable for research into JAK3 kinase and BTK-related diseases, facilitating the exploration of innovative treatment strategies in immunology and related fields.

Cat. No.

A33707

CAS No.

2764609-97-2

RSH-7

RSH-7 is a potent inhibitor of Bruton's tyrosine kinase (BTK) and Fms-like tyrosine kinase 3 (FLT3), exhibiting IC50 values of 47 nM and 12 nM, respectively. This compound induces apoptosis and demonstrates significant antiproliferative activity. By inhibiting BTK and FLT3 signaling pathways, RSH-7 is a valuable tool for research in oncology and targeted therapies for hematological malignancies.

Cat. No.

A34381

CAS No.

2101700-15-4

Pirtobrutinib

Synonyms: LOXO-305

Pirtobrutinib is a highly selective, non-covalent inhibitor of Bruton's tyrosine kinase (BTK). It effectively targets diverse BTK C481 substitution mutations, demonstrating strong antitumor activity in BTK-dependent lymphoma models in vivo. Pirtobrutinib exhibits over 300-fold selectivity for BTK compared to a panel of 370 other kinases and shows minimal inhibition of non-kinase off-targets at 1 μM. This specificity makes it a valuable tool for studying BTK-related signaling pathways and therapeutic applications in hematological malignancies.

Cat. No.

A34382

CAS No.

72707-66-5

2-(Bromomethyl)acrylic acid

Synonyms: α-(Bromomethyl)acrylic acid; α-Methylated acrylamide; α-MAA

2-(Bromomethyl)acrylic acid functions as a selective inhibitor of Bruton's tyrosine kinase (BTK). It covalently modifies the cysteine 481 residue of BTK through a nucleophilic addition-elimination mechanism, leading to the inhibition of the B-cell receptor signaling pathway. This compound promotes immunogenic cell death in BTK-expressing B-cell lymphoma cells by triggering the release of damage-associated molecular patterns like extracellular ATP and HMGB1. It exhibits significant cytotoxicity against BTK-expressing cells while demonstrating minimal toxicity to BTK-negative counterparts, making it valuable for research into B-cell lymphoma.

Cat. No.

A34383

CAS No.

2242394-65-4

Acalabrutinib maleate

Synonyms: Calquence maleate; ACP-196 maleate

Acalabrutinib maleate is an oral, irreversible, and highly selective BTK inhibitor targeting cysteine residue Cys481 in the ATP-binding pocket of BTK. This compound exhibits potent activity against chronic lymphocytic leukemia (CLL) in mouse models, making it a valuable tool for CLL research. Additionally, Acalabrutinib maleate features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating its use in click chemistry applications.

Cat. No.

A34384

CAS No.

1971920-73-6

Tolebrutinib

Synonyms: SAR442168; PRN2246

Tolebrutinib, a selective inhibitor of Bruton tyrosine kinase (BTK), demonstrates potent activity with IC50 values of 0.4 nM in Ramos B cells and 0.7 nM in HMC microglia cells. Its ability to penetrate the blood-brain barrier underscores its relevance in studying central nervous system immunity. Tolebrutinib is a valuable tool for research into multiple sclerosis (MS) and other neurological conditions influenced by BTK activity.

Cat. No.

A34386

CAS No.

2247614-80-6

BIIB091

BIIB091 is a selective and potent reversible Bruton’s tyrosine kinase (BTK) inhibitor, demonstrating an IC50 of less than 0.5 nM. By binding to the BTK protein and inducing an inactive conformation via sequestering of TYR-551, BIIB091 effectively obstructs BTK signaling pathways. This compound is valuable for research applications in multiple sclerosis and other immune-mediated disorders.

Cat. No.

A34388

CAS No.

1643570-24-4

Elsubrutinib

Synonyms: ABBV-105

Elsubrutinib is a potent and selective irreversible inhibitor of Bruton's tyrosine kinase (BTK). With an IC50 value of 0.18 μM for the BTK catalytic domain, it demonstrates strong inhibitory activity. Elsubrutinib is utilized in research related to inflammatory diseases, providing valuable insights into BTK's role in various cellular processes.

Cat. No.

A34389

CAS No.

330786-01-1

KIN-8194

KIN-8194 is an orally active dual inhibitor targeting HCK and BTK, exhibiting IC50 values of 0.915 nM and

Cat. No.

A34390

CAS No.

1621002-24-1

PF-06658607

PF-06658607 is an alkynylated irreversible inhibitor of Bruton's tyrosine kinase (BTK), designed to covalently bind to active site cysteines in the ATP-binding pocket. This compound effectively serves as a research tool for identifying off-target effects of covalent kinase inhibitors in cancer cell models. Its unique alkyne functionality facilitates the use of azide-based detection probes through copper-catalyzed click chemistry, enhancing the study of BTK-related signaling pathways.

Cat. No.

A34391

CAS No.

1469988-63-3

QL-X-138

QL-X-138 is a selective dual inhibitor of Bruton's tyrosine kinase (BTK) and MAPK-interacting kinase (MNK), demonstrating potent covalent binding to BTK and non-covalent binding to MNK. It exhibits IC50 values of 9.4 nM for BTK, and 107.4 nM and 26 nM for MNK1 and MNK2, respectively. Additionally, QL-X-138 displays antiviral activity against dengue virus serotype 2, with an IC50 of 3.5 μM. This compound is valuable for research involving B-cell malignancies and related therapeutic investigations.

Cat. No.

A34394

CAS No.

2694871-86-6

BLK-IN-2

BLK-IN-2 is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), exhibiting an IC50 of 5.9 nM. In addition, it inhibits Bruton’s tyrosine kinase (BTK) with an IC50 of 202 nM. This compound demonstrates strong antiproliferative activity against various lymphoma cell lines, making it a valuable tool for research in B-cell malignancies and related signaling pathways.

Cat. No.

A34395

CAS No.

1202758-21-1

CNX-500

CNX-500 is a covalent probe that targets Bruton's tyrosine kinase (Btk) through a potent inhibitor (CC-292) chemically linked to biotin. With an IC50 of 0.5 nM, CNX-500 exhibits strong inhibitory activity against Btk while forming a stable covalent bond. The compound demonstrates low off-target effects on epidermal growth factor receptor and upstream Src-family kinases such as Syk and Lyn, making it suitable for research applications focused on Btk-related pathways in cellular signaling and disease models.

Cat. No.

A34396

CAS No.

2231747-18-3

N-piperidine Ibrutinib hydrochloride

N-piperidine Ibrutinib hydrochloride is a reversible derivative of Ibrutinib, functionally acting as a potent Bruton Tyrosine Kinase (BTK) inhibitor. It demonstrates IC50 values of 51.0 nM for wild-type BTK and 30.7 nM for the C481S mutant. This compound serves as a valuable BTK ligand in the synthesis of PROTACs, including SJF620, which has shown a DC50 of 7.9 nM, highlighting its potential utility in targeted protein degradation research applications.