BTK

Cat. No.

A24841

CAS No.

2416130-57-7

NRX-0492

NRX-0492 is an orally active PROTAC BTK degrader that promotes the ubiquitination and proteasomal degradation of Bruton's tyrosine kinase (BTK) with DC50 values as low as 0.2 nM. This compound effectively inhibits B cell receptor (BCR)-mediated signaling, transcriptional programs, and chemokine secretion, demonstrating significant antitumor activity against chronic lymphocytic leukemia. NRX-0492 comprises a BTK inhibitor, an E3 ligase ligand derived from Thalidomide, and a PROTAC linker, making it a valuable tool for studying BTK-related pathways and therapies.

Cat. No.

A25707

CAS No.

1431727-04-6

PLS-123

PLS-123 is a covalent, irreversible inhibitor of Bruton's tyrosine kinase (BTK), displaying an IC50 of less than 5 nM. It effectively disrupts BTK's catalytic activity at Tyr551 and self-activation at Tyr223, leading to the inhibition of key signaling pathways, including AKT/mTOR and MAPK, as well as blocking PLCγ2 activation. PLS-123 exhibits potent anti-proliferative effects against a range of B-cell lymphoma cell lines, inducing apoptosis through a caspase-dependent mechanism. Additionally, it demonstrates substantial antitumor efficacy in the OCI-Ly7 xenograft model, making it a valuable tool for research in lymphoma.

Cat. No.

A26245

CAS No.

1415823-49-2

TL-895

TL-895 is a potent, orally bioavailable, irreversible inhibitor of Bruton's tyrosine kinase (BTK) that functions as an ATP-competitive agent. It demonstrates high selectivity with an average IC50 of 1.5 nM against recombinant BTK and minimal activity against BLK, BMX, and TXK. TL-895 effectively inhibits BTK auto-phosphorylation at the Y223 site (IC50: 1-10 nM) and suppresses the production of inflammatory cytokines such as IL-8, IL-1β, MCP-1, and TNF-α in monocytes and macrophages. This compound is valuable for investigating chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and various B-cell malignancies.

Cat. No.

A28621

CAS No.

1466445-39-5

EGFR-IN-40

EGFR-IN-40 is a selective inhibitor targeting Bruton's tyrosine kinase (BTK), epidermal growth factor receptor (EGFR), and IL-2-inducible T-cell kinase (ITK). It exhibits potent inhibitory activity with IC50 values of 1.2 nM for BTK, 5.3 nM for EGFR, and 46.1 nM for ITK. This compound is valuable for research applications focusing on cancer therapeutics and signaling pathways related to these kinases.

Cat. No.

A28880

CAS No.

2370013-49-1

(S)-Sunvozertinib

Synonyms: (S)-DZD9008

(S)-Sunvozertinib, the S-enantiomer of Sunvozertinib, acts as a selective inhibitor of the ErbB family of receptors and Bruton's tyrosine kinase (BTK). It demonstrates potent inhibitory activity against multiple oncogenic variants of EGFR, including exon 20 insertions and the L858R/T790M mutation, with IC50 values of 51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively. Due to its dual action on both ErbBs and BTK, (S)-Sunvozertinib is poised for applications in targeted cancer therapy and research into mechanisms of resistance in EGFR-driven malignancies.

Cat. No.

A28922

CAS No.

2485861-07-0

Rocbrutinib

Synonyms: LP-168

Rocbrutinib is a highly selective Bruton's tyrosine kinase (BTK) inhibitor, exhibiting an IC50 of 0.11 nM for wild-type BTK and 1.0 nM for the C481S-mutated variant. It demonstrates significant anti-leukemic activity by reducing cell viability, inducing cytotoxic effects, and inhibiting cell migration. This compound is applicable in research surrounding chronic lymphocytic leukemia, non-Hodgkin's lymphoma, and mantle cell lymphoma.

Cat. No.

A30403

CAS No.

1616428-23-9

Luxeptinib

Synonyms: CG-806

Luxeptinib is a first-in-class, non-covalent pan-FLT3 and pan-BTK inhibitor that exhibits potent oral activity. This compound effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells, making it a significant tool for cancer research. Its dual-targeting mechanism positions Luxeptinib as a potential therapeutic candidate in the treatment of hematological malignancies.

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.

A31585

CAS No.

3092208-36-8

DFCI-002-06

DFCI-002-06 is an orally active PROTAC degrader targeting both HCK and BTK, demonstrating DC₅₀ values of 1.3 nM and 4.5 nM, respectively. This compound exhibits superior anti-tumor activity compared to a dual-target inhibitor, promoting apoptosis in cancer cells, particularly in MYD88 mutant B-cell malignancies. DFCI-002-06 serves as a valuable tool for researching mechanisms underlying these specific cancer types.

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.