Btk Inhibitor

Btk Inhibitors (199):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-115944

BTK-IN-9	Inhibitor
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells.

HY-176172

BTK-IN-44	Inhibitor
BTK-IN-44 (Compound 10) is a potent noncovalent inhibitor of Bruton’s tyrosine kinase (BTK) with an IC₅₀ value of 24.7 nM. BTK-IN-44 interferes with signaling pathways of B cell malignancies, showing antitumor effects in lymphoma cells. BTK-IN-44 is promising for research of B cell malignancies (such as lymphoma).

HY-120406

PLS-123	Inhibitor
LPS-123 is a covalently irreversible BTK inhibitor with an IC₅₀ of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.

HY-117628

RN983	Inhibitor
RN983 (Compound 1) is a highly selective Bruton's tyrosine kinase (Btk) inhibitor. RN983 inhibits IgG production in B-cells with an IC₅₀ of 2.5 nM and PGD2 production from mast cells with an IC₅₀ of 8.3 nM. RN983 is promising for research of asthma and other allergic diseases.

HY-182943

BTK-IN-49	Inhibitor
BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC₅₀ of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis.

HY-182671

SRX3305	Inhibitor
SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC₅₀s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL.

HY-158064

BTK-IN-36	Inhibitor
BTK-IN-36 (S-016) is a BTK inhibitor, with IC₅₀ of 0.5 nM. BTK-IN-36 can be used in cancer-related research.

HY-144170

RET-IN-14	Inhibitor
RET-IN-14 (compound 49) is a potent RET inhibitor with IC₅₀s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research

HY-151961

RSH-7	Inhibitor	99.07%
RSH-7 is a potent BTK and FLT3 inhibitor with IC₅₀s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity.

HY-150752

BTK-IN-15	Inhibitor
BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC₅₀ value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis.

HY-123117

VA5	Inhibitor
VA5 is a BTK kinaseinhibitor. VA5 has the potential to be used to study diseases associated with BTK kinase activity.

HY-169307

BTK-IN-38	Inhibitor
BTK-IN-38 (Example 125) is a potent BTK inhibitor. BTK-IN-38 inhibits DOHH2 and BT474 cells proliferation with IC₅₀s of 114 and 340 nM, respectively.

HY-180884

BTK-IN-46	Inhibitor
BTK-IN-46 (compound 24) is a reversible covalent BTK inhibitor. BTK-IN-46 covalently labels a lysine in the inositol phosphate (PIP3) binding site, thereby blocking Pleckstrin homology (PH) domain-mediated membrane recruitment and activation of BTK.

HY-143720

JAK3/BTK-IN-5	Inhibitor
JAK3/BTK-IN-5 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-5 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147953A1, example 35)

HY-182293

BTK-IN-48	Inhibitor
BTK-IN-48 is a BTK inhibitor with an IC₅₀ of 1.14 μM. BTK-IN-48 inhibits recombinant BTK and c-Src, and exerts moderate inhibitory effects on LCK, BMX/ETK, FLT3 and PIM1. BTK-IN-48 can be used in the research of B-cell malignancies and autoimmune diseases.

HY-148594

BTK-IN-23	Inhibitor
BTK-IN-23 is a BTK inhibitor (IC₅₀: 12.8 nM). BTK-IN-23 also inhibits BLX and BMX with IC₅₀s of 35.6 and 5.7 nM respectively. BTK-IN-23 shows improved kinase selectivity compared to Ibrutinib (HY-10997).

HY-172589

BTK-IN-43	Inhibitor
BTK-IN-43 (compound 9) is an inhibitor of BTK with an IC₅₀ value of 21.6 nM. BTK-IN-43 has oral activity.

HY-147784

HZ-A-005	Inhibitor
HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models.

HY-142932

BTK-IN-6	Inhibitor
BTK-IN-6 is a potent inhibitor of Bruton's Tyrosine Kinase (BTK). BTK is a member of the Tec family of tyrosine kinases and plays an important role in the regulation of early B-cell development and mature B-cell activation and survival. BTK-IN-6 has the potential for the research of immune disorders, cancer, cardiovascular diseases, viral infections, inflammation, metabolism/endocrine function disorders, and neurological disorders (extracted from patent WO2021136219A1, compound 8).

HY-162081

BTK-IN-32	Inhibitor
BTK-IN-32 (compound C2) is a potent inhibitor of BTK. BTK-IN-32 activates full-length BTK and smaller multidomain BTK fragments instead of the isolated kinase domain.

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