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BTK+inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (1) Antibiotic (1) Apoptosis (13) BCRP (1) BMX Kinase (4) Btk (123) Calcium Channel (1) Caspase (1) CCR (1) Cytochrome P450 (2) Drug Intermediate (1) Drug Isomer (1) Drug Metabolite (2) EGFR (5) ERK (1) Fc Receptor (FcR) (1) FLT3 (2) Fluorescent Dye (2) HMG Family (1) Interleukin Related (1) Isotope-Labeled Compounds (3) JAK (1) Ligands for Target Protein for PROTAC (3) Molecular Glues (1) mTOR (1) p38 MAPK (1) PARP (1) PERK (1) Pim (1) PROTACs (1) Pyroptosis (1) Reference Standards (9) Src (3) Syk (1) TNF Receptor (1) Toll-like Receptor (TLR) (2)
By Research Areas:	Cancer (89) Cardiovascular Disease (3) Endocrinology (1) Infection (3) Inflammation/Immunology (51) Metabolic Disease (4) Neurological Disease (4)
Click Chemistry:	Azide (1) Alkynes (1)

125

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10997

Ibrutinib Maximum Cited Publications 126 Publications Verification PCI-32765	Btk Ligands for Target Protein for PROTAC	Infection Inflammation/Immunology Cancer
Ibrutinib (PCI-32765) is a selective, irreversible *Btk* inhibitor with an IC₅₀ of 0.5 nM .

HY-101474A

Zanubrutinib 20+ Cited Publications BGB-3111	Btk	Cancer
Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC₅₀: 0.3 nM) .

HY-128757

Remibrutinib 5 Publications Verification LOU064	Btk	Inflammation/Immunology Cancer
Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC₅₀ value of 1 nM. Remibrutinib inhibits BTK activity with an IC₅₀ value of 0.023 μM in blood . Remibrutinib has the potential for Chronic urticaria (CU) treatment .

HY-19834

Fenebrutinib 10+ Cited Publications GDC-0853	Btk	Cancer
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with K_is of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .

HY-129390

Orelabrutinib 3 Publications Verification ICP-022	Btk	Cancer
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK .

HY-15771

Tirabrutinib 5+ Cited Publications ONO-4059; GS-4059	Btk Apoptosis	Inflammation/Immunology Cancer
Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC₅₀ of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies .

HY-19816

Avitinib 3 Publications Verification Abivertinib; AC0010	EGFR Btk Apoptosis	Cancer
Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a *BTK* inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects .

HY-101215

Evobrutinib 5+ Cited Publications M2951; MSC2364447C	Btk	Inflammation/Immunology Cancer
Evobrutinib (M2951) is an orally active, potent, highly selective and irreversibly covalent *BTK* inhibitor, with an IC₅₀ of 8.9 nM. Evobrutinib (M2951) can be used for the research of autoimmune diseases .

HY-13036A

IBT6A	Btk	Cancer
IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-19816A

Avitinib maleate 3 Publications Verification Abivertinib maleate; AC0010 maleate	EGFR Btk Apoptosis	Cancer
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a *BTK* inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .

HY-18018

RN486 3 Publications Verification	Btk	Inflammation/Immunology
RN486 is a potent, selective and orally active *Btk* inhibitor with an IC₅₀ of 4.0 nM and a K_d of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research .

HY-109010

Poseltinib 2 Publications Verification HM71224; LY3337641	Btk BMX Kinase Toll-like Receptor (TLR)	Metabolic Disease
Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC₅₀ of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis .

HY-135334

ACP-5862 1 Publications Verification	Drug Metabolite Btk Cytochrome P450	Cancer
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC₅₀ of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC₅₀ of 3 nM and EC₅₀ of 8 nM .

HY-78727

Ibrutinib deacryloylpiperidine IBT4A	Drug Intermediate Btk	Inflammation/Immunology Cancer
Ibrutinib deacryloylpiperidine (IBT4A) is a derivative of an Ibrutinib (HY-10997) intermediate and an Ibrutinib impurity. Ibrutinib deacryloylpiperidine serves as a starting material and is used in the synthesis of a modified *BTK* inhibitor derivative via the Mitsunobu reaction .

HY-109143

Elsubrutinib 2 Publications Verification ABBV-105	Btk	Inflammation/Immunology
Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor. The IC₅₀ of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .

HY-139535

Luxeptinib 1 Publications Verification CG-806	FLT3 Btk Apoptosis	Cancer
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent *pan-FLT3/pan-BTK* inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .

HY-15771A

Tirabrutinib hydrochloride 5+ Cited Publications ONO-4059 hydrochloride; GS-4059 hydrochloride	Btk Apoptosis	Inflammation/Immunology Cancer
Tirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC₅₀ of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies .

HY-13943

CNX-774 2 Publications Verification	Btk	Cancer
CNX-774 is an orally active, irreversible and selective *BTK* inhibitor, with an IC₅₀ of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification .

HY-139984

BIIB091	Btk	Neurological Disease Inflammation/Immunology
BIIB091 is a potent, selective, orally active and reversible *BTK* inhibitor, with an IC₅₀ of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis .

HY-15427

GDC-0834 1 Publications Verification	Btk	Inflammation/Immunology Cancer
GDC-0834 is an orally active selective, potent, and reversible *BTK* inhibitor with an IC₅₀ of 5.9 nM. GDC-0834 demonstrates pBTK-Tyr223 inhibition in mice and rats. GDC-0834 can be used for research of rheumatoid arthritis (RA) .

HY-15809

(Rac)-Ibrutinib alkyne	Btk Calcium Channel	Inflammation/Immunology
(Rac)-Ibrutinib alkyne (Compound 8) is a *Btk* inhibitor with an IC₅₀ of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC₅₀ of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis .

HY-100338

CNX-500	Btk	Cancer
CNX-500 is a probe consisting of a covalent *Btk* inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC₅₀ of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn .

HY-132879

TAK-020	Btk	Inflammation/Immunology
TAK-020 is a covalent *Btk* inhibitor, which becomes the clinical candidate.

HY-101941

BTK IN-1 SNS062 analog	Btk	Inflammation/Immunology Cancer
BTK IN-1 (SNS062 analog) is a potent *BTK* inhibitor, with an IC₅₀ of <100 nM.

HY-10997A

Ibrutinib Racemate 1 Publications Verification PCI-32765 Racemate	Btk	Cancer
Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible *Btk* inhibitor with IC₅₀ value of 0.5 nM.

HY-18951

ONO-4059 analog 3 Publications Verification	Btk Apoptosis	Cancer
ONO-4059 analog is an analogue of ONO-4059, and ONO-4059 (HY-15771) is a highly potent and selective Btk inhibitor.

HY-151232

(E/Z)-Rilzabrutinib (E/Z)-PRN1008	Btk	Inflammation/Immunology
(E/Z)-Rilzabrutinib ((E/Z)-PRN1008) is a cis-trans isomer of Rilzabrutinib (HY-112166). Rilzabrutinib is a BTK inhibitor .

HY-10997R

Ibrutinib (Standard) PCI-32765 (Standard)	Reference Standards Btk Ligands for Target Protein for PROTAC	Cancer
Ibrutinib (Standard) is the analytical standard of Ibrutinib. This product is intended for research and analytical applications. Ibrutinib (PCI-32765) is a selective, irreversible *Btk* inhibitor with an IC₅₀ of 0.5 nM .

HY-153245

JNJ-64264681	Btk	Inflammation/Immunology Cancer
JNJ-64264681 is a potent, orally active, selective and irreversible covalent *BTK* inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research .

HY-12679

PF-06658607	Btk	Cancer
PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry .

HY-17600S

Acalabrutinib-d4 ACP-196-d₄	Btk	Cancer
Acalabrutinib-d₄ (ACP-196-d₄) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-128403

*BTK inhibitor* 8**	Btk	Inflammation/Immunology
BTK inhibitor 8 (Compound 27) is a *Btk* inhibitor with an IC₅₀ of 0.11 nM. BTK inhibitor 8 inhibits Btk activity. BTK inhibitor 8 suppresses B cell activation. BTK inhibitor 8 is applicable to research related to arthritis and asthma .

HY-101766

*Btk inhibitor* 2**	Btk	Inflammation/Immunology
Btk inhibitor 2 is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.

HY-109143B

(R)-Elsubrutinib (R)-ABBV-105	Btk	Inflammation/Immunology Cancer
(R)-Elsubrutinib ((R)-ABBV-105) is a *Btk* inhibitor. (R)-Elsubrutinib can be used in studies of immune diseases (such as rheumatoid arthritis, psoriasis, ankylosing spondylitis, asthma, systemic lupus erythematosus) and cancer .

HY-101474AR

Zanubrutinib (Standard) BGB-3111 (Standard)	Reference Standards Btk	Cancer
Zanubrutinib (Standard) is the analytical standard of Zanubrutinib. This product is intended for research and analytical applications. Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC₅₀: 0.3 nM) .

HY-131328A

(R)-Pirtobrutinib (R)-LOXO-305	Btk	Others
(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations .

HY-13036

(Rac)-IBT6A	Btk	Cancer
(Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-136531

XMU-MP-3	Btk Apoptosis	Cancer
XMU-MP-3 is a potent non-covalent *BTK* inhibitor with IC₅₀s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis .

HY-15427A

GDC-0834 Racemate	Btk Drug Isomer	Inflammation/Immunology
GDC-0834 Racemate is the racemic form of GDC-0834 (HY-15427). GDC-0834 is an orally active selective, potent, and reversible *BTK* inhibitor with an IC₅₀ of 5.9 nM. GDC-0834 demonstrates pBTK-Tyr223 inhibition in mice and rats. GDC-0834 can be used for research of rheumatoid arthritis (RA) .

HY-130255

*BTK inhibitor* 13**	Btk	Inflammation/Immunology
BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC₅₀ of 1.2 nM .

HY-152212

BTK-IN-19	Btk	Inflammation/Immunology
BTK-IN-19 (Compound 51) is a reversible *BTK* inhibitor with an IC₅₀ of <0.001 μM .

HY-15427B

GDC-0834 (S-enantiomer)	Btk	Others
GDC-0834 (S-enantiomer) is the S-enantiomer of GDC-0834. GDC-0834 is a potent and selective BTK inhibitor.

HY-136113

Ibrutinib dimer	Btk	Cancer
Ibrutinib dimer is a Dimer of Ibrutinib. Ibrutinib dimer is an impurity of Ibrutinib . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-10997S

Ibrutinib-d5 PCI-32765-d₅	Btk	Cancer
Ibrutinib-d₅ (PCI-32765-d₅) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor .

HY-102036

G-744	Btk	Inflammation/Immunology
G-744 is a highly potent, selective and orally active *Btk* inhibitor with an IC₅₀ of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis .

HY-145373

BMS-986143	Btk	Inflammation/Immunology
BMS-986143 is an orally active, reversible *BTK* inhibitor with an IC₅₀ of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC₅₀s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases .

HY-18010

PCI 29732 3 Publications Verification	Btk BCRP	Inflammation/Immunology
PCI 29732 is a potent, orally active, reversible BTK inhibitor with K_i ^app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .

HY-131705

*BTK inhibitor* 17**	Btk	Inflammation/Immunology
BTK inhibitor 17 is a potent and orally active irreversible *BTK* inhibitor with an IC₅₀ of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research .

HY-139881

*BTK inhibitor* 19**	Btk	Cancer
BTK inhibitor 19 is a highly selective, covalent *BTK* inhibitor (IC₅₀ = 2.7 nM).

HY-125997

*BTK inhibitor* 10**	Btk	Inflammation/Immunology
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-110013

Terreic acid	Microorganisms Source Classification	Btk Antibiotic
Terreic acid, a quinone epoxide antibiotic, acts as an effective *Btk* inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC₅₀ of approximately 100 μM .

Cat. No.	Product Name	Chemical Structure

HY-17600S

Acalabrutinib-d4
Acalabrutinib-d₄ (ACP-196-d₄) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-10997S

Ibrutinib-d5
Ibrutinib-d₅ (PCI-32765-d₅) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor .

HY-101474S

Zanubrutinib-d5
Zanubrutinib-d₅ is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor .

HY-101474BS

(R)-Zanubrutinib-d5
(R)-Zanubrutinib-d₅ is deuterium labeled (R)-Zanubrutinib. (R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.

HY-160219S

BTK-IN-33
BTK-IN-33 is a *Btk* inhibitor with anticancer effects (WO2023174300A1; compound I) .

HY-W757743

Acalabrutinib-d3
Acalabrutinib-d₃ (ACP-196-d₃) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).

HY-135334S

ACP-5862-d4

ACP-5862-d₄ is deuterium labeled ACP-5862. ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC₅₀ of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC₅₀ of 3 nM and EC₅₀ of 8 nM .

Cat. No.	Product Name		Classification

HY-15809

(Rac)-Ibrutinib alkyne		Alkynes
(Rac)-Ibrutinib alkyne (Compound 8) is a *Btk* inhibitor with an IC₅₀ of 0.72 nM. (Rac)-Ibrutinib alkyne can effectively inhibit functions related to the B-cell receptor signaling pathway, with an IC₅₀ of 9 nM for inhibiting Ca flux in Ramos cells. (Rac)-Ibrutinib alkyne can be used in the research of diseases such as rheumatoid arthritis .

HY-159589

BTK-IN-37		Azide
BTK-IN-37 (compound 8d) is a *BTK* inhibitor that can induce apoptosis in cancer cells. BTK-IN-37 targets BTK with K_i and IC₅₀ of 5.07 nM and 3.6 nM, respectively. BTK-IN-37 can also selectively induce enrichment of genes involved in necroptosis and pyroptosis .

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