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BTK ligand

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (29) E3 Ligase Ligand-Linker Conjugates (5) ByeTAC (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (1) Itk (1) Ligands for E3 Ligase (4) Ligands for Target Protein for PROTAC (11) Molecular Glues (1) NF-κB (1) p38 MAPK (1) PROTAC Linkers (1) PROTACs (21) Toll-like Receptor (TLR) (2) Tyrosinase (1)
By Research Areas:	Cancer (38) Cardiovascular Disease (1) Inflammation/Immunology (6)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Btk Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-49421

BTK ligand 12	Ligands for Target Protein for PROTAC	Cancer
BTK ligand 12 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BTK ligand 12 can serve as an active control for the target protein ligand of NRX-0492 (HY-153357) .

HY-175543

BTK ligand 16	Ligands for Target Protein for PROTAC Btk	Cancer
BTK ligand 16 is a *BTK* ligand that can be used for synthesis of TQ-3959 (HY-175541) .

HY-168302

BTK ligand 10	Ligands for Target Protein for PROTAC Tyrosinase Btk	Cancer
BTK ligand 10 is the ligand of *BTK. BTK* ligand 10 can be used to synthesize NX-2127 (HY-153220) .

HY-168965

BTK ligand 15	Ligands for Target Protein for PROTAC	Others
BTK ligand 15 is the target protein ligand of PROTAC BTK Degrader-13 (HY-168963). PROTAC BTK Degrader-13 can selectively degrade *BTK* .

HY-150885

BTK ligand 1	Ligands for Target Protein for PROTAC Btk	Cancer
BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting *Btk* can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies .

HY-173126

BTK ligand-14	Btk Ligands for Target Protein for PROTAC	Others
BTK ligand-14 is a PROTAC target protein ligand that targets *BTK* and can be used for the synthesis of FDU73 (HY-173125) .

HY-168292

BTK ligand 9	Ligands for Target Protein for PROTAC Btk	Cancer
BTK ligand 9 is a target protein ligand for *BTK* and can be used to synthesize PROTAC DD-03-171 (HY-122830) .

HY-168314

BTK ligand 11	Ligands for Target Protein for PROTAC	Cancer
BTK ligand 11 is a PROTAC target protein ligand that can be used to synthesize BCPyr (HY-142621) .

HY-159956

BTK-IN-39	Ligands for Target Protein for PROTAC	Cancer
BTK-IN-39 (0204) is a PROTAC target protein ligand that can be used to synthesize PROTAC BTK Degrader-11 (HY-159947) .

HY-130982

Lenalidomide-PEG3-iodine	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-PEG3-iodine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a 3-unit PEG linker. Lenalidomide-PEG3-iodine can be used in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC₅₀ of 7.9 nM .

HY-170413

PROTAC BTK Degrader-12	PROTACs Btk	Cancer
PROTAC BTK Degrader-12 (EXAMPLE 19) is a PROTAC-based *BTK* degrader (Pink & black: BTK ligand & linker (HY-170414); Black: linker (HY-30105); Blue: VHL ligand ( HY-W245311)) .

HY-172822

TLT8	ByeTAC Btk	Cancer
TLT8 is a ByeTAC protein degrader targeting *BTK. TLT8 non-covalently binds to Rpn-13 and BTK, thereby inducing BTK* degradation. TLT8 can be used in chronic lymphocytic leukemia research. (Rpn-13 ligand: HY-159808; BTK ligand: HY-Z3101; linker: HY-172823) .

HY-168963

PROTAC BTK Degrader-13	PROTACs Btk Itk p38 MAPK	Inflammation/Immunology Cancer
PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for *BTK* with a DC₅₀ of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of *BTK* with an IC₅₀ of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC₅₀ of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway . (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))

HY-160966

PROTAC BTK Degrader-10	PROTACs Btk	Cancer
PROTAC BTK Degrader-10 (Example 1P) is a PROTAC degrader for *BTK. PROTAC BTK* Degrader-10 can be used for research of chronic lymphocytic leukemia (CLL) (Pink: ligand for target protein (HY-170758); Black: linker (HY-W392857); Blue: ligand for E3 ligase Cereblon (HY-W733176))

HY-156746

DBt-10	PROTACs Btk	Cancer
DBt-10 is a potent *BTK* PROTAC degrader (DC₅₀: 137 nM). Blue: DCAF1 binder (HY-149934); Black: linker; Pink: BTK ligand .

HY-156745

DDa-1	PROTACs Btk	Cancer
DDa-1 is a potent *BTK* degrader (DC₅₀: 90 nM). Blue: DCAF1 binder (HY-149934), Black: linker, Pink: BTK ligand (HY-107447) .

HY-130983

N-piperidine Ibrutinib hydrochloride	Btk Ligands for Target Protein for PROTAC	Cancer
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent *BTK* inhibitor with IC₅₀s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC₅₀ of 7.9 nM .

HY-139660

*PROTAC PTK6 ligand-1*	Ligands for Target Protein for PROTAC	Cancer
PROTAC PTK6 ligand-1 is an intermediate for BTK kinase inhibitor preparation . PROTAC PTK6 ligand-1 can be used in the synthesis of ARD-61 (HY-139659) .

HY-175541

TQ-3959	PROTACs Btk	Cancer
TQ-3959 is an orally active *BTK* PROTAC degrader, with a DC₅₀ of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type *BTK* and C481S mutant *BTK* cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .

HY-173125

FDU73	PROTACs Btk	Cancer
FDU73 is a highly effective and selective BTK PROTAC degrader with a DC₅₀ of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity . (Pink: BTK ligand-14 (HY-173126); Black: Linker (HY-168297); Blue: E3 ligase ligand 59 (HY-173378); E3 ligase ligand+Linker (HY-173127))

HY-159947

PROTAC BTK Degrader-11	PROTACs Btk	Cancer
PROTAC BTK Degrader-11 is a PROTAC degrader that can break down *BTK, with a DC₅₀* of 1.7 nM. PROTAC BTK Degrader-11 can be used in cancer research. (Pink: target protein ligand (HY-159956); Black: linker; Blue: E3 ligase (HY-150839)) .

HY-W245311

*E3 ligase Ligand* 51**	Ligands for E3 Ligase	Others
E3 ligase Ligand 51 is the ligand for E3 ligase VHL, that can be used for synthesis of PROTAC BTK Degrader-12 (HY-170413) .

HY-W733176

*E3 ligase Ligand* 50**	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 50 is the ligand for E3 ligase Cereblon. E3 ligase Ligand 50 can be used for synthesis of PROTAC BTK Degrader-10 (HY-160966) .

HY-122562

MT-802 3 Publications Verification	PROTACs Btk	Cancer
MT-802 is a *BTK* PROTAC degrader. MT-802 degrades wild-type *BTK* (DC₅₀ = 14.6 nM) and *BTK* mutants including E41K, C481S (DC₅₀ = 14.9 nM), C481R, C481Y, C481T, C481F, L528W, and inhibits their Y223 phosphorylation. BI-4732 can be used for the study of Ibrutinib (HY-10997)-resistant chronic lymphocytic leukemia (CLL). (Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-141371), E3 ligase ligand-linker conjugate (HY-176340)) .

HY-156743

DCAF1 binder 2	Ligands for E3 Ligase Btk Epigenetic Reader Domain	Others
DCAF1 binder 2, a ligands for E3 Ligase, involves in BRD9, kinase and selective BTK degration.

HY-142621

BCPyr	PROTACs Btk	Cancer
BCPyr is a PROTAC-class *BTK* degrader (DC₅₀ = 800 nM) . BCPyr consists of a PROTAC target protein ligand (red part) BTK ligand 11 (HY-168314), an E3 ubiquitin ligase ligand (blue part) E3 ligase Ligand 20 (HY-135997), and a PROTAC linker (black part) (5-(Bromomethyl)pyrazin-2-yl)methanol (HY-168315). E3 ubiquitin ligase+linker can form E3 Ligase Ligand-linker Conjugate 146 (HY-168316).

HY-153321

Bexobrutideg 1 Publications Verification NX-5948; BTK-IN-24	PROTACs Btk	Inflammation/Immunology Cancer
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific *BTK* protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .

HY-154860

PTD10	PROTACs Btk	Cancer
PTD10 is a highly potent PROTAC *BTK* degrader (DC₅₀: 0.5 nM, K_D: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC₅₀s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation. (Pink: Btk ligand (HY-19834); Blue: E3 ligase ligand (HY-14658); Black: linker (HY-Y0966); E3 ligase ligand + linker (HY-131717)) .

HY-133137A

SJF620 hydrochloride	PROTACs Btk	Cancer
SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and *Btk* with a DC₅₀ of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .

HY-136269A

A 410099.1, amine-Boc	E3 Ligase Ligand-Linker Conjugates	Cancer
A 410099.1, amine-Bocis a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5) .

HY-136269

A 410099.1, amine-Boc hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
A 410099.1, amine-Boc hydrochloride is a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5) .

HY-133137

SJF620	PROTACs Btk	Cancer
SJF620 is a PROTAC connected by ligands for Cereblon and *Btk* with a DC₅₀ of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .

HY-155072

PROTAC BTK Degrader-5	PROTACs Btk	Cancer
PROTAC BTK degraders-5(compound 3e) is a selective *BTK* PROTAC degrader with a DC₅₀ value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297；Pink:BKT inhibitor (HY-150898)) ¹.

HY-133144

Lenalidomide-OH	Ligands for E3 Ligase	Cancer
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137) .

HY-168964

Ethanolamine-Thalidomide-4-OH	E1/E2/E3 Enzyme E3 Ligase Ligand-Linker Conjugates	Cancer
Ethanolamine-Thalidomide-4-OH is an *E3 Ligase Ligand-Linker Conjugate* composed of an CRBN ligand (HY-103596) and a linker (HY-Y0524), and can be used for synthesis of PROTACs (eg: PROTAC BTK Degrader-13 (HY-168963)) .

HY-153357

NRX-0492	PROTACs Btk	Cancer
NRX-0492 is an orally active PROTAC-class *BTK* degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC₅₀ ≤ 0.2 nM, DC₉₀ ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 has antitumor effects against chronic lymphocytic leukemia.NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263).

HY-122830

DD-03-171	PROTACs Btk NF-κB	Cardiovascular Disease Cancer
DD-03-171 is a PROTAC *BTK* degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC₅₀ = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading *BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK* ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717)) .

HY-W591307

P131	PROTAC Linkers	Cancer
P131 is a PROTAC molecule comprised of Pomalidomide-based cereblon ligand and IBT6A, linked by a PEG 3 chain. P131 can degrade both wild-type and C481S mutant BTK with nanomolar potencies.

HY-153220A

(R)-NX-2127	PROTACs Btk	Inflammation/Immunology Cancer
(R)-NX-2127 ((R)-Compound 28) is an isomer of the BTK PROTAC degrader NX-2127 (HY-153220) . (Pink: BTK ligand 10 (HY-168302); Black: (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303); Blue: Thalidomide 5-fluoride (HY-W087383).

HY-168298

Lenalidomide-6-F-piperidine-C2-Pip-C-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
Lenalidomide-6-F-piperidine-C2-Pip-C-COOH is a linker and E3 ligase ligand for PROTAC BTK Degrader-5 (HY-155072) and can be used in malignant lymphoma research .

HY-153220

NX-2127	PROTACs Btk	Cancer
NX-2127 (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK ^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)

HY-153803

GBD-9	PROTACs Molecular Glues Btk	Cancer
GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets *BTK* and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) . GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).

HY-163962

L18I	PROTACs Btk	Inflammation/Immunology
L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964) ^{[1] ^.}

HY-P1181

Pam2CSK4	Toll-like Receptor (TLR)	Inflammation/Immunology
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages .

HY-P1181A

Pam2CSK4 TFA	Toll-like Receptor (TLR)	Inflammation/Immunology
Pam2CSK4 (TFA), a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 (TFA) promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 (TFA) also activates iNOS expression and NO production in mouse macrophages .

Cat. No.	Product Name

HY-L129

Target Protein Ligand Library

64 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 64 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

HY-L156

Autoimmune Disease Compound Library

742 compounds

Autoimmune disease is a pathological disease characterized by inflammatory disorders targeting autoantigens. The routine treatment of autoimmune diseases suppresses general immune function to regulate uncontrolled inflammation. The current targeted immunotherapy suppresses the main pro-inflammatory signaling pathways by blocking inflammatory cytokines, cell surface molecules, and intracellular kinases. As key participants in innate immunity, macrophages and dendritic cells (DCs) are crucial for Ag presentation and pro-inflammatory cytokine production, such as TNF and IL-1 β、 IL-6, IL-23, B cell activating factor (BAFF), and the proliferation-inducing ligand (APRIL, also known as TNFSF13A).

MCE designs a unique collection of 742 autoimmune disease-related compounds, covering multiple targets and subtypes, such as TNF Receptor, IFNAR, JAK, Btk, TLR, IL-6, IL-17, IL-23, etc. It is a useful tool for screening autoimmune disease drugs.

Cat. No.	Product Name	Target	Research Area

HY-P1181A

Pam2CSK4 TFA	Toll-like Receptor (TLR)	Inflammation/Immunology
Pam2CSK4 (TFA), a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 (TFA) promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 (TFA) also activates iNOS expression and NO production in mouse macrophages .

HY-P1181

Pam2CSK4	Toll-like Receptor (TLR)	Inflammation/Immunology
Pam2CSK4, a lipopeptide, is a TLR6-independent TLR2 ligand and agonist. Pam2CSK4 promotes platelet aggregation, and increases platelet adhesion to collagen-coated surfaces in a TLR2/NF-κB/BTK-dependent manner. Pam2CSK4 also activates iNOS expression and NO production in mouse macrophages .

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