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Pathways Recommended:	PROTAC

Results for "

BTK PROTAC

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (15) Ligands for Target Protein for PROTAC (3) PROTAC Linkers (3) CDK (1) E3 Ligase Ligand-Linker Conjugates (3) Ligands for E3 Ligase (1) Molecular Glues (1) Nuclear Factor of activated T Cells (NFAT) (1) PROTACs (12) RANKL/RANK (1)
By Research Areas:	Cancer (22) Inflammation/Immunology (2)
Click Chemistry:	PROTAC Synthesis (2) Alkynes (2)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

Targets Recommended: Btk PROTAC Linkers PROTAC-Linker Conjugates for PAC Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-157763

PROTAC BTK Degrader-8

PROTACs Btk Cancer

PROTAC BTK Degrader-8 (compound 3) is a potent PROTAC BTK degrader .

PROTAC BTK Degrader-8	PROTACs Btk	Cancer
PROTAC BTK Degrader-8 (compound 3) is a potent PROTAC BTK degrader .

HY-153536

PROTAC BTK Degrader-3	PROTACs Btk	Cancer
PROTAC BTK Degrader-3 is a potent *BTK* degrader with a DC₅₀ value of 10.9 nM of BTK degradation in Mino cells. PROTAC BTK Degrader-3 has the potential for B-cell malignancies, including chronic lymphoid malignancies research .

HY-122828

PROTAC BTK Degrader-2

PROTACs Btk Others

PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels .

PROTAC BTK Degrader-2	PROTACs Btk	Others
PROTAC BTK Degrader-2 is a potent **BTK PROTAC** degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels .

HY-147943

PROTAC BTK Degrader-1	PROTACs Btk	Cancer
PROTAC BTK Degrader-1 is a potent, selective and orally active **PROTAC BTK degrader with an IC₅₀** value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 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-162280

PROTAC BTK Degrader-9	PROTACs RANKL/RANK Nuclear Factor of activated T Cells (NFAT) Btk	Cancer
PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca ²⁺-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .

HY-155072

PROTAC BTK Degrader-5	Btk	Cancer
PROTAC BTK degraders-5(compound 3e) is a selective *BTK* 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 ¹.

HY-149391

PROTAC BTK Degrader-6	PROTACs Btk	Inflammation/Immunology
PROTAC BTK Degrader-6 (Compound 15) is a *PROTAC* *BTK* degrader (DC₅₀: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6) .

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 .

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-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-153803

GBD-9	PROTACs Molecular Glues Btk	Cancer
GBD-9 is a double-mechanism degrader that efficiently degrades *BTK* and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a *PROTAC* molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth .

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-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-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-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-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-130481

Propargyl-PEG4-acid	PROTAC Linkers	Cancer
Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC₅₀ of 200 nM in THP-1 cells . Propargyl-PEG4-acid 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-130504

Propargyl-PEG1-acid 1 Publications Verification	PROTAC Linkers	Cancer
Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM . Propargyl-PEG1-acid 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-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-160142

UBX-382	Btk	Cancer
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target *BTK* to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant *BTK* proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .

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-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 .

HY-153321

NX-5948 BTK-IN-24	Btk PROTACs	Inflammation/Immunology Cancer
NX-5948 (BTK-IN-24) 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. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a *PROTAC* composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .

HY-133143

1,2-Bis(2-iodoethoxy)ethane	PROTAC Linkers	Cancer
1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker. 1,2-Bis(2-iodoethoxy)ethane can be used in the synthesis of MT802 (HY-122562) and SJF620 (HY-133137). MT-802 and SJF620 are potent PROTAC BTK degraders with DC₅₀s of 1 nM and 7.9 nM, respectively .

HY-130665

TL12-186 1 Publications Verification	PROTACs CDK	Cancer
TL12-186 is a Cereblon-dependent multi-kinase *PROTAC* degrader. Multi-kinases include CDK, *BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A* (IC₅₀=73 nM) and CDK9/cyclin T1 (IC₅₀=55 nM) .

Target Protein Ligand Library	39 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 39 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.

Propargyl-PEG4-acid		PROTAC Synthesis Alkynes
Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC₅₀ of 200 nM in THP-1 cells . Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Propargyl-PEG1-acid 1 Publications Verification		Alkynes PROTAC Synthesis
Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM . Propargyl-PEG1-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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