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Pathways Recommended:	PROTAC

Results for "

PROTAC BTK degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (21) Ligands for Target Protein for PROTAC (2) PROTAC Linkers (4) PROTAC-Linker Conjugates for PAC (1) CDK (1) E3 Ligase Ligand-Linker Conjugates (2) Ligands for E3 Ligase (1) Molecular Glues (1) Nuclear Factor of activated T Cells (NFAT) (1) PROTACs (19) RANKL/RANK (1)
By Research Areas:	Cancer (28) Inflammation/Immunology (3)
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-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-157763

PROTAC BTK Degrader-8	PROTAC-Linker Conjugates for PAC Btk	Cancer
PROTAC BTK Degrader-8 (compound 3) is an effective PROTAC BTK degrader that can be coupled to an ADC antibody to form a PAC.

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 .

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-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-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-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-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-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-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-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-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-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-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-168297

Piperidine-C2-Pip-C-COOH	PROTAC Linkers	Cancer
Piperidine-C2-Pip-C-COOH is a linker for *PROTAC* BTK Degrader-5 (HY-155072), significantly improving metabolic stability, and can be used in cancer research .

HY-122830

DD-03-171	PROTACs Btk	Cancer
DD-03-171 is a *BTK* PROTAC degrader, the *BTK* IC₅₀ a value of 5.1 nM. DD-03-171 has an antiproliferative effect on mantle cell lymphoma (MCL) cells . (Pink: BTK inhibitor (HY-168292); Black: linker (HY-28875); Blue: CRBN Ligand (HY-131717))

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-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-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-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-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-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) . (R)-NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).

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-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-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 can bind non-covalently to the BTK binding domain and cereblon, which is an adapter protein in the E3 ubiquitin ligase complex . 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). E3 ubiquitin ligase and linker can form Thalidomide 5-pyrrolidine-CHO (HY-49372A); the active control for the target protein ligand is BTK ligand 12 (HY-49421).

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) .

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 . NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).

Cat. No.	Product Name

HY-L129

Target Protein Ligand Library	37 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 37 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.

Target Protein Ligand Library

37 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 37 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.

Cat. No.	Product Name		Classification

HY-130504

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.

HY-130481

Propargyl-PEG4-acid		Alkynes PROTAC Synthesis
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.

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