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Results for "

BTK degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (42) ADC Payload (1) Akt (1) Apoptosis (2) Bcl-2 Family (1) ByeTAC (1) Caspase (1) CDK (1) Drug Intermediate (1) Drug Isomer (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (4) ERK (1) IKZF Family (2) Itk (1) Ligands for E3 Ligase (4) Ligands for Target Protein for PROTAC (6) MEK (1) Molecular Glues (1) NF-κB (3) Nuclear Factor of activated T Cells (NFAT) (1) p38 MAPK (1) PIKfyve (1) PROTAC Linkers (7) PROTAC-Linker Conjugates for PAC (1) PROTACs (34) RANKL/RANK (1) Src (1) Syk (1)
By Research Areas:	Cancer (55) Cardiovascular Disease (1) Inflammation/Immunology (10)
Click Chemistry:	PROTAC Synthesis (2) Alkynes (1)

Inhibitors & Agonists

Bibliotecas de Screening

Click Chemistry

Targets Recommended: Btk

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

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-153220

Zelebrudomide NX-2127	PROTACs Btk	Inflammation/Immunology Cancer
Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTK ^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide 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-160141

Catadegbrutinib BGB-16673; BTK-IN-29	PROTACs Btk NF-κB	Inflammation/Immunology Cancer
BGB-16673 (BGB-16673) is an orally active, selective *BTK* PROTAC degrader (IC₅₀=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma .

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-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-122562

MT-802 4 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-157763

*Mal-PEG1-Val-Cit-PABC-diphosphate-BTK* degrader-1**	PROTAC-Linker Conjugates for PAC Btk	Cancer
Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 is a cleavable linker-payload conjugate and cereblon-binding *BTK* bifunctional degrader. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 induces *BTK* degradation and exerts cytotoxic effects when delivered via CD79b monoclonal antibody. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1, when formulated as a CD79b antibody-drug conjugate, achieves sustained in vivo *BTK* degradation in tumor-bearing mice with reduced systemic payload exposure. Mal-PEG1-Val-Cit-PABC-diphosphate-BTK degrader-1 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ADC linker: (HY-130944); PROTAC: (HY-163295)) .

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-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-160142

UBX-382	PROTACs Btk Syk MEK ERK	Cancer
UBX-382 is an orally active *BTK* PROTAC degrader with a DC₅₀ of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant *BTK* proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant *BTK*-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .

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-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-163295

BTK degrader-1	ADC Payload Btk	Cancer
BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect .

HY-154860

PTD10	PROTACs Btk Apoptosis Caspase Bcl-2 Family NF-κB Akt	Inflammation/Immunology Cancer
PTD10 is a selective and potent *BTK* PROTAC degrader (DC₅₀ = 0.5 nM, K_D = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease .

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-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-153119

TMX-4153	PROTACs PIKfyve	Inflammation/Immunology
TMX-4153 is a selective PIP4K2C PROTAC degrader. TMX-4153 induces PIP4K2C degradation in MOLT4 cells (DC₅₀ = 24 nM) and HAP1 cells (DC₅₀ = 361 nM). TMX-4153 can be used for the study of biological functions of PIP4K2C (immune modulation)-related diseases. (Pink: BTK ligand (HY-177432), Blue: VHL Ligand (HY-112078), Black: Linker) .

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-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-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-153220A

(R)-Zelebrudomide (R)-NX-2127	PROTACs Btk	Inflammation/Immunology Cancer
(R)-Zelebrudomide ((R)-NX-2127) ((R)-Compound 28) is an isomer of the BTK PROTAC degrader Zelebrudomide (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-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-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-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: CRBN ligand ( HY-W245311)) .

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-133143

1,2-Bis(2-iodoethoxy)ethane 1 Publications Verification	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-179562

BTK degrader-2	Btk	Cancer
BTK degrader-2 (Example 2) is a *BTK* dual-functional degrading agent, which causes the degradation of BTK through the ubiquitin-proteasome pathway. BTK degrader-2 can be used for the study of B-cell-related diseases .

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-176526

BTK degrader-1 intermediate	Drug Intermediate Btk	Cancer
BTK degrader-1 intermediate (compound 5) is an intermediate for the synthesis of BTK degrader-1 (HY-163295). BTK degrader-1 can be used as an ADC toxin to synthesize antibody-drug conjugate (ADC) .

HY-W245311

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

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-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-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-176381

BTK ligand 11-alcohol-PEG6-azido	E3 Ligase Ligand-Linker Conjugates	Cancer
BTK ligand 11-alcohol-PEG6-azido is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as TDP-43 degrader-1 (HY-122828) .

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-179077

*PROTAC BTK/IKZF1/3 Degrader-1*	PROTACs Btk IKZF Family	Cancer
PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma . (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))

HY-179076

BTK/IKZF1/3 ligand 1	Ligands for Target Protein for PROTAC Btk IKZF Family	Cancer
BTK/IKZF1/3 ligand 1 is a BTK/IKZF1/3 PROTAC ligand. BTK/IKZF1/3 ligand 1 can be conjugated with E3 ligase Ligand (HY-41547) and linker to synthesize PROTAC BTK/IKZF1/3 Degrader-1 (HY-179077). PROTAC BTK/IKZF1/3 Degrader-1 can be used for cancer research .

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-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-W209253

1-(Piperidin-4-ylmethyl)piperidine	PROTAC Linkers	Others
1-(Piperidin-4-ylmethyl)piperidine is a PROTAC linker that can be used for synthesis of PROTACs, such as PROTAC BTK Degrader-9 (HY-162280) .

HY-153321A

(R,R)-Bexobrutideg (R,R)-NX-5948; (R,R)-BTK-IN-24	Drug Isomer PROTACs Btk	Inflammation/Immunology Cancer
(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific *BTK* protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .

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-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-181623

*PROTAC BTK* degrader-14**	PROTACs Btk	Cancer
PROTAC BTK degrader-14 (compound 112) is a PROTAC protein degrader targeting BTK. PROTAC BTK degrader-14 can be used for the research of cancer .

HY-128408

*PROTAC BTK* Degrader-4**	PROTACs Btk	Inflammation/Immunology Cancer
PROTAC BTK Degrader-4 (compound 15) is a potent PROTAC Bruton's tyrosine kinases (BTK) degrader (DC₅₀ < 100 nM) with little immunomodulatory imide drug (IMiD) activity (DC₅₀ = 0.345 μM, D_max = 27.4%). PROTAC BTK Degrader-4 can be used for cancers, autoimmune diseases, and inflammatory diseases that are mediated by BTK .

HY-W392857

(S)-NH2-Pyridine-piperazine(Me)-Boc	PROTAC Linkers	Others
(S)-NH2-Pyridine-piperazine(Me)-Boc is a PROTAC Linker that can be used to synthesize PROTAC BTK Degrader-10 (HY-160966) .

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-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 .

Cat. No.	Nombre del producto

HY-L129

Target Protein Ligand Library

96 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 96 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.	Nombre del producto		Classification

HY-147943

*PROTAC BTK* Degrader-1**		PROTAC Synthesis
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-130504

Propargyl-PEG1-acid 1 Publications Verification		PROTAC Synthesis Alkynes
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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