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Pathways Recommended:	PROTAC

Results for "

BTK PROTAC

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Btk (29) Ligands for Target Protein for PROTAC (9) PROTAC Linkers (6) PROTAC-Linker Conjugates for PAC (1) CDK (1) E1/E2/E3 Enzyme (1) E3 Ligase Ligand-Linker Conjugates (5) Itk (1) Ligands for E3 Ligase (3) Molecular Glues (1) Nuclear Factor of activated T Cells (NFAT) (1) p38 MAPK (1) PROTACs (24) RANKL/RANK (1)
By Research Areas:	Cancer (42) Inflammation/Immunology (5)
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-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-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-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 .

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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 and can be used for synthesis of PROTACs (eg: PROTAC BTK Degrader-13 (HY-168963)) .

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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).

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-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-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] ^.}

Cat. No.	Product Name

HY-L129

Target Protein Ligand Library

56 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 56 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-130481

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.

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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