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Pathways Recommended:	PROTAC

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PROTAC Linker 1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Linker (1) E3 Ligase Ligand-Linker Conjugates (1) PROTAC Linkers (5) PROTAC-Linker Conjugates for PAC (2) ADC Cytotoxin (1) Adrenergic Receptor (1) Androgen Receptor (1) Apoptosis (5) Autophagy (4) Bcl-2 Family (2) Btk (1) CDK (1) Epigenetic Reader Domain (1) FAK (1) FKBP (1) GLP Receptor (1) Histone Acetyltransferase (2) Ligands for E3 Ligase (5) NAMPT (1) PROTACs (19) Ras (1) ROS Kinase (1) STING (2)
By Research Areas:	Cancer (30) Infection (1) Inflammation/Immunology (3)
Click Chemistry:	ADC Synthesis (1) DBCO (1) PROTAC Synthesis (2) Azide (2) Alkynes (1)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: PROTAC-Linker Conjugates for PAC PROTAC Linkers Ligands for Target Protein for PROTAC ADC Linker Target Protein Ligand-Linker Conjugates Drug-Linker Conjugates for ADC E3 Ligase Ligand-Linker Conjugates

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-108371

Boc-C1-PEG2-C4-Cl PROTAC Linker 1	PROTAC Linkers	Cancer
Boc-C1-PEG2-C4-Cl (PROTAC Linker 1) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs .

HY-129938

PROTAC BRD4 Degrader-24	PROTAC-Linker Conjugates for PAC	Cancer
PROTAC BRD4 Degrader-24 (compound 5), a PROTAC-linker Conjugate for PAC, comprises the chimeric BET degrader GNE-987 and disulfide-containing linker .

HY-101838

dBET1 Maximum Cited Publications 13 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker .

HY-W259932

Lenalidomide 5'-piperazine	Ligands for E3 Ligase	Cancer
Lenalidomide 5'-piperazine is a functionalized cerebellar ligand for PROTAC development that binds an E3 ligand to terminal piperazine for subsequent chemical reactions to produce a protein deactivator with a rigid linker .

HY-103634

dFKBP-1 1 Publications Verification	PROTACs FKBP	Cancer
dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker .

HY-111546

BI-3663	PROTACs FAK	Cancer
BI-3663 is a highly selective PTK2/FAK PROTAC (DC₅₀=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC₅₀ of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .

HY-162608

PROTAC JAK1 degrader 1	PROTACs	Cancer
PROTAC JAK1 degrader 1 degrader 1 (compound 10c) is an effective and selective PROTAC JAK1 degrader with a DC₅₀ of 214 nM. PROTAC JAK1 degrader 1 has antitumor activity. (Structure Note: PINK, JAK1 ligand 1 (HY-10961); Blue, VHL ligand Thalidomide (HY-14658); Black, linker) .

HY-163440

PROTAC NAMPT Degrader-1	PROTACs NAMPT	Cancer
PROTAC NAMPT Degrader-1 is a potent PROTAC targeting NAMPT with aDC₅₀ value of 217 nM. PROTAC NAMPT Degrader-1 has anti-proliferative activity with an IC₅₀ value of 0.12μM against A2780 cells. (Srtucture Note: PINK, NAMPT activator (HY-163445); Blue, VHL ligand (HY-163440); Black, linker) .

HY-147052

Boc-Pip-butyn	PROTAC Linkers	Cancer
Boc-Pip-butyn is an Alkyl/ether-based **PROTAC linker** . Boc-Pip-butyn is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-158383

Pomalidomide-CO-C3-PEG4-C6-NH2	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide-CO-C3-PEG4-C6-NH2 is an *E3 ligase ligand-linker* conjugate** part of PROTAC PIPIB degrader 1 (HY-158381). Pomalidomide consists of the E3 ligase ligand Pomalidomide (HY-10984) and a linker .

HY-130435

DBCO-PEG4-amine	ADC Linker PROTAC Linkers	Cancer
DBCO-PEG4-amine is a PEG-based **PROTAC linker** can be used in the synthesis of PROTACs. DBCO-PEG4-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-amine can be used in the synthesis of FPM-PEG4-DBCO (a homobifunctional azide-to-azide cross-linker) . DBCO-PEG4-amine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

HY-161177

PROTAC KRAS G12D degrader 2	PROTACs Ras	Infection
PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker .

HY-162412

PROTAC AR/AR-V7 degrader-1	PROTACs Adrenergic Receptor Apoptosis	Cancer
PROTAC AR/AR-V7 degrader-1 (27c) is a *PROTAC*-based and dual AR, AR-V7 degrader, with DC₅₀ values of 2.67 and 2.64 μM for AR and AR-V7, respectively. PROTAC AR/AR-V7 degrader-1 (27c) induces apoptosis (Red: AR antagonist; Blue: E3 ligase ligand; Black: linker) .

HY-W190796A

Mal-PEG3-NH2 TFA	PROTAC Linkers	Cancer
Mal-PEG3-NH2 TFA is a linear heterobifunctional PEG crosslinker with Maleimide (HY-W007324) and amine. Mal-PEG3-NH2 TFA is a non-degradable (non-cleavable) PROTAC linker .

HY-133736

PROTAC BRD4 Degrader-5-CO-PEG3-N3	PROTAC-Linker Conjugates for PAC ADC Cytotoxin	Cancer
PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-158048

UNC9036	PROTACs STING	Inflammation/Immunology
UNC9036 is a *PROTAC*-based STING degrader, with a DC₅₀ of 227 nM. UNC9036-mediated STING degradation is proteasome and VHL dependent (Srtucture Note: Red, STING agonist diABZI (HY-112921A); Blue, VHL ligand VH032 (HY-120217); Black, linker) .

HY-158036

PROTAC STING Degrader-2	PROTACs STING	Others Inflammation/Immunology
PROTAC STING degrader-2 is a protein Degrader that targets Stimulator of interferon genes (STING) (DC₅₀=0.53 μM). PROTAC STING Degrader-2 is combined with STING protein and E3 ubiquitin ligase in a covalent manner to induce the degradation of STING protein. PROTAC STING Degrader-2 can be used to investigate the role of STING in autoinflammation and autoimmune diseases (PINK: STING binder (HY-145009); Blue: VHL ligand (HY-164043); Black: linker) .

HY-163229

(1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc	Ligands for E3 Ligase Autophagy	Cancer
(1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-161615

PROTAC ATR degrader-2	Apoptosis PROTACs	Cancer
PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC₅₀ of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)

HY-162791

(1s,4s)-C1-Piperidine-C1-cyclohexane-C1	PROTAC Linkers	Cancer
(1s,4s)-C1-Piperidine-C1-cyclohexane-C1 is a PROTAC linker. (1s,4s)-C1-Piperidine-C1-cyclohexane-C1 can be used to synthesize (HY-162741) .

HY-163230

(1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc	Ligands for E3 Ligase Autophagy	Cancer
(1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-162362

MS8709	PROTACs GLP Receptor	Cancer
MS8709 (10), a potential anticancer therapeutic, is a first-in-class G9a/GLP *PROTAC* degrader. MS8709 (10) is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .

HY-162702

AZ'3137	Androgen Receptor PROTACs	Cancer
AZ‘3137 (Compound 22) is an orally active *PROTAC*-type androgen receptor (AR) degrader, with a DC₅₀ value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI₅₀ value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .

HY-130604

DT2216 1 Publications Verification	Bcl-2 Family PROTACs Apoptosis	Cancer
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on *PROTAC* technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .

HY-163814

CDK2 degrader 1	CDK	Cancer
CDK2 degrader 1 (Compound 3) is an orally active cyclin-dependent kinase 2 (CDK2) degrader based on PROTAC technology. CDK2 degrader 1 binds to cereblon to induce ubiquitination and subsequent proteasomal degradation of the CDK2. CDK2 degrader 1 is used in the research of a wide range of cancers (Red: spiro[3.3]heptan-2- ylmethyl carbonochloridate; Blue: N,N-diisopropylethylamine; Black: linker) .

HY-158113

CBPD-409	Histone Acetyltransferase PROTACs	Cancer
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC₅₀ of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC₅₀s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .

HY-163226

(1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc	Ligands for E3 Ligase Autophagy	Cancer
(1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-163227

(1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc	Ligands for E3 Ligase Autophagy	Cancer
(1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

HY-162704

JMV7048	PROTACs	Cancer
JMV7048 is an effective *PROTAC* degrader targeting PXR (Pregnane X Receptor) with a DC₅₀ of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .

HY-161369

CBPD-268	PROTACs Histone Acetyltransferase	Cancer
CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC₅₀ value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .

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-161410

WH244	PROTACs Apoptosis Bcl-2 Family	Cancer
WH244 is a second generation BCL-2 and BCL-xL dual depressant (PROTAC). The primary activity of WH244 is the specific degradation of BCL-2 and BCL-xL proteins (BCL-xL: DC₅₀=0.6 nM, BCL-2: DC₅₀=7.4 nM). WH244 promotes their ubiquitination and subsequent proteasome degradation by targeting these proteins, thereby restoring the cell's apoptosis pathway. WH244 has good antitumor activity. (Pink: BCL-2/BCL-xL ligand (HY-161415); Blue: E3 ligase ligand (HY-112078); Black: linker) .

HY-159147

SIAIS039	PROTACs ROS Kinase Apoptosis	Cancer
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific *PROTAC* with DC₅₀s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .

Cat. No.	Product Name		Classification

HY-133736

PROTAC BRD4 Degrader-5-CO-PEG3-N3		Azide
PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) is a PROTAC-linker Conjugate for PAC, comprises the BRD4 degrader GNE-987 and PEG-based linker . PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-147052

Boc-Pip-butyn		Alkynes PROTAC Synthesis
Boc-Pip-butyn is an Alkyl/ether-based **PROTAC linker** . Boc-Pip-butyn is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-130435

DBCO-PEG4-amine		PROTAC Synthesis ADC Synthesis DBCO
DBCO-PEG4-amine is a PEG-based **PROTAC linker** can be used in the synthesis of PROTACs. DBCO-PEG4-amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). DBCO-PEG4-amine can be used in the synthesis of FPM-PEG4-DBCO (a homobifunctional azide-to-azide cross-linker) . DBCO-PEG4-amine is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.

HY-159147

SIAIS039		Azide
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific *PROTAC* with DC₅₀s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .

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