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PROTAC-based

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PROTAC Linkers (1) Adrenergic Receptor (1) Akt (3) Anaplastic lymphoma kinase (ALK) (3) Apoptosis (6) Autophagy (2) Bcl-2 Family (2) c-Met/HGFR (1) Casein Kinase (1) CDK (1) EGFR (2) Ephrin Receptor (2) Epigenetic Reader Domain (6) Ferroptosis (1) FKBP (3) Glutathione Peroxidase (1) HDAC (2) Hedgehog (1) IRAK (1) Ligands for E3 Ligase (10) MAP4K (2) MDM-2/p53 (1) Molecular Glues (1) p38 MAPK (2) PD-1/PD-L1 (1) PDGFR (1) PROTACs (37) RIP kinase (1) STAT (1) STING (1) VEGFR (2)
By Research Areas:	Cancer (47) Inflammation/Immunology (5) Metabolic Disease (1)
Click Chemistry:	PROTAC Synthesis (1) Alkynes (1)

Inhibitors & Agonists

Click Chemistry

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-130714

TD-165	PROTACs	Cancer
TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group .

HY-129610

KB02-SLF	PROTACs FKBP	Cancer
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF .

HY-155398

PRO-HD3

PROTACs HDAC Cancer

PRO-HD3 is a cell-specific, PROTAC-based HDAC6 degrader .
HY-155397

PRO-HD2

PROTACs HDAC Cancer

PRO-HD2 is a cell-specific, PROTAC-based HDAC6 degrader .
HY-143882

MS5033

PROTACs Akt Cancer

MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC₅₀ of 430 nM in PC3 cells .

PRO-HD3	PROTACs HDAC	Cancer
PRO-HD3 is a cell-specific, PROTAC-based HDAC6 degrader .

PRO-HD2	PROTACs HDAC	Cancer
PRO-HD2 is a cell-specific, PROTAC-based HDAC6 degrader .

MS5033	PROTACs Akt	Cancer
MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC₅₀ of 430 nM in PC3 cells .

HY-115568

BETd-246 1 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
BETd-246 is a second-generation and *PROTAC*-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity .

HY-163152

PROTAC BRM degrader-1	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRM degrader-1 (compound 17) is a *PROTAC*-based BRM and BRG1 degrader, with DC₅₀ values of 93 pM and 4.9 nM, respectively .

HY-149236

PROTAC GPX4 degrader-1

PROTACs Glutathione Peroxidase Ferroptosis Cancer

PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC₅₀ of 0.03 μM in HT1080 cells .
HY-155393

PROTAC BRD4 Degrader-22

PROTACs Epigenetic Reader Domain Cancer

PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC₅₀ (MOLT4, 24 h) of 9.2 .
HY-129180

XY028-133

PROTACs CDK Cancer

XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK .

PROTAC GPX4 degrader-1	PROTACs Glutathione Peroxidase Ferroptosis	Cancer
PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC₅₀ of 0.03 μM in HT1080 cells .

PROTAC BRD4 Degrader-22	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-22 (Compd 44h) is a PROTAC-based BRD4 degrader, with a pDC₅₀ (MOLT4, 24 h) of 9.2 .

XY028-133	PROTACs CDK	Cancer
XY028-133 (example 14) is a *PROTAC*-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK .

HY-139707

Thalidomide-NH-CBP/p300 ligand 2	PROTACs Molecular Glues Epigenetic Reader Domain	Cancer
Thalidomide-NH-CBP/p300 ligand 2 (P-007) is a *PROTAC*-based CBP and p300 degrader (extracted from patent WO2020173440) .

HY-146231

SS47	PROTACs MAP4K	Inflammation/Immunology Cancer
SS47, a *PROTAC*-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the antitumor efficacy .

HY-103634

dFKBP-1	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-162450

Antitumor agent-150	PROTACs MDM-2/p53 Apoptosis	Cancer
Antitumor agent-150 (V10), an anti-breast cancer agent, is a *PROTAC*-based MDM2 protein degrader (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand) .

HY-161157

dTAG-13-NEG	PROTACs	Cancer
dTAG-13-NEG is a negative control of dTAG-13. dTAG-13 (HY-114421), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 ^F36V with expression of FKBP12F36V in-frame with a protein of interest .

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-147219

SIAIS164018	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 is a *PROTAC*-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .

HY-147219A

SIAIS164018 hydrochloride	PROTACs Anaplastic lymphoma kinase (ALK) EGFR Apoptosis	Cancer
SIAIS164018 hydrochloride is a *PROTAC*-based ALK and EGFR degrader, with IC₅₀ value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .

HY-133120

INY-03-041	PROTACs Akt	Cancer
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-133120A

INY-03-041 trihydrochloride	PROTACs Akt	Cancer
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC₅₀s of 2.0, 6.8 and 3.5 nM, respectively .

HY-114421

*FKBP12 PROTAC* dTAG-13** 1 Publications Verification dTAG-13	PROTACs FKBP	Cancer
FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 ^F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 ^F36V and CRBN, thereby selectively degrading FKBP12 ^F36V .

HY-135382

PROTAC IRAK4 degrader-2	PROTACs IRAK	Inflammation/Immunology Cancer
PROTAC IRAK4 degrader-2 (Compound 9) is a PROTAC-based IRAK4 degrader that affords potent IRAK4 degradation with a DC₅₀ in peripheral blood mononuclear cells (PBMCs) cells of 151 nM. PROTAC IRAK4 degrader-2 induce a reduction of IRAK4 protein levels with a DC₅₀ of 36 nM in PBMC cells. PROTAC IRAK4 degrader-2 also leads to the inhibition of multiple cytokines in PBMCs .

HY-150251

STAT3 degrader-2	STAT PROTACs	Cancer
STAT3 degrader-2 is a PROTAC-based degrader of STAT3. STAT3 degrader-2 can degrade the level of total STAT3 protein. STAT3 degrader-2 can be used for the research of cancer and other diseases . STAT3 degrader-2 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-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-146231A

SS47 TFA	MAP4K PROTACs	Inflammation/Immunology Cancer
SS47 TFA, a *PROTAC*-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies . SS47 (TFA) 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-129917

KB02-JQ1 2 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1 .

HY-130985

9-Decyn-1-ol	PROTAC Linkers	Cancer
9-Decyn-1-ol is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs. 9-Decyn-1-ol can be used to conjugate GDC-0068 with Lenalidomide to generate INY-03-041. INY-03-041 is a potent, highly selective and PROTAC-based pan-Akt degrader. INY-03-041 inhibits Akt1, Akt2 and Akt3 with IC₅₀s of 2.0 nM, 6.8 nM and 3.5 nM, respectively . 9-Decyn-1-ol 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-157334

DEG-77	Casein Kinase	Cancer
DEG-77, a PROTAC based IKZF2 and CK1α degrader, possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t_1/2=8h) .

HY-156814

HPP-9	Hedgehog	Cancer
HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC₅₀ of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity ^[1[.

HY-114405

SJFδ	PROTACs p38 MAPK Autophagy	Cancer
SJFδ is a 10-atom linker *PROTAC* based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC₅₀ of 46.17 nM, but does not degrade p38α, p38β, or p38γ .

HY-155684

SA-PA	PROTACs VEGFR PDGFR Ephrin Receptor	Cancer
SA-PA is an intracellular self-assembled *PROTAC* based on azide and alkyne. SA-PA is able to selectively degrade VEGFR-2, PDGFR-β and EphB4 proteins in U87 cells. SA-PA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues .

HY-155685

SA-VA	PROTACs VEGFR Ephrin Receptor Apoptosis	Cancer
SA-VA is an intracellular self-assembled *PROTAC* based on azide and alkyne. SA-VA is able to selectively degrade VEGFR-2 and EphB4 proteins in U87 cells. SA-VA can be converted to PROTAC in situ by click reaction with the help of endogenous copper in tumor tissues. SA-VA promotes apoptosis and blocks cells in S phase .

HY-114404

SJFα	PROTACs p38 MAPK Autophagy	Cancer
SJFα is a 13-atom linker *PROTAC* based on von Hippel-Lindau ligand. SJFα degrades p38α with a DC₅₀ of 7.16 nM, but is far less effective at degrading p38δ (DC₅₀=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM .

HY-125877

PROTAC Mcl1 degrader-1	PROTACs Bcl-2 Family	Cancer
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM .

HY-146022

SIAIS117	PROTACs Anaplastic lymphoma kinase (ALK)	Cancer
SIAIS117 is a potent *Brigatinib-PROTAC* degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer .

HY-W584527

VH032 analogue-1	Ligands for E3 Ligase	Cancer
VH032 analogue-1 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-1 will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032 analogue-1 is a key intermediate in the synthesis of PROTACs based on VHL ligands.

HY-W584528

VH032 analogue-2	Ligands for E3 Ligase	Cancer
VH032 analogue-2 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-2 will remove the protective group under acidic conditions, and can be directly used for the synthesis of PROTAC molecules. VH032 analogue-2 is a key intermediate for the synthesis of PROTACs based on VHL ligands.

HY-100972

ARV-771 Maximum Cited Publications 21 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with K_ds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively .

HY-111866

PROTAC RIPK degrader-2	PROTACs RIP kinase	Metabolic Disease Cancer
PROTAC RIPK degraders -2 is a non-peptide *PROTAC* based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .

HY-W584525

VH032-NH-CO-CH2-NHBoc	Ligands for E3 Ligase	Cancer
VH032-NH-CO-CH2-NHBoc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-NH-CO-CH2-NHBoc will remove the Boc protection under acidic conditions, and connect with the target protein ligand through a linker to form a PROTAC molecule, which is a key intermediate for the synthesis of PROTAC based on VHL ligand.

HY-W584534

VH032-CH2-Boc	Ligands for E3 Ligase	Cancer
VH032-CH2-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-CH2-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-CH2-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.

HY-W584535

VH032-C3-Boc	Ligands for E3 Ligase	Cancer
VH032-C3-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C3-Boc will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032-C3-Boc is a key intermediate for the synthesis of PROTACs based on VHL ligands.

HY-W584529

VH032-C2-NH-Boc	Ligands for E3 Ligase	Cancer
VH032-C2-NH-Boc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C2-NH-Boc will remove the protecting group under acidic conditions, and can be directly used for the synthesis of PROTAC molecules. VH032-C2-NH-Boc is a key intermediate for the synthesis of PROTACs based on VHL ligands.

HY-W584530

VH032-C4-NH-Boc	Ligands for E3 Ligase	Cancer
VH032-C4-NH-Boc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-C4-NH-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-C4-NH-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.

HY-W584531

VH032-C6-NH-Boc	Ligands for E3 Ligase	Cancer
VH032-C6-NH-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-C6-NH-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-C6-NH-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.

HY-W584533

VH032-PEG2-NH-BOC	Ligands for E3 Ligase	Cancer
VH032-PEG2-NH-BOC is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-PEG2-NH-BOC will remove the protecting group under acidic conditions and be directly used for PROTAC molecule synthesis. VH032-PEG2-NH-BOC is a key intermediate in the synthesis of PROTAC based on VHL ligand.

HY-160506

PRO-6E	PROTACs c-Met/HGFR Apoptosis
PRO-6E is an oral active *PROTAC* based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .

HY-W584532

VH032-O-C2-NH-Boc	Ligands for E3 Ligase	Cancer
VH032-O-C2-NH-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-O-C2-NH-Boc will remove the protecting group under acidic conditions and can be directly used in PROTAC molecule synthesis. VH032-O-C2-NH-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.

HY-125876

PROTAC Bcl2 degrader-1	PROTACs Bcl-2 Family	Cancer
PROTAC Bcl2 degrader-1 (Compound C5) is a *PROTAC* based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC₅₀, 4.94 μM; DC₅₀, 3.0 μM) and Mcl-1 (IC₅₀, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).

HY-131183

PROTAC PD-1/PD-L1 degrader-1	PROTACs PD-1/PD-L1	Inflammation/Immunology
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC₅₀ of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .

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