Search Result
Results for "
PROTACs
" in MCE Product Catalog:
3540
Inhibitors & Agonists
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-153023
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PROTAC STAT3 degrader-2
|
PROTACs
STAT
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Cancer
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PROTAC STAT3 degrader-2 is a selective and efficacious PROTAC degrader of STAT3 protein with a DC50 of 3.54 μM in Molm-16 Cell. PROTAC STAT3 degrader-2 has the potential for cancer research.
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- HY-152145
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PROTAC SOS1 degrader-3
|
PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-3 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-3 effectively targeted SOS1 for degradation through the ubiquitin-proteasome system.
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- HY-144657
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PROTAC SOS1 degrader-2
|
PROTACs
Ras
|
Cancer
|
PROTAC SOS1 degrader-2 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-2 decreases the expression of pERK and RAS-GTP level in a dose-dependent manner. PROTAC SOS1 degrader-2 significantly inhibits the tumor growth in vivo.
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- HY-150608
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- HY-145737
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PROTAC SOS1 degrader-1
|
PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-1 is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM. PROTAC SOS1 degrader-1 shows antiproliferation activity in cancer cells with various KRAS mutations. PROTAC SOS1 degrader-1 shows antitumor effect with low toxicity.
|
-
- HY-125878
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PROTAC SGK3 degrader-1
SGK3-PROTAC1
|
PROTACs
SGK
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Cancer
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PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on von Hippel-Lindau ligand. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
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- HY-103636
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PROTAC Sirt2 Degrader-1
|
Sirtuin
PROTACs
|
Cancer
|
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
|
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- HY-107453
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SirReal1-O-propargyl
PROTAC Sirt2-binding moiety 1
|
Ligands for Target Protein for PROTAC
|
Cancer
|
SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2.
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- HY-W190966
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-
- HY-139304
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-
- HY-130404
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-
- HY-130536
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-
- HY-130520
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-
- HY-130662
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-
- HY-130416
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-
- HY-140736A
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-
- HY-140736B
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-
- HY-140204
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-
- HY-141399
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-
- HY-141222
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-
- HY-140057
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-
- HY-141400
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-
- HY-141408
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-
- HY-141224
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- HY-130589
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-
- HY-141398
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-
- HY-140360
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-
- HY-140398
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-
- HY-141403
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-
- HY-141376
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-
- HY-141401
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-
- HY-141219
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-
- HY-141223
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-
- HY-130507
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-
- HY-141221
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-
- HY-141375
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-
- HY-141402
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-
- HY-141396
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-
- HY-126948
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- HY-126950
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- HY-140056
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- HY-141112
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- HY-140284A
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- HY-113828
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-
- HY-140507
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- HY-130500
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- HY-108368
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-
- HY-140164
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-
- HY-140001
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- HY-140594
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- HY-140809
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- HY-140590
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- HY-141407
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-
- HY-130228
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-
- HY-130598
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- HY-146368
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PROTAC VEGFR-2 degrader-1
|
PROTACs
VEGFR
|
Cancer
|
PROTAC VEGFR-2 degrader-1(PROTAC-1), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM).
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- HY-145073
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- HY-146369
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PROTAC VEGFR-2 degrader-2
|
PROTACs
VEGFR
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Cancer
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PROTAC VEGFR-2 degrader-2(PROTAC-4), a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100μM).
|
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- HY-140828
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m-PEG4-azide
13-Azido-2,5,8,11-tetraoxatridecane
|
PROTAC Linkers
|
Cancer
|
m-PEG4-azide (13-Azido-2,5,8,11-tetraoxatridecane) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
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- HY-124011
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-
- HY-145484
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PROTAC IRAK4 ligand-3
|
PROTACs
|
Cancer
|
PROTAC IRAK4 ligand-3 is a ligand of PROTAC IRAK4 degrader-7 (HY-145483). PROTAC IRAK4 ligand-3 can be used for the research of cancer.
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- HY-130641
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Br-C10-methyl ester
|
PROTAC Linkers
|
Cancer
|
Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432). PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein.
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- HY-130568
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- HY-135796
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- HY-W067489
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- HY-22340
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- HY-W016735
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- HY-130619
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Boc-C1-PEG3-C4-OBn
|
PROTAC Linkers
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Cancer
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Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
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- HY-W039197
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- HY-42617
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- HY-126456
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- HY-130330
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- HY-130599
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- HY-147192
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- HY-139549
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Thalidomide-benzo
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Ligands for E3 Ligase
|
Cancer
|
Thalidomide-benzo hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-benzo can be connected to the ligand for protein by a linker to form PROTACs.
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- HY-W008296
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NH2-C6-NH-Boc
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PROTAC Linkers
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Cancer
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NH2-C6-NH-Boc is a PROTAC linker which refers to the alkyl/ether composition. NH2-C6-NH-Boc can be used in the synthesis the Mcl-1 inhibitor based on PROTAC.
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- HY-W014099
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Boc-NH-C4-acid
|
PROTAC Linkers
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Cancer
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Boc-NH-C4-acid is a PROTAC linker, which belongs to a Alkyl/ether linker. Boc-NH-C4-acid can be used in the synthesis of the compound PROTAC1, and specifically degrades EED, EZH2, and SUZ12 in the PRC2 Complex.
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- HY-130334
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- HY-126959
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- HY-133176
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- HY-126962
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- HY-126887
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- HY-126961
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- HY-126963
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- HY-140455
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- HY-147205E
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- HY-40178
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NH2-C4-NH-Boc
|
PROTAC Linkers
|
Cancer
|
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
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- HY-143458
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FAK PROTAC B5
|
FAK
PROTACs
|
Cancer
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FAK PROTAC B5 (Compound B5) is a FAK PROTAC degrader with an IC50 value of 14.9 nM. FAK PROTAC B5 presents strong FAK degradation activity, antiproliferative activity, outstanding plasma stability and moderate membrane permeability. FAK PROTAC B5 inhibits cell migration and invasion.
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- HY-23167
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- HY-140802
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- HY-133061
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- HY-140217
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- HY-122459
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- HY-140801
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- HY-140218
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- HY-122456
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- HY-140759
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-
- HY-126882
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- HY-130291
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- HY-133009
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- HY-130586
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- HY-130290
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- HY-133008
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- HY-135179
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- HY-133175
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- HY-126957
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- HY-133174
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- HY-132004
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- HY-130560
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- HY-120781
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- HY-140074
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- HY-141406
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- HY-140239
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- HY-130742
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- HY-130420
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- HY-140077
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- HY-35261A
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- HY-23095
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Thalidomide-5-OH
|
Ligands for E3 Ligase
|
Cancer
|
Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.
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- HY-135382A
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- HY-139540
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Pomalidomide-6-OH
|
Ligands for E3 Ligase
|
Cancer
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Pomalidomide-6-OH is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-OH can be connected to the ligand for protein by a linker to form PROTAC.
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- HY-141404
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- HY-W016087
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Monoethyl pimelate
|
PROTAC Linkers
|
Cancer
|
Monoethyl pimelate is a PROTAC linker, which refers to the alkyl/ether composition. Monoethyl pimelate can be used in the synthesis of (S,R,S)-AHPC-Me-C7 ester, a specific BCL-XL PROTAC degrader.
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- HY-122725A
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- HY-151476
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- HY-42745
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m-PEG2-Tos
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG2-Tos is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG2-Tos is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-140067
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- HY-140406
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- HY-140596
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- HY-130715
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tert-Butyl 11-aminoundecanoate
|
PROTAC Linkers
|
Cancer
|
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
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- HY-130470
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- HY-120773
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- HY-126881
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-
- HY-130077
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- HY-120918
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NH2-PEG7
|
PROTAC Linkers
|
Cancer
|
NH2-PEG7 is a PROTAC linker, which refers to the PEG composition. NH2-PEG7 can be used in the synthesis of the PROTAC PARP1 degrader iRucaparib-AP6.
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- HY-123324
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Pomalidomide-5-OH
5-Hydroxy pomalidomide; CC-17368
|
Ligands for E3 Ligase
|
Cancer
|
Pomalidomide-5-OH (5-hydroxy pomalidomide) is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTAC.
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- HY-130312
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- HY-139546
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- HY-133006
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- HY-148834
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- HY-130693
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- HY-139541
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Pomalidomide-5-O-CH3
|
Ligands for E3 Ligase
|
Cancer
|
Pomalidomide-5-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
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- HY-139542
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Pomalidomide-6-O-CH3
|
Ligands for E3 Ligase
|
Cancer
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Pomalidomide-6-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
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- HY-138752
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- HY-130490
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- HY-130143
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- HY-W010764
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- HY-130197
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- HY-139543
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Thalidomide-5-PEG2-Cl
|
Ligands for E3 Ligase
|
Cancer
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Thalidomide-5-PEG2-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-PEG2-Cl can be connected to the ligand for protein by a linker to form PROTACs.
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- HY-138752A
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- HY-148771
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- HY-149236
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- HY-117519A
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- HY-126458
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- HY-135306
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- HY-126888
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- HY-117519
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- HY-146349
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PROTAC EGFR degrader 4
|
PROTACs
EGFR
Autophagy
|
Cancer
|
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
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- HY-139545
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- HY-132991
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ML 2-14
|
PROTAC Linkers
|
Others
|
ML 2-14 is a PROTAC for degrading BRD4, with C4 alkyl linker. ML 2-14 exerts degradation of BRD4 in 231MFP breast cancer cells.
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- HY-130549
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Acid-PEG3-C2-Boc
|
PROTAC Linkers
|
Cancer
|
Acid-PEG3-C2-Boc is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs for the degradation of EGFR and inhibition of mTOR.
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- HY-130695
-
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- HY-118764
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Propargyl-PEG2-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Propargyl-PEG2-acid is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-117104
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Hydroxy-PEG4-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Hydroxy-PEG4-acid is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG4-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-141159
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- HY-112559
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- HY-141160
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- HY-141161
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- HY-120587
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- HY-126891
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- HY-141162
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- HY-140015
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- HY-133737
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- HY-151475
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- HY-141178
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-
- HY-141181
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- HY-133049
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- HY-130382
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-
- HY-141187
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-
- HY-41921
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- HY-141166
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- HY-141183
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- HY-130374
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- HY-133229
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- HY-141180
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- HY-130375
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- HY-126977
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- HY-141189
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- HY-141179
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- HY-141177
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- HY-141169
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- HY-130378
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- HY-130584
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- HY-130380
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- HY-130384
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- HY-141188
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- HY-141168
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- HY-23408
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Tos-PEG3
|
PROTAC Linkers
|
Cancer
|
Tos-PEG3 is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Tos-PEG3 (structure 1) can be used for the synthesis of 3'-aminooxy oligonucleotides solid supports.
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- HY-126886
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Mal-PEG1-NHS ester
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Mal-PEG1-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Mal-PEG1-NHS ester is PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
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- HY-130499
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ERRα Ligand-Linker Conjugates 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
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- HY-130620
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PEG3-C4-OBn
|
PROTAC Linkers
|
Cancer
|
PEG3-C4-OBn is a polyethylene glycol (PEG)-based PROTAC linker. PEG3-C4-OBn can be used in the synthesis of the PROTAC SGK3 degrader-1 (HY-125878). PROTAC SGK3 degrader-1 is a potent SKG3 degrader based on PROTAC.
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- HY-140501
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m-PEG11-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG11-acid is a non-cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG11-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-140500
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m-PEG10-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG10-acid is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG10-acid is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-130146
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-
- HY-141395
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m-PEG4-Boc
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG4-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG4-Boc is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-21577
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-
- HY-108369
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Azido-PEG1-CH2CO2H
|
PROTAC Linkers
|
Cancer
|
Azido-PEG1-CH2CO2H is a PROTAC linker, which refers to the alkyl/ether composition. Azido-PEG1-CH2CO2H can be used in the synthesis of PROTAC BRD4 Degrader-1.
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- HY-133131
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-
- HY-140215
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Azido-PEG6-amine
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PROTAC Linkers
ADC Linker
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Cancer
|
Azido-PEG6-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-amine is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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- HY-140226
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m-PEG10-amine
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG10-amine is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG10-amine is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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- HY-126951
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Aminooxy-PEG2-alcohol
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Aminooxy-PEG2-alcohol is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Aminooxy-PEG2-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-140004
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Azide-PEG3-Tos
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Azide-PEG3-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azide-PEG3-Tos is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-113931
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Aminooxy-PEG2-azide
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Aminooxy-PEG2-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Aminooxy-PEG2-azide is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-130211
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Azido-PEG5-alcohol
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG5-alcohol is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG5-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-141220
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m-PEG12-OH
|
PROTAC Linkers
ADC Linker
|
Cancer
|
m-PEG12-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. m-PEG12-OH is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-140227
-
m-PEG12-amine
|
PROTAC Linkers
ADC Linker
|
Cancer
|
m-PEG12-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. m-PEG12-amine is also a non-cleavable 12 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-124123
-
Aminooxy-PEG4-alcohol
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Aminooxy-PEG4-alcohol is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Aminooxy-PEG4-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-131386A
-
-
- HY-135382
-
PROTAC IRAK4 degrader-2
|
PROTACs
IRAK
|
Cancer
Inflammation/Immunology
|
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-120775
-
-
- HY-129704
-
-
- HY-130563
-
-
- HY-133736
-
-
- HY-137538
-
-
- HY-129704A
-
-
- HY-130639
-
-
- HY-137537
-
-
- HY-151719
-
Azidoacetic Acid
2-Azidoacetic acid
|
ADC Linker
|
Others
|
Azidoacetic Acid (2-Azidoacetic acid) (compound 92-1) is a click chemistry reagent containing an azide group. Azidoacetic Acid can be used as a small molecule tool for the synthesis of PROTAC.
|
-
- HY-130389
-
-
- HY-148406
-
-
- HY-140150
-
Azido-PEG3-Val-Cit-PAB-PNP
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG3-Val-Cit-PAB-PNP is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG3-Val-Cit-PAB-PNP is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-140149
-
Azido-PEG4-Val-Cit-PAB-OH
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG4-Val-Cit-PAB-OH is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG4-Val-Cit-PAB-OH is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-126949
-
Aminooxy-PEG3-azide
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Aminooxy-PEG3-azide is a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Aminooxy-C2-PEG3-azide is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-141218
-
m-PEG10-alcohol
Decaethylene glycol monomethyl ether
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG10-alcohol (Decaethylene glycol monomethyl ether) is a non-cleavable 10 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). m-PEG10-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-133191
-
-
- HY-W043277
-
-
- HY-133189
-
-
- HY-135309
-
-
- HY-120217
-
VH032
|
Ligands for E3 Ligase
|
Cancer
|
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a KdPROTACs.
|
-
- HY-130737
-
-
- HY-148362
-
-
- HY-133192
-
Bis-propargyl-PEG3
|
PROTAC Linkers
|
Cancer
Infection
|
Bis-propargyl-PEG3 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG3 is used in the synthesis of zinc-dipicolylamine (ZnDPA) complexes with antiplasmodial activity .
|
-
- HY-130554
-
-
- HY-133230
-
-
- HY-130147
-
-
- HY-117045
-
-
- HY-114670
-
-
- HY-130373
-
-
- HY-113921
-
-
- HY-130194
-
Azido-PEG5-CH2CO2H
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG5-CH2CO2H is a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG5-CH2CO2H is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-130640
-
-
- HY-130422
-
Tos-PEG4-t-butyl ester
Tos-PEG4-Boc
|
PROTAC Linkers
|
Cancer
|
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 (HY-111546). BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC50 of 18 nM.
|
-
- HY-130770
-
-
- HY-130820
-
-
- HY-131184
-
-
- HY-130617
-
Pomalidomide-amido-C1-Br
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity.
|
-
- HY-114872
-
-
- HY-132856
-
-
- HY-133484B
-
-
- HY-115414
-
-
- HY-130981
-
-
- HY-117186
-
Bis-propargyl-PEG6
|
PROTAC Linkers
|
Metabolic Disease
|
Bis-propargyl-PEG6 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG6 can be used to synthesize the polymer linked multimers of guanosine-3', 5'-cyclic monophosphates.
|
-
- HY-133190
-
Bis-propargyl-PEG7
|
PROTAC Linkers
|
Metabolic Disease
|
Bis-propargyl-PEG7 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG7 can be used to synthesize the polymer linked multimers of guanosine-3', 5'-cyclic monophosphates.
|
-
- HY-129941
-
-
- HY-129941A
-
-
- HY-130442
-
Mal-PEG2-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Mal-PEG2-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Mal-PEG2-acid can be conjugated to Tubulysin (HY-128914) and its derivative cytotoxic molecule. Mal-PEG2-acid is also a PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-114872A
-
-
- HY-121507
-
-
- HY-130137
-
-
- HY-139185
-
PROTAC ERRα Degrader-3
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
|
-
- HY-130708
-
UNC6852
|
Histone Methyltransferase
PROTACs
|
Cancer
|
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED.
|
-
- HY-135345
-
PROTAC FKBP Degrader-3
|
PROTACs
FKBP
|
Cancer
|
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.
|
-
- HY-W013253
-
-
- HY-130390
-
-
- HY-130537
-
Azido-PEG6-alcohol
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Azido-PEG6-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Azido-PEG6-alcohol is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-139436
-
-
- HY-130474
-
Azido-PEG6-NHS ester
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG6-NHS ester is a cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG6-NHS ester is also a PEG- and Alkyl/ether based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-130184
-
Azido-PEG8-NHS ester
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG8-NHS ester is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG8-NHS ester is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-130821
-
-
- HY-130819
-
-
- HY-141481
-
-
- HY-130407
-
Lipoamido-PEG3-OH
|
PROTAC Linkers
|
Cancer
|
Lipoamido-PEG3-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Lipoamido-PEG3-OH (compound TA-TEG-G2CN) can be used in the formation of a highly stable, dendronized gold nanoparticle (AuNP)-based drug delivery platform.
|
-
- HY-128716A
-
Pomalidomide-PEG3-C2-NH2 TFA
Cereblon Ligand-Linker Conjugates 5 TFA; E3 ligase Ligand-Linker Conjugates 30 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Pomalidomide-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 5 (TFA)) is a synthetic E3 ligase ligand-linker conjugate comprising a Pomalidomide (HY-10984)-based cereblon ligand and a 3-unit PEG linker. Pomalidomide-PEG3-C2-NH2 TFA can be used for the synthesis of PROTACs.
|
-
- 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-137531
-
-
- HY-139661
-
-
- HY-146423
-
PROTAC EGFR degrader 6
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.
|
-
- HY-42618
-
Azido-PEG4-CH2-Boc
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Azido-PEG4-CH2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG4-CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-141798
-
-
- HY-146422
-
PROTAC EGFR degrader 5
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR Del19 in HCC827 cells with the DC50 of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase.
|
-
- HY-135090
-
m-PEG8-Tos
|
PROTAC Linkers
|
Cancer
|
Tos-PEG8-m is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-d). Tos-PEG8-m is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277).
|
-
- HY-131188
-
PROTAC Bcl-xL degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL (Bcl-2 family member) ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
|
-
- HY-140345A
-
L-Homopropargylglycine hydrochloride
|
PROTAC Linkers
|
Cancer
|
L-Homopropargylglycine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-homopropargylglycine hydrochloride is an amino acid analog of methionine containing an alkyne moiety that can undergo a classic click chemical reaction with azide containing Alexa Fluor.
|
-
- HY-140345
-
L-Homopropargylglycine
|
PROTAC Linkers
|
Cancer
|
L-Homopropargylglycine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. L-homopropargylglycine is an amino acid analog of methionine containing an alkyne moiety that can undergo a classic click chemical reaction with azide containing Alexa Fluor.
|
-
- HY-136166
-
-
- HY-136156
-
-
- HY-136186
-
-
- HY-W067061
-
Hydroxy-PEG2-(CH2)2-Boc
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Hydroxy-PEG2-(CH2)2-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG2-(CH2)2-Boc is extracted from patent WO2004008101A2 (compound 196). Hydroxy-PEG2-(CH2)2-Boc is also a PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-42489
-
N3-PEG3-CH2CH2-Boc
|
ADC Linker
PROTAC Linkers
|
Cancer
|
N3-PEG3-CH2CH2-Boc is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N3-PEG3-CH2CH2-Boc is also a PEG- and Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-139309
-
-
- HY-152261
-
MS6105
|
PROTACs
|
Cancer
|
MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) that effectively degrades LDHA and LDHB in a time- and ubiquitin-proteasome system-dependent manner and has anticancer activity.
|
-
- HY-145818
-
JPS035
|
HDAC
PROTACs
|
Cancer
|
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-145816
-
JPS016
|
HDAC
PROTACs
|
Cancer
|
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-145819
-
JPS036
|
HDAC
PROTACs
|
Cancer
|
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-136187
-
-
- HY-145815
-
JPS014
|
HDAC
PROTACs
|
Cancer
|
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.
|
-
- HY-148777
-
A031
|
PROTACs
Androgen Receptor
|
Cancer
|
A031 is a highly effective PROTAC androgen receptor (AR) degrader with an IC50 value less than 0.25 μM for AR protein degradation. A031 has an inhibitory effect on tumor growth in zebrafish with human prostate cancer (VCaP).
|
-
- HY-118808
-
-
- HY-126976
-
Propargyl-PEG5-amine
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Propargyl-PEG5-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- HY-114661
-
m-PEG4-Tos
|
PROTAC Linkers
|
Cancer
|
m-PEG4-Tos is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-b). m-PEG4-Tos is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277).
|
-
- HY-W042501
-
m-PEG5-Tos
|
PROTAC Linkers
|
Cancer
|
m-PEG5-Tos is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-c). m-PEG5-Tos is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277).
|
-
- HY-W051634
-
Propargyl-PEG2-amine
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Propargyl-PEG2-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
|
-
- 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-130711A
-
(S,R,S)-AHPC-C3-NH2 TFA
VH032-C3-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
|
-
- HY-130711
-
(S,R,S)-AHPC-C3-NH2
VH032-C3-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
|
-
- HY-115718A
-
PZ703b TFA
|
PROTACs
|
Cancer
|
PZ703b TFA is a Bcl-xl PROTAC degradation agent that induces apoptosis and inhibits cancer cell proliferation for bladder cancer research.
|
-
- HY-150879
-
-
- HY-43722
-
Lenalidomide-Br
|
Ligands for E3 Ligase
|
Cancer
|
Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
|
-
- HY-150400
-
-
- HY-150616
-
-
- HY-129966
-
PROTAC IRAK4 degrader-1
|
PROTACs
IRAK
|
Cancer
|
PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
|
-
- 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.
|
-
- HY-151110
-
PROTAC CDK12/13 Degrader-1
|
CDK
|
Cancer
|
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research.
|
-
- HY-126534
-
-
- 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-W087383
-
-
- HY-147235
-
RIPK2-IN-2
|
RIP kinase
PROTACs
|
Infection
|
RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases.
|
-
- HY-133044
-
Boc-Pip-alkyne-Ph-COOH
|
PROTAC Linkers
|
Cancer
|
Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-130845
-
-
- HY-136257
-
CMP98
|
PROTACs
|
Others
|
CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11. CMP98 consists of two von Hippel-Lindau ligands on their active domain.
|
-
- HY-130845A
-
-
- HY-136010
-
-
- HY-126894
-
Bis-PEG9-acid
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Bis-?PEG9-?acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-?PEG9-?acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-126893
-
Bis-PEG8-acid
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Bis-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG8-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-126892
-
Bis-PEG7-acid
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Bis-PEG7-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG6-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-130813
-
-
- HY-130716
-
-
- HY-130408
-
m-PEG6-Amine
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG6-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG6-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-W018174
-
m-PEG3-Amine
|
ADC Linker
PROTAC Linkers
|
Cancer
|
m-PEG3-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG3-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-140310
-
TCO-PEG4-DBCO
|
ADC Linker
PROTAC Linkers
|
Cancer
|
TCO-PEG4-DBCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. TCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-130410
-
Bis-PEG6-NHS ester
|
ADC Linker
PROTAC Linkers
|
Cancer
|
Bis-PEG6-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG6-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-147858
-
PROTAC EGFR degrader 7
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research.
|
-
- 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-115718B
-
PZ703b hydrochloride
|
PROTACs
Apoptosis
|
Cancer
|
PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research.
|
-
- HY-115718
-
PZ703b
|
PROTACs
|
Cancer
|
PZ703b is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b can be used for the research of bladder cancer research.
|
-
- HY-130387
-
Propargyl-PEG4-Tos
|
PROTAC Linkers
ADC Linker
|
Cancer
|
Propargyl-PEG4-Tos is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG4-Tos is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-134823
-
MD-222
|
MDM-2/p53
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
|
-
- HY-129703B
-
-
- HY-136165
-
-
- HY-129703
-
-
- HY-126534A
-
-
- HY-130988A
-
-
- HY-132998
-
HDAC6 degrader-1
|
PROTACs
|
Others
|
HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation.
|
-
- HY-126885
-
DBCO-PEG5-NHS ester
|
ADC Linker
PROTAC Linkers
|
Cancer
|
DBCO-PEG5-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG5-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-129703A
-
-
- HY-129776
-
K-Ras ligand-Linker Conjugate 2
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-129775
-
K-Ras ligand-Linker Conjugate 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-114312
-
MD-224
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
|
-
- HY-130991
-
K-Ras ligand-Linker Conjugate 6
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-138551A
-
-
- HY-130683
-
-
- HY-147525
-
-
- HY-133699
-
Pomalidomide-PEG4-COOH
|
Ligands for E3 Ligase
|
Others
|
Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1).
|
-
- HY-139156
-
SK-575
|
PARP
PROTACs
|
Cancer
|
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations.
|
-
- HY-130682
-
-
- HY-145479
-
PROTAC AR-V7 degrader-1
|
PROTACs
Androgen Receptor
|
Cancer
|
PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC50 of 0.32 µM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC50 of 0.88 µM.
|
-
- HY-133799
-
-
- HY-136688
-
MI-389
|
PROTACs
|
Cancer
|
MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4 CRBN E3 ligase.
|
-
- HY-141881
-
PROTAC-O4I2
|
PROTACs
Apoptosis
|
Cancer
|
PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.
|
-
- HY-141680
-
CPS2
|
CDK
|
Cancer
|
CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia.
|
-
- HY-146324
-
-
- HY-130988
-
Ipatasertib-NH2
GDC-0068-NH2; RG7440-NH2
|
Ligands for Target Protein for PROTAC
|
Cancer
|
Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
|
-
- HY-132296
-
GSK215
|
FAK
PROTACs
|
Cancer
|
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
|
-
- HY-130612
-
PROTAC BRD2/BRD4 degrader-1
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
|
-
- HY-130979
-
-
- HY-130521
-
Pomalidomide-amido-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 22; E3 ligase Ligand-Linker Conjugates 55
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Pomalidomide-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-130652
-
Pomalidomide 4'-PEG3-azide
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1 degrader based on Rucaparib by using the PROTAC approach.
|
-
- HY-141438
-
SIM1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.
|
-
- HY-134592
-
-
- HY-115881
-
SR-1114
|
PROTACs
|
Cancer
|
SR-1114 is a first-in-class PROTAC ENL degrader. SR-1114 elicits rapid, CRBN-dependent degradation of ENL with DC50s of 150 nM, 311 nM, and 1.65 μM in MV4;11 , MOLM-13, and OCI/AML-2 cells, respectively.
|
-
- HY-145177
-
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader. (From patent WO2017180417A1 compound s7).
|
-
- HY-138550A
-
-
- HY-144323
-
YF135
|
PROTACs
PERK
|
Cancer
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
|
-
- HY-136055
-
-
- HY-145226
-
XY-06-007
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
XY-06-007 is a selective and potent bump-and-hole (B&H)-PROTAC BRD4BD1L94V degrader. XY-06-007 shows a DC50, 6 h of 10 nM against BRD4BD1L94V with no degradation of off-targets. XY-06-007 demonstrates suitable pharmacokinetics for in vivo studies.
|
-
- HY-122582
-
TL13-12
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984).
|
-
- HY-145281
-
MS98
|
PROTACs
Akt
|
Cancer
|
MS98 is a potent and selective PROTAC AKT degrader. MS98 depletes cellular total AKT (T-AKT) with the DC50 value of 78 nM. MS98 binds to AKT1, AKT2, and AKT3 with Kds of 4 nM, 140 nM, and 8.1 nM, respectively.
|
-
- HY-145282
-
MS170
|
PROTACs
Akt
|
Cancer
|
MS170 is a potent and selective PROTAC AKT degrader. MS170 depletes cellular total AKT (T-AKT) with the DC50 value of 32 nM. MS170 binds to AKT1, AKT2, and AKT3 with Kds of 1.3 nM, 77 nM, and 6.5 nM, respectively.
|
-
- HY-147025
-
-
- HY-141512
-
JB170
|
PROTACs
Aurora Kinase
|
Cancer
|
JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase.
|
-
- HY-152154
-
Nampt degrader-2
|
PROTACs
NAMPT
|
Cancer
|
Nampt degrader-2 is a fluorescent PROTAC, which efficiently degrades NAMPT with an IC50 of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD + and exerts potent antitumor activities.
|
-
- HY-130854
-
Thalidomide-NH-C6-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
|
-
- HY-134485
-
CD147 degrader 1
|
PROTACs
|
Cancer
|
CD147 degrader 1 is a PROTAC targets CD147 with an DC50 value of 6.72 µM. CD147 degrader 1 inhibits cell proliferation, migration and invasion. CD147 degrader 1 decreases the expression of CD147, MMP9, and p-STAT3 protein. CD147 degrader 1 shows anti-cancer acyivity.
|
-
- HY-144691
-
PP-C8
|
PROTACs
CDK
|
Cancer
|
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC).
|
-
- HY-145388
-
AU-15330
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
|
-
- HY-146393
-
PROTAC CYP1B1 degrader-1
|
PROTACs
Cytochrome P450
|
Cancer
|
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer.
|
-
- HY-148813
-
AK-2292
|
PROTACs
STAT
|
Cancer
|
AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models.
|
-
- HY-110167
-
TFC 007
|
PGE synthase
Ligands for Target Protein for PROTAC
|
Cancer
|
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitory activity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon).
|
-
- HY-146346
-
HD-TAC7
|
PROTACs
HDAC
|
Inflammation/Immunology
|
HD-TAC7 is a potent PROTAC HDAC degrader with IC50 values of 3.6 μM, 4.2 μM and 1.1 μM for HDAC1, HDAC2 and HDAC3, respectively. HD-TAC7 can decreases NF-κB p65 in RAW 264.7 macrophages. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
|
-
- HY-138642
-
Vepdegestrant
ARV-471
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of ~2 nM.
|
-
- HY-75706
-
N-Descyclopropanecarbaldehyde Olaparib
|
E3 Ligase Ligand-Linker Conjugates
PARP
|
Cancer
|
N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a CRBN-based ligand for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4. N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
|
-
- HY-133487A
-
-
- HY-122653
-
CCT367766
|
PROTACs
|
Cancer
|
CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein.
|
-
- HY-122653A
-
CCT367766 formic
|
PROTACs
|
Cancer
|
CCT367766 formic is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 formic exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 formic reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 formic provides a potential chemical tool to study a largely unexplored protein.
|
-
- HY-129602
-
SD-36
|
PROTACs
STAT
Apoptosis
|
Cancer
|
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.
|
-
- HY-W017440
-
-
- HY-W018745
-
-
- HY-146231
-
SS47
|
PROTACs
MAP4K
|
Cancer
Inflammation/Immunology
|
SS47, 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.
|
-
- HY-151792
-
Pomalidomid-C6-PEG3-butyl-N3
|
PROTACs
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader.
|
-
- HY-W004896
-
-
- HY-W004816
-
-
- HY-W017772
-
-
- HY-W025896
-
-
- HY-W140896
-
-
- HY-126916
-
-
- HY-128803
-
-
- HY-125907
-
-
- HY-128805
-
-
- HY-141233
-
-
- HY-W007341
-
-
- HY-130458
-
EGNHS
EGS crosslinker
|
PROTAC Linkers
|
Cancer
|
EGNHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-141232
-
-
- HY-138749
-
-
- HY-141263
-
-
- HY-W050087
-
-
- HY-143820
-
-
- HY-141230
-
-
- HY-116899
-
-
- HY-141231
-
-
- HY-130292
-
-
- HY-W096085
-
-
- HY-W096121
-
-
- HY-134751
-
-
- HY-43614
-
-
- HY-125842
-
-
- HY-128833
-
-
- HY-141260
-
-
- HY-124480
-
-
- HY-119343
-
-
- HY-141186
-
-
- HY-140338
-
-
- HY-143819
-
-
- HY-130888
-
-
- HY-124318
-
-
- HY-W067705
-
-
- HY-140341
-
-
- HY-140346
-
-
- HY-140339
-
-
- HY-140656A
-
-
- HY-D1295
-
-
- HY-140335
-
-
- HY-134719
-
-
- HY-130887
-
-
- HY-W019795
-
-
- HY-123916
-
-
- HY-141293
-
-
- HY-141165
-
-
- HY-141175
-
-
- HY-130893
-
-
- HY-141176
-
-
- HY-140346A
-
-
- HY-138467
-
-
- HY-W004945
-
-
- HY-144304
-
PROTAC EGFR degrader 2
|
PROTACs
EGFR
|
Cancer
|
PROTAC EGFR degrader 2 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 2 exhibits excellent antiproliferative activity with IC50 of 4.0 nM and good EGFR degradation activity with DC50 of 36.51 nM. PROTAC EGFR degrader 2 can be used for the synthesis of nitroreductase (NTR)-responsive PROTAC.
|
-
- HY-126908
-
-
- HY-W096096
-
-
- HY-130908
-
-
- HY-141186A
-
-
- HY-130283
-
-
- HY-140293
-
-
- HY-22393
-
-
- HY-127056
-
-
- HY-W190971
-
-
- HY-138401
-
-
- HY-134746
-
-
- HY-113336B
-
-
- HY-138461
-
-
- HY-120175
-
-
- HY-140280
-
-
- HY-W076543
-
-
- HY-140329
-
-
- HY-136168
-
-
- HY-133404
-
-
- HY-W042657
-
-
- HY-42145
-
-
- HY-W018365
-
-
- HY-W044459
-
-
- HY-132065
-
-
- HY-134695
-
-
- HY-138409
-
-
- HY-140357
-
-
- HY-W096150
-
-
- HY-77959
-
-
- HY-140343
-
-
- HY-140991
-
-
- HY-140208
-
-
- HY-141136
-
-
- HY-W042713
-
-
- HY-124531
-
-
- HY-W142506
-
-
- HY-141128
-
-
- HY-140947
-
-
- HY-130898
-
BM-PEG3
1,11-Bis-maleimidotetraethyleneglycol
|
PROTAC Linkers
|
Cancer
|
BM-PEG3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-140328
-
-
- HY-W037355
-
-
- HY-W007853
-
-
- HY-W018464
-
-
- HY-W096158
-
-
- HY-W042625
-
-
- HY-141268
-
-
- HY-40171
-
-
- HY-125844
-
-
- HY-W004710
-
-
- HY-130186
-
-
- HY-135820
-
-
- HY-140408
-
-
- HY-140179
-
-
- HY-132012
-
-
- HY-147205C
-
-
- HY-140281
-
-
- HY-140318
-
-
- HY-141099
-
-
- HY-133051
-
-
- HY-140496
-
-
- HY-140651
-
-
- HY-140695
-
-
- HY-140642
-
-
- HY-140652
-
-
- HY-138393
-
-
- HY-140367
-
-
- HY-140655
-
-
- HY-133050
-
-
- HY-130425
-
-
- HY-140549
-
-
- HY-141026
-
-
- HY-133386
-
-
- HY-W096116
-
-
- HY-140038
-
-
- HY-140020
-
-
- HY-140548
-
-
- HY-141332
-
-
- HY-133334
-
-
- HY-147205A
-
-
- HY-140657
-
-
- HY-140692
-
-
- HY-141267
-
-
- HY-135153
-
-
- HY-141021
-
-
- HY-138379
-
-
- HY-133054
-
-
- HY-133377
-
-
- HY-141354
-
-
- HY-140717
-
-
- HY-140962
-
-
- HY-140334
-
-
- HY-113924
-
-
- HY-140697
-
-
- HY-140183
-
-
- HY-120368
-
-
- HY-141027
-
-
- HY-W096086
-
-
- HY-133481
-
-
- HY-23166
-
-
- HY-W004447
-
-
- HY-133306
-
-
- HY-140661
-
-
- HY-140184
-
-
- HY-133308
-
-
- HY-130417
-
-
- HY-130896
-
-
- HY-140696
-
-
- HY-140674
-
-
- HY-140731
-
-
- HY-140547
-
-
- HY-140709
-
-
- HY-141020
-
-
- HY-140322
-
-
- HY-141334
-
-
- HY-W096129
-
-
- HY-130857
-
-
- HY-132078
-
-
- HY-140666
-
-
- HY-133406
-
-
- HY-140656D
-
-
- HY-140703
-
-
- HY-132098
-
-
- HY-141022
-
-
- HY-43055
-
-
- HY-133318
-
-
- HY-140690
-
-
- HY-W190901
-
-
- HY-140996
-
-
- HY-140716
-
-
- HY-140411
-
-
- HY-130555
-
-
- HY-138487
-
-
- HY-W096089
-
-
- HY-140707
-
-
- HY-140660
-
-
- HY-140672
-
-
- HY-140499
-
-
- HY-140649
-
-
- HY-140182
-
-
- HY-140176
-
-
- HY-23417
-
-
- HY-141264
-
-
- HY-141266
-
-
- HY-140265
-
-
- HY-140641
-
-
- HY-140953
-
-
- HY-W035417
-
-
- HY-W250928E
-
-
- HY-132075
-
-
- HY-141363
-
-
- HY-140656
-
-
- HY-140673
-
-
- HY-140656B
-
-
- HY-147206D
-
-
- HY-138763
-
-
- HY-140268
-
-
- HY-140667
-
-
- HY-138455
-
-
- HY-42569
-
-
- HY-W250928A
-
-
- HY-140185
-
-
- HY-143815
-
-
- HY-140018
-
-
- HY-141019
-
-
- HY-141352
-
-
- HY-140654
-
-
- HY-140721
-
-
- HY-140704
-
-
- HY-140648
-
-
- HY-124380
-
-
- HY-140409
-
-
- HY-140683
-
-
- HY-140700
-
-
- HY-140332
-
-
- HY-140693
-
-
- HY-140348
-
-
- HY-140638
-
-
- HY-140267
-
-
- HY-140161
-
-
- HY-140407
-
-
- HY-130542
-
-
- HY-140653
-
-
- HY-130904
-
-
- HY-140509
-
-
- HY-140153
-
-
- HY-138435
-
-
- HY-140723
-
-
- HY-133052
-
-
- HY-141023
-
-
- HY-W010948
-
-
- HY-140713
-
-
- HY-141393
-
-
- HY-140994
-
-
- HY-W013731
-
-
- HY-140388
-
-
- HY-140178
-
-
- HY-140659
-
-
- HY-138524
-
-
- HY-140495
-
-
- HY-141024
-
-
- HY-141383
-
-
- HY-133385
-
-
- HY-140177
-
-
- HY-140735
-
-
- HY-140640
-
-
- HY-140718
-
-
- HY-140684
-
-
- HY-140021
-
-
- HY-133384
-
-
- HY-141326
-
-
- HY-140682
-
-
- HY-140394
-
-
- HY-140665
-
-
- HY-140320
-
-
- HY-140269
-
-
- HY-140720
-
-
- HY-140410
-
-
- HY-140186
-
-
- HY-140929
-
-
- HY-130909
-
-
- HY-138764
-
-
- HY-133425
-
-
- HY-W190962
-
-
- HY-141164
-
-
- HY-130198
-
-
- HY-140494
-
-
- HY-132027
-
-
- HY-140995
-
-
- HY-140333
-
-
- HY-140708
-
-
- HY-140457
-
-
- HY-140734
-
-
- HY-133290
-
-
- HY-133324
-
-
- HY-132015
-
-
- HY-133323
-
-
- HY-140662
-
-
- HY-140502
-
-
- HY-120678
-
-
- HY-W250928B
-
-
- HY-140639
-
-
- HY-141333
-
-
- HY-140694
-
-
- HY-140705
-
-
- HY-136159
-
-
- HY-140041
-
-
- HY-138486
-
-
- HY-140699
-
-
- HY-140702
-
-
- HY-130938
-
-
- HY-140458
-
-
- HY-140358
-
-
- HY-140330
-
-
- HY-140663
-
-
- HY-132091
-
-
- HY-140724
-
-
- HY-140646
-
-
- HY-130895
-
-
- HY-141335
-
-
- HY-140685
-
-
- HY-132088
-
-
- HY-140368
-
-
- HY-W096147
-
-
- HY-43581
-
-
- HY-140656C
-
-
- HY-140710
-
-
- HY-140691
-
-
- HY-140180
-
-
- HY-140993
-
-
- HY-140040
-
-
- HY-W096166
-
-
- HY-140706
-
-
- HY-W096131
-
-
- HY-140698
-
-
- HY-140395
-
-
- HY-133322
-
-
- HY-141265
-
-
- HY-140656E
-
-
- HY-140650
-
-
- HY-141025
-
-
- HY-W096155
-
-
- HY-140715
-
-
- HY-140670
-
-
- HY-138507
-
-
- HY-140319
-
-
- HY-133231
-
-
- HY-141163
-
-
- HY-140000
-
-
- HY-147205
-
-
- HY-140005
-
-
- HY-130213
-
-
- HY-140321
-
-
- HY-140266
-
-
- HY-140022
-
-
- HY-138436
-
-
- HY-140181
-
-
- HY-140453
-
-
- HY-133291
-
-
- HY-140658
-
-
- HY-140421
-
-
- HY-138411
-
-
- HY-140736
-
-
- HY-147205D
-
-
- HY-133307
-
-
- HY-W096160
-
-
- HY-140714
-
-
- HY-138723
-
-
- HY-140456
-
-
- HY-133317
-
-
- HY-138505
-
-
- HY-140664
-
-
- HY-140671
-
-
- HY-140719
-
-
- HY-133325
-
-
- HY-140647
-
-
- HY-W096142
-
-
- HY-W096161
-
-
- HY-140039
-
-
- HY-134754
-
-
- HY-140689
-
-
- HY-125888
-
-
- HY-126313
-
-
- HY-128844
-
-
- HY-120430
-
-
- HY-140722
-
-
- HY-133493
-
-
- HY-140784
-
-
- HY-140516
-
-
- HY-140756
-
-
- HY-141368
-
-
- HY-140852
-
-
- HY-133279
-
-
- HY-138354
-
-
- HY-140450
-
-
- HY-134710
-
-
- HY-133354
-
-
- HY-133394
-
-
- HY-140387
-
-
- HY-140156
-
-
- HY-133345
-
-
- HY-143844
-
-
- HY-123629
-
-
- HY-140984
-
-
- HY-140775
-
-
- HY-133399
-
-
- HY-130534
-
-
- HY-140272
-
-
- HY-140162
-
-
- HY-140197
-
-
- HY-133395
-
-
- HY-132049
-
-
- HY-132097
-
-
- HY-135142
-
-
- HY-134752
-
-
- HY-140933
-
-
- HY-141174
-
-
- HY-138352
-
-
- HY-120724
-
-
- HY-140302
-
-
- HY-135917
-
-
- HY-132052
-
-
- HY-140957
-
-
- HY-138385
-
-
- HY-133393
-
-
- HY-141298
-
-
- HY-141367
-
-
- HY-141302
-
-
- HY-134698
-
-
- HY-140365
-
-
- HY-138449
-
-
- HY-138513
-
-
- HY-140857
-
-
- HY-133327
-
-
- HY-130600
-
-
- HY-140615
-
-
- HY-138347
-
-
- HY-138324
-
-
- HY-140036
-
-
- HY-W096069
-
-
- HY-130834
-
-
- HY-134711
-
-
- HY-138428
-
-
- HY-140618
-
-
- HY-133495
-
-
- HY-140305
-
-
- HY-126919
-
-
- HY-132070
-
-
- HY-141258
-
-
- HY-140058
-
-
- HY-130830
-
-
- HY-132095
-
-
- HY-138515
-
-
- HY-140946
-
-
- HY-140965
-
-
- HY-138518
-
-
- HY-140029
-
-
- HY-133278
-
-
- HY-140842
-
-
- HY-132053
-
-
- HY-133319
-
-
- HY-140861
-
-
- HY-140876
-
-
- HY-140963
-
-
- HY-140742
-
-
- HY-W096078
-
-
- HY-140955
-
-
- HY-140862
-
-
- HY-138382
-
-
- HY-140975
-
-
- HY-133494
-
-
- HY-W044155
-
-
- HY-130901
-
-
- HY-140823
-
-
- HY-132014
-
-
- HY-140362
-
-
- HY-141109
-
-
- HY-143827
-
-
- HY-140958
-
-
- HY-140954
-
-
- HY-138490
-
-
- HY-140396
-
-
- HY-W007529
-
-
- HY-138503
-
-
- HY-138738
-
-
- HY-141337
-
-
- HY-138325
-
-
- HY-140601
-
-
- HY-140165
-
-
- HY-140206
-
-
- HY-133300
-
-
- HY-133289
-
-
- HY-140779
-
-
- HY-W096073
-
-
- HY-138525
-
-
- HY-141357
-
-
- HY-140283
-
-
- HY-140973
-
-
- HY-138437
-
-
- HY-141272
-
-
- HY-140806
-
-
- HY-135169
-
-
- HY-138482
-
-
- HY-141394
-
-
- HY-140807
-
-
- HY-133344
-
-
- HY-W096075
-
-
- HY-141271
-
-
- HY-141106
-
-
- HY-141269
-
-
- HY-141369
-
-
- HY-140971
-
-
- HY-140399
-
-
- HY-130336
-
-
- HY-140863
-
-
- HY-130942
-
-
- HY-138722
-
-
- HY-140822
-
-
- HY-130469
-
-
- HY-141206
-
-
- HY-141366
-
-
- HY-140782
-
-
- HY-133299
-
-
- HY-130672
-
-
- HY-W096081
-
-
- HY-132068
-
-
- HY-140832
-
-
- HY-133437
-
-
- HY-140829
-
-
- HY-130890
-
-
- HY-140381
-
-
- HY-133298
-
-
- HY-140777
-
-
- HY-138342
-
-
- HY-138334
-
-
- HY-138337
-
-
- HY-W096072
-
-
- HY-140620
-
-
- HY-133294
-
-
- HY-134697
-
-
- HY-133496
-
-
- HY-141373
-
-
- HY-138477
-
-
- HY-141100
-
-
- HY-130512
-
-
- HY-W096120
-
-
- HY-140028
-
-
- HY-138391
-
-
- HY-140617
-
-
- HY-138424
-
-
- HY-133383
-
-
- HY-135940
-
-
- HY-141255
-
-
- HY-135819
-
-
- HY-140799
-
-
- HY-132021
-
-
- HY-140171
-
-
- HY-143855
-
-
- HY-140826
-
-
- HY-141093
-
-
- HY-140273
-
-
- HY-140285
-
-
- HY-141217
-
-
- HY-133352
-
-
- HY-W040527
-
-
- HY-W096157
-
-
- HY-141236
-
-
- HY-140951
-
-
- HY-140440
-
-
- HY-140059
-
-
- HY-140765
-
-
- HY-W096153
-
-
- HY-140744
-
-
- HY-138346
-
-
- HY-138483
-
-
- HY-133378
-
-
- HY-141282
-
-
- HY-140833
-
-
- HY-132104
-
-
- HY-140037
-
-
- HY-134700
-
-
- HY-140771
-
-
- HY-134720
-
-
- HY-133351
-
-
- HY-132048
-
-
- HY-130342
-
-
- HY-140751
-
-
- HY-140989
-
-
- HY-140909
-
-
- HY-140355
-
-
- HY-141101
-
-
- HY-135941
-
-
- HY-138323
-
-
- HY-138333
-
-
- HY-140282
-
-
- HY-140758
-
-
- HY-140008
-
-
- HY-140065
-
-
- HY-140733
-
-
- HY-138468
-
-
- HY-140983
-
-
- HY-130152
-
-
- HY-133295
-
-
- HY-133329
-
-
- HY-140284
-
-
- HY-138395
-
-
- HY-144081
-
-
- HY-133382
-
-
- HY-140904
-
-
- HY-133475
-
-
- HY-138739
-
-
- HY-W096077
-
-
- HY-140240
-
-
- HY-126717
-
-
- HY-140263
-
-
- HY-141238
-
-
- HY-132013
-
-
- HY-140200
-
-
- HY-140006
-
-
- HY-140616
-
-
- HY-130910
-
-
- HY-140210
-
-
- HY-141203
-
-
- HY-132114
-
-
- HY-133348
-
-
- HY-141096
-
-
- HY-133281
-
-
- HY-138472
-
-
- HY-130216
-
-
- HY-140303
-
-
- HY-140804
-
-
- HY-W096139
-
-
- HY-133277
-
-
- HY-138741
-
-
- HY-138744
-
-
- HY-133282
-
-
- HY-140913
-
-
- HY-133353
-
-
- HY-134683
-
-
- HY-133297
-
-
- HY-138721
-
-
- HY-140505
-
-
- HY-141159A
-
-
- HY-W190795
-
-
- HY-133438
-
-
- HY-132043
-
-
- HY-140175
-
-
- HY-140830
-
-
- HY-140351
-
-
- HY-141275
-
-
- HY-W042579
-
-
- HY-141204
-
-
- HY-133212
-
-
- HY-140749
-
-
- HY-133287
-
-
- HY-140754
-
-
- HY-134676
-
-
- HY-138499
-
-
- HY-140219
-
-
- HY-133498
-
-
- HY-140511
-
-
- HY-134703
-
-
- HY-138338
-
-
- HY-140898
-
-
- HY-140451
-
-
- HY-132018
-
-
- HY-133316
-
-
- HY-140382
-
-
- HY-133390
-
-
- HY-132115
-
-
- HY-130399
-
-
- HY-135049
-
-
- HY-134704
-
-
- HY-140772
-
-
- HY-138737
-
-
- HY-140278
-
-
- HY-132055
-
-
- HY-133284
-
-
- HY-140373
-
-
- HY-141171
-
-
- HY-133389
-
-
- HY-133330
-
-
- HY-141083
-
-
- HY-141082
-
-
- HY-141270
-
-
- HY-138378
-
-
- HY-134722
-
-
- HY-141338
-
-
- HY-138727
-
-
- HY-W190970
-
-
- HY-141328
-
-
- HY-141262
-
-
- HY-W143484
-
-
- HY-132085
-
-
- HY-117028
-
-
- HY-140370
-
-
- HY-138450
-
-
- HY-141308
-
-
- HY-132092
-
-
- HY-126917
-
-
- HY-140461
-
-
- HY-141226
-
-
- HY-138498
-
-
- HY-141318
-
-
- HY-132009
-
-
- HY-138531
-
-
- HY-133456
-
-
- HY-138426
-
-
- HY-140412
-
-
- HY-133439
-
-
- HY-130891
-
-
- HY-140752
-
-
- HY-140317
-
-
- HY-133276
-
-
- HY-135924
-
-
- HY-140743
-
-
- HY-132072
-
-
- HY-141184
-
-
- HY-141173
-
-
- HY-135921
-
-
- HY-W019794
-
-
- HY-140199
-
-
- HY-138423
-
-
- HY-140174
-
-
- HY-133272
-
-
- HY-140205
-
-
- HY-130195
-
-
- HY-140490
-
-
- HY-140034
-
-
- HY-153153
-
-
- HY-141331
-
-
- HY-140515
-
-
- HY-141107
-
-
- HY-42774
-
Ms-PEG4-Ms
1,11-Bis(methanesulfonyloxy)-3,6,9-trioxandecane
|
PROTAC Linkers
|
Cancer
|
Ms-PEG4-Ms is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-132051
-
-
- HY-138433
-
-
- HY-133350
-
-
- HY-132105
-
-
- HY-140448
-
-
- HY-132059
-
-
- HY-133454
-
-
- HY-132029
-
-
- HY-141294
-
-
- HY-133467
-
-
- HY-133396
-
-
- HY-138479
-
-
- HY-140371
-
-
- HY-141097
-
-
- HY-140396A
-
-
- HY-138336
-
-
- HY-W096156
-
-
- HY-140966
-
-
- HY-140969
-
-
- HY-138368
-
-
- HY-132028
-
-
- HY-140196
-
-
- HY-132074
-
-
- HY-141307
-
-
- HY-130900
-
-
- HY-138720
-
-
- HY-130597
-
-
- HY-138733
-
-
- HY-140229
-
-
- HY-W096146
-
-
- HY-138459
-
-
- HY-134707
-
-
- HY-140404
-
-
- HY-138335
-
-
- HY-138759
-
-
- HY-140805
-
-
- HY-140814
-
-
- HY-140209
-
-
- HY-133210
-
-
- HY-140974
-
-
- HY-140827
-
-
- HY-133478
-
-
- HY-132077
-
-
- HY-138420
-
-
- HY-138766
-
-
- HY-130907
-
-
- HY-130856
-
-
- HY-138434
-
-
- HY-140220
-
-
- HY-125534
-
-
- HY-141306
-
-
- HY-141205
-
-
- HY-133474
-
-
- HY-W096074
-
-
- HY-133497
-
-
- HY-130833
-
-
- HY-W096145
-
-
- HY-W096071
-
-
- HY-134747
-
-
- HY-140959
-
-
- HY-130832
-
-
- HY-130348
-
-
- HY-W004697
-
-
- HY-140066
-
-
- HY-W096164
-
-
- HY-W096107
-
-
- HY-140195
-
-
- HY-143832
-
-
- HY-130855
-
-
- HY-141207
-
-
- HY-133379
-
-
- HY-140363
-
-
- HY-133349
-
-
- HY-138340
-
-
- HY-140701
-
-
- HY-140936
-
-
- HY-134717
-
-
- HY-133455
-
-
- HY-140821
-
-
- HY-141098
-
-
- HY-140170
-
-
- HY-133000
-
-
- HY-138371
-
-
- HY-141261
-
-
- HY-140797
-
-
- HY-138374
-
-
- HY-141214
-
-
- HY-130496
-
-
- HY-141283
-
-
- HY-138419
-
-
- HY-133270
-
-
- HY-138427
-
-
- HY-133347
-