Search Result
Results for "
4-1BB Ligand Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1437
Inhibitors & Agonists
13
Biochemical Assay Reagents
22
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-P99419
-
|
GEN1046
|
PD-1/PD-L1
|
Cancer
|
|
Acasunlimab (GEN1046) is a bispecific antibody (bsAb) targeting PD-L1 and 4-1BB. Acasunlimab enhances T-cell and NK-cell function through conditional 4-1BB stimulation while constitutively blocking the PD-1/PD-L1 inhibitory axis. Acasunlimab can be used in research of cancer.
|
-
- HY-P99119
-
-
- HY-P99572
-
|
BNT-312; DuoBody-CD40x-4-1BB; GEN1042
|
TNF Receptor
|
Cancer
Inflammation/Immunology
|
|
Tecaginlimab (BNT-312) is a Fc-inert bispecific antibody for dual targeting and conditional stimulation of CD40 and 4-1BB. Tecaginlimab can enhance priming and reactivation of tumor-specific immunity.
|
-
- HY-P99605
-
|
PRS 343
|
EGFR
TNF Receptor
|
Cancer
|
|
Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research.
|
-
- HY-P990017
-
|
CD19-4-1BBL; RO7227166; RG6076
|
CD19
|
Cancer
|
|
Englumafusp alfa (CD19-4-1BBL; RO7227166) is a fusion construct comprised of a CD19-specific antibody domain fused to a trimerized extracellular domains of human 41BBL. Englumafusp alfa promotes CD19-specific 4-1BB cross-linking on the surface of T and NK cells.
|
-
- HY-P990067
-
|
ATOR-1017
|
TNF Receptor
|
Cancer
|
|
Evunzekibart (ATOR-1017) is an Fc-γ receptor conditional 4-1BB agonist and IgG4-type antibody. Evunzekibart can be used as monotherapy or in combination with anti-PD1 to exert anticancer activity.
|
-
- HY-W342590
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs.
|
-
- HY-145484
-
|
|
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.
|
-
- HY-146441
-
|
|
STAT
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Prohibitin ligand 1 (Compound 22i), a cardioprotectant prohibitin ligand, induces a phosphorylation of the pro-survival factor STAT3. Prohibitin ligand 1 exhibits in vitro cardioprotectant activities at nanomolar concentrations.
|
-
- HY-150859
-
|
|
HDAC
|
Cancer
|
|
HDAC ligand-1 is a HDAC ligand that can be used to synthesize PROTAC HDAC degraders.
|
-
- HY-156595
-
|
|
BCL6
|
Neurological Disease
|
|
BCL6 ligand-1 (compound I-94) is a ligand for TCIP 1 (HY-156531). TCIP 1 is a BCL6 inhibitor that activates apoptosis and is used in cancer research.
|
-
- HY-133045
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-147366
-
|
|
Others
|
Metabolic Disease
|
|
RBP4 ligand-1 is a non-retinoid ligands for (RBP4) retinol-binding protein 4. The hRBP4SPA IC50 and RBP4–TTR FRET IC50 values are 0.23±0.11 and 0.13±0.12 μM in the radioligand binding assay and FRET assay, respectively.
|
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- HY-150407
-
|
|
Ligands for Target Protein for PROTAC
Autophagy
|
Cancer
Neurological Disease
Others
|
|
TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.
|
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- HY-151479
-
|
|
Others
|
Cancer
|
|
GID4 Ligand 3 (compound 16) is a binder of GID4 with an Kd value of 110 μM in vitro and an IC50 value of 148.5 μM. GID4 Ligand 3 can be used for the research related to cereblon and Von Hippel-Lindau.
|
-
- HY-43869
-
|
PSMA-617 Ligand-Linker Conjugate
|
ADC Linker
|
Cancer
|
|
Vipivotide tetraxetan Ligand-Linker Conjugate (PSMA-617 Ligand-Linker Conjugate) is composed of a linker and Glutamate-urea-Lysine, can be used to synthesize Vipivotide tetraxetan (PSMA-617). Glutamate-urea-Lysine is is the selective pharmacophore to bind to prostate specific membrane antigen (PSMA).
|
-
- HY-145308
-
-
- HY-133073
-
|
CCR7-Cmp2105
|
CCR
Ligands for Target Protein for PROTAC
|
Cancer
|
|
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
|
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- HY-126456
-
|
VH032-propargyl; VHL Ligand 7
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs. (S,R,S)-AHPC-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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- HY-P1840A
-
|
|
Neuropeptide Y Receptor
|
Endocrinology
Neurological Disease
|
|
Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively.
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- HY-P1840
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively.
|
-
- HY-133046
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader. VHL Ligand-Linker Conjugates 17 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-115953
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM).
|
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- HY-128808
-
|
E3 ligase Ligand 12
|
Ligands for E3 Ligase
|
Cancer
|
|
cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-128809
-
|
E3 ligase Ligand 11
|
Ligands for E3 Ligase
|
Cancer
|
|
cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-103597
-
|
Cereblon Ligand 3; E3 ligase Ligand 3
|
Ligands for E3 Ligase
|
Others
|
|
Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-150885
-
|
|
Ligands for Target Protein for PROTAC
Btk
|
Cancer
|
|
BTK ligand 1 (compound 1) is a ligand targeting Bruton’s tyrosine kinase (Btk). BTK ligand 1 can combine with E3 ligase ligand (Ligand for E3 Ligase) through PROTAC Linker to form PROTAC. PROTACs targeting Btk can be used in the study of chronic lymphocytic leukemia (CLL) and other BK cell malignancies.
|
-
- HY-103596
-
|
Cereblon Ligand 2; E3 ligase Ligand 2
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-128837
-
|
MDM2 Ligand 1; E3 ligase Ligand 16
|
Ligands for E3 Ligase
|
Cancer
|
|
Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-41547
-
|
Cereblon Ligand 4; E3 ligase Ligand 4
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
|
-
- HY-146102
-
|
|
mAChR
|
Others
|
|
M1 ligand 1 (compound 3b-b) is a muscarinic acetylcholine receptor M1 ligand. M1 ligand 1 is a N-desmethyl congener of arecoline derivative. M1 ligand 1 can be used as PET (positron emission tomography) radiotracer.
|
-
- HY-139656
-
-
- HY-156994
-
|
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Others
|
Others
|
|
ASGPR ligand-1 is an asialoglycoprotein receptor (ASGPR) ligand compound. ASGPR ligand-1 can be used for kinds of diseases research.
|
-
- HY-141724
-
|
|
Ser/Thr Protease
|
Cancer
|
|
PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. PCSK9 ligand 1 does not affect PCSK9 function.
|
-
- HY-128807
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
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- HY-129653
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
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- HY-128811
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-43961
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-128810
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-128806
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-139906
-
-
- HY-146125
-
|
|
Others
|
Metabolic Disease
|
|
CGCG/CGG ligand 1 (compound 10), an anthracenone derivative, is a CGCG or CGG short spacer-ligand. CGCG/CGG ligand 1 can protect cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme.
|
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- HY-114399
-
-
- HY-154844
-
|
|
Others
|
Cancer
|
|
FAP Ligand 1 (FL), a high-affinity FAP small-molecule ligand, is used to target attached drugs to FAP-expressing fibroblasts and can be used in radiation imaging studies of targeted cancers.
|
-
- HY-150410
-
|
|
AUTACs
|
Cancer
|
|
TSPO ligand-3 is a ligand of AUTAC2. AUTAC2 contains an p-fluorobenzylguanine (FBnG) and an synthetic ligand of FKBP (SLF) moiety, which can cause significant silencing of FKBP12 in HeLa cells.
|
-
- HY-125905
-
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VHL Ligand 3; E3 ligase Ligand 19
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.
|
-
- HY-149337
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling.
|
-
- HY-146081
-
|
|
CD22
|
Cancer
|
|
CD22 ligand-1 (compound 12) is a potent and selective CD22 ligand with KD of 0.335, 30.7 µM for hCD22 and MAG, respectively. CD22 ligand-1 has the potential for the research of B-cell related disease.
|
-
- HY-150409
-
|
|
AUTACs
|
Cancer
|
|
TSPO ligand-2 is a ligand of AUTAC1. AUTAC1 contains an p-fluorobenzylguanine (FBnG) and a Fumagillol moiety, which can silence endogenous MetAP2 in HeLa cells.
|
-
- HY-128836
-
|
MDM2 Ligand 2; E3 ligase Ligand 15
|
Ligands for E3 Ligase
|
Cancer
|
|
(4R,5S)-Nutlin carboxylic acid (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-145990
-
|
MF6
|
FABP
|
Inflammation/Immunology
|
|
FABPs ligand 6 (MF6) is an FABP5 and FABP7 inhibitor with KD values of 874 nM and 20 nM, respectively. FABPs ligand 6 can be used for multiple sclerosis research.
|
-
- HY-151476
-
-
- HY-111823
-
|
VHL Ligand 6
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
|
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- HY-115729
-
-
- HY-132942A
-
-
- HY-139304
-
-
- HY-132942
-
-
- HY-138539
-
-
- HY-129967
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4 (IRAK4). PROTAC IRAK4 ligand-1 can be used in the synthesis of PROTAC IRAK4 degrader-1 (HY-129966).
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-
- HY-141486
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP.
|
-
- HY-147810
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7 receptor ligand 1 (Compound 5c) is a 5-HT7 receptor ligand with a Ki of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6.
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-
- HY-156499
-
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Others
|
Others
|
|
RNF114 ligand 1 is a E3 Ubiquitin ligase binder.
|
-
- HY-156793
-
|
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Others
|
Others
|
|
hRIO2 kinase ligand-1 (com 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM.
|
-
- HY-139660
-
-
- HY-145922
-
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Others
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Inflammation/Immunology
|
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ChemR23 ligand-1 is a chemical probe that contributes to the elucidation and analysis of the functions of ChemR23.
|
-
- HY-111845
-
-
- HY-111839
-
|
CRABP-II Ligand 1
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells.
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-
- HY-U00126
-
-
- HY-132970
-
|
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Histone Methyltransferase
|
Cancer
|
|
EED ligand 1 is a diverse, potent, and efficacious inhibitor that target the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.
|
-
- HY-126351
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
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- HY-151475
-
|
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Ligands for Target Protein for PROTAC
|
Cancer
|
|
GID4 Ligand 1 (compound 88) is a cell-permeable and high-selective GID4 binder (IC50=5.4 μM; Kd=5.6 μM), binds to GID4 in cells (EC50=558 nM). GID4 Ligand 1 can be used for the synthesis of PROTACs.
|
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- HY-115955
-
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Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor ligand-3 (compound 12C) is a potent D3 receptor ligand with a Ki of 3.6 nM. Dopamine D3 receptor ligand-3 have high selectivity for D3 over D2 (Ki=353 nM).
|
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- HY-101626A
-
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Sigma Receptor
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Neurological Disease
|
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Sigma-LIGAND-1 hydrochloride is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 hydrochloride has a Ki of 4000 nM at the dopamine D2 receptor.
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- HY-101626
-
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Sigma Receptor
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Neurological Disease
|
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Sigma-LIGAND-1 is a selective sigma receptor ligand with an IC50s of 16 nM, 19 nM at the DTG site and the PPP site, respectively. Sigma-LIGAND-1 has a Ki of 4000 nM at the dopamine D2 receptor.
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- HY-129939
-
-
- HY-115954
-
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Dopamine Receptor
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Neurological Disease
|
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Dopamine D3 receptor ligand-2 (compound 8) is a potent D3 receptor ligand with a Ki of 11.4 nM. Dopamine D3 receptor ligand-2 have high selectivity for D3 over D2 (Ki=1228 nM).
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- HY-111843
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- HY-115968
-
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Dopamine Receptor
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Neurological Disease
|
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Dopamine D3 receptor ligand-4 (compound 6) is a potent and selective dopamine D3 receptor ligand, with a Ki of 0.5 nM. Dopamine D3 receptor ligand-4 shows high level of selectivity for D3 over D2 (Ki=7.43 nM).
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- HY-130297
-
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Bcr-Abl
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Cancer
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PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.
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- HY-130270
-
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E3 Ligase Ligand-Linker Conjugates 57
|
E3 Ligase Ligand-Linker Conjugates
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Cancer
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AhR Ligand-Linker Conjugates 1 (E3 Ligase Ligand-Linker Conjugates 57) incorporates an IAP ligand for the E3 ubiquitin ligase, and a SNIPER linker. AhR Ligand-Linker Conjugates 1 can be used to design SNIPER.
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- HY-144983
-
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
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- HY-144980
-
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
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-
- HY-125906
-
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E3 Ligase Ligand-Linker Conjugates 56
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs.
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- HY-144985
-
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Ligands for E3 Ligase
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Cancer
|
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E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
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-
- HY-128822
-
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E3 ligase Ligand-Linker Conjugates 43
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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cIAP1 Ligand-Linker Conjugates 13 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 13 can be used to design SNIPERs.
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-
- HY-128813A
-
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E3 ligase Ligand-Linker Conjugates 34 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
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Cancer
|
|
cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs.
|
-
- HY-128815
-
|
E3 ligase Ligand-Linker Conjugates 36
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 14 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 14 can be used to design SNIPERs.
|
-
- HY-128816A
-
|
E3 ligase Ligand-Linker Conjugates 37 Hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 2 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 Hydrochloride can be used to design SNIPERs.
|
-
- HY-128820
-
|
E3 ligase Ligand-Linker Conjugates 41
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 1 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 1 can be used to design SNIPERs.
|
-
- HY-128819
-
|
E3 ligase Ligand-Linker Conjugates 40
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 3 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 3 can be used to design SNIPERs.
|
-
- HY-128826
-
|
E3 ligase Ligand-Linker Conjugates 47
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 10 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 10 can be used to design SNIPERs.
|
-
- HY-128812A
-
|
E3 ligase Ligand-Linker Conjugates 33 Hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 11 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 Hydrochloride can be used to design SNIPERs.
|
-
- HY-128813
-
|
E3 ligase Ligand-Linker Conjugates 34
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 15 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 can be used to design SNIPERs.
|
-
- HY-128824
-
|
E3 ligase Ligand-Linker Conjugates 45
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 9 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 9 can be used to design SNIPERs.
|
-
- HY-128812
-
|
E3 ligase Ligand-Linker Conjugates 33
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 11 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 can be used to design SNIPERs.
|
-
- HY-128817
-
|
E3 ligase Ligand-Linker Conjugates 38
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 12 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 12 can be used to design SNIPERs.
|
-
- HY-128825
-
|
E3 ligase Ligand-Linker Conjugates 46
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 8 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 8 can be used to design SNIPERs.
|
-
- HY-128823
-
|
E3 ligase Ligand-Linker Conjugates 44
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 7 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 7 can be used to design SNIPERs.
|
-
- HY-128818
-
|
E3 ligase Ligand-Linker Conjugates 39
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 5 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 5 can be used to design SNIPERs.
|
-
- HY-128821
-
|
E3 ligase Ligand-Linker Conjugates 42
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 4 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 4 can be used to design SNIPERs.
|
-
- HY-128816
-
|
E3 ligase Ligand-Linker Conjugates 37
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 2 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 can be used to design SNIPERs.
|
-
- HY-128814
-
|
E3 ligase Ligand-Linker Conjugates 35 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
cIAP1 Ligand-Linker Conjugates 6 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 6 hydrochloride can be used to design SNIPERs.
|
-
- HY-141486A
-
-
- HY-U00425
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50s of 0.04 and 2.8 μM for ERRα and ERRγ, respectively.
|
-
- HY-42424
-
|
VHL Ligand 2 hydrochloride; E3 ligase Ligand 1
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
|
-
- HY-42424A
-
|
VHL Ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
|
-
- HY-44012B
-
-
- HY-44012
-
-
- HY-44012A
-
-
- HY-130296
-
|
PROTAC CDK6 Ligand 1
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6. Palbociclib-propargyl 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-P1887
-
|
|
HSP
|
Infection
|
|
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ.
|
-
- HY-148179
-
-
- HY-P99133
-
-
- HY-44148
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
FAK ligand-Linker Conjugate 1 incorporates a ligand for FAK, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). FAK ligand-Linker Conjugate 1 can be extensively used for PROTAC-mediated protein degradation.
|
-
- HY-136306
-
|
|
Bacterial
|
Infection
|
|
Metallo-beta-lactamase ligand 1 is a class B β-lactamase inhibitor with antibacterial activity extracted from patent WO2019221122A1, compound A.
|
-
- HY-115729A
-
-
- HY-KT001
-
-
- HY-132943
-
-
- HY-P5889
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent.
|
-
- HY-139655
-
-
- HY-139707
-
-
- HY-112078
-
|
VHL Ligand 2; E3 ligase Ligand 1A
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
|
-
- HY-115446A
-
|
Cereblon Ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
|
-
- HY-130499
-
|
|
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.
|
-
- HY-P4205
-
|
|
Aminopeptidase
|
Cancer
|
|
Aminopeptidase N Ligand (CD13) NGR peptide is a polypeptide targeting CD13 and can be used as a carrier to mediate intracellular transmission. Aminopeptidase N Ligand (CD13) NGR peptide is often used in cancer research.
|
-
- HY-107439
-
|
Cereblon Ligand-Linker Conjugates 2; E3 Ligase Ligand-Linker Conjugates 20
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-107438
-
|
Cereblon Ligand-Linker Conjugates 6; E3 Ligase Ligand-Linker Conjugates 19
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-111824
-
|
VHL Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 29
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-112618
-
|
Cereblon Ligand-Linker Conjugates 11; E3 Ligase Ligand-Linker Conjugates 25
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C6-NH2 (Cereblon Ligand-Linker Conjugates 11), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-128716B
-
|
Cereblon Ligand-Linker Conjugates 5 hydrochloride; E3 ligase Ligand-Linker Conjugates 30 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 5) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-147225
-
|
|
AUTACs
Mitophagy
|
Cancer
Metabolic Disease
Neurological Disease
|
|
TSPO Ligand-Linker Conjugates 1 contains a ligand for translocator protein (TSPO) and a linker, which is used for the synthesis of mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC can bind the TSPO on the outer mitochondrial membrane (OMM) of mitochondria and degrades impaired mitochondria and proteins via mitophagy, and improves mitochondrial activity. TSPO Ligand-Linker Conjugates 1 can be used in mitochondrial dysfunction related research, including neurodegenerative diseases, cancer, and diabetes.
|
-
- HY-121867
-
-
- HY-111194
-
|
|
Others
|
Others
|
|
Ro 22-8515 is a ligand of Benzodiazepine receptor.
|
-
- HY-132943A
-
-
- HY-152538
-
|
|
G-quadruplex
|
Cancer
|
|
Antitumor agent-85 is a G-quadruplex (G4)-ligand with the ability to stabilize different G4-DNA structures. Antitumor agent-85 has highly effective anti-tumor properties.
|
-
- HY-103612
-
|
Cereblon Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 15
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-21930
-
|
Cereblon Ligand -Linker Conjugates 1; E3 Ligase Ligand-Linker Conjugates 1
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG4-C-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.
|
-
- HY-152537
-
|
|
G-quadruplex
|
Cancer
|
|
Antitumor agent-84 (compound 21a) is a G-quadruplex (G4)-ligand with the ability to stabilize different G4-DNA structures. Antitumor agent-84 has highly effective anti-tumor properties.
|
-
- HY-146077
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.
|
-
- HY-146076
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research.
|
-
- HY-129776
-
|
|
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
-
|
|
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-103614
-
|
Cereblon Ligand -Linker Conjugates 2 TFA; E3 Ligase Ligand-Linker Conjugates 20 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Thalidomide-O-amido-C8-NH2 TFA (Cereblon Ligand -Linker Conjugates 2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-103613
-
|
Cereblon Ligand-Linker Conjugates 6 TFA; E3 ligase Ligand-Linker Conjugates 19 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Thalidomide-O-amido-C4-NH2 TFA (Cereblon Ligand-Linker Conjugates 6 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130521
-
|
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-130822
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 4 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 4 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-130823
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 5 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 5 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-130991
-
|
|
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-130707
-
|
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 3 (Compound 001371) 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 3 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-112618A
-
|
Cereblon Ligand-Linker Conjugates 11 TFA; E3 Ligase Ligand-Linker Conjugates 25 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-107440
-
|
Cereblon Ligand-Linker Conjugates 3 ; E3 Ligase Ligand-Linker Conjugates 14
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-115560
-
|
Cereblon Ligand-Linker Conjugates 16; E3 Ligase Ligand-Linker Conjugates 52
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-128941
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
|
-
- HY-125845
-
|
VH032-NH2; VHL Ligand 1
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
|
-
- HY-41549
-
|
Cereblon Ligand-Linker Conjugates 9; E3 Ligase Ligand-Linker Conjugates 2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG4-Ph-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.
|
-
- HY-153990
-
|
|
FKBP
|
Neurological Disease
|
|
FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52.
|
-
- HY-129608
-
|
Cereblon Ligand-linker Conjugate
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-acetylene-C5-COOH can be connected to the ligand for protein by a linker to form PROTAC. Lenalidomide-acetylene-C5-COOH is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-128716
-
|
Cereblon Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 30
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG3-C2-NH2 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-112599
-
|
Cereblon Ligand-Linker Conjugates 8; E3 Ligase Ligand-Linker Conjugates 22
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG4-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.
|
-
- HY-148406
-
-
- HY-W584525
-
|
|
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-125884
-
|
Cereblon Ligand-Linker Conjugates 21; E3 Ligase Ligand-Linker Conjugates 54
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C4-amido-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-115560A
-
|
Cereblon Ligand-Linker Conjugates 16 TFA; E3 Ligase Ligand-Linker Conjugates 52 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-128846A
-
|
Cereblon Ligand-Linker Conjugates 15 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-120217
-
VH032
2 Publications Verification
|
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 Kdligand for protein by a linker to form PROTACs.
|
-
- HY-128846
-
|
Cereblon Ligand-Linker Conjugates 15
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.
|
-
- HY-153337A
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-C11-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155258
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-PEG7-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-PEG7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-101763A
-
|
VH032-NH2 monohydrochloride; VHL Ligand 1 monohydrochloride
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC (VH032-NH2) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
|
-
- HY-W007648
-
|
β-Alanine methyl ester hydrochloride
|
Others
|
Others
|
|
Methyl 3-aminopropanoate hydrochloride is prepared by esterification of Β-Alanine (I). Methyl 3-aminopropanoate hydrochloride can be used in the synthesis of bidentate pyridine-acid ligand.
|
-
- HY-125554
-
-
- HY-132856
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-amido-Boc is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-amido-Boc can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-128716A
-
|
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-130965B
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-PEG3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-PEG3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-110402
-
|
VH032-NH2 TFA; VHL Ligand 1 TFA
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC (VH032-NH2) TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
|
-
- HY-156159
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-156172
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-156161
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-156160
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-N0927
-
|
Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine
|
Dopamine Receptor
|
Others
|
|
(-)-Isocorypalmine (Tetrahydrocolumbamine), isolated from the crude base fraction of Corydalis chaerophylla, is a dopamine receptor ligand. Recombinant CYP719A21 displays strict substrate specificity and high affinity (Km=4.63 ± 0.71 μM) for (-)-Isocorypalmine.
|
-
- HY-156743
-
|
|
Others
|
Others
|
|
DCAF1 binder 2, a ligands for E3 Ligase, involves in BRD9, kinase and selective BTK degration.
|
-
- HY-155263
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C7-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155267
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C11-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-5-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155270
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C14-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155268
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C12-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-5-C12-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155265
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C9-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-5-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155266
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C10-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-5-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-P5072
-
|
|
Bombesin Receptor
|
Metabolic Disease
|
|
GRP (14-27) (human, porcine, canine) is a bombesin receptor ligand. The specific binding of GRP (14-27) is inhibited by GTP and GDP, whereas GMP was without effect.
|
-
- HY-125846
-
|
VH032-PEG1-OTs; VHL Ligand-Linker Conjugates 2; E3 ligase Ligand-Linker Conjugates 51
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-OTs is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.
|
-
- HY-W087383
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide 5-fluoride is Thalidomide-based cereblon ligand that incorporates to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.
|
-
- HY-155256
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-155255
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-PEG2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-148662
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-PEG5-C2-NH2 hydrochloride is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.Pomalidomide-PEG5-C2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155257
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-PEG7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-130979
-
-
- HY-W584528
-
|
|
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-W584527
-
|
|
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-149569
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C12-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C12-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149576
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C14-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-156170
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-NH-PEG5-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-NH-PEG5-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149566
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149561
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C4-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149567
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-156171
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-NH-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-NH-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149564
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149574
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C12-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C12-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149562
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C5-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C5-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149575
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-130949B
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-130963B
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149571
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C14-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149573
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C11-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149559
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149565
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C8-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C8-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149560
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149572
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149570
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149568
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C11-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-149563
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-C6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-125883
-
|
Cereblon Ligand-Linker Conjugates 20; E3 Ligase Ligand-Linker Conjugates 53
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C4-amido-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
|
-
- HY-112617A
-
|
Cereblon Ligand-Linker Conjugates 10 TFA; E3 Ligase Ligand-Linker Conjugates 24 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
Inflammation/Immunology
|
|
Thalidomide-O-amido-PEG2-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
|
-
- HY-103611
-
|
Cereblon Ligand-Linker Conjugates 3 TFA; E3 ligase Ligand-Linker Conjugates 14 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-133869
-
|
cGMP-HaloTag-Ligand
|
Autophagy
|
Cancer
|
|
cGMP-HTL contains a HT-ligand, a linker and the Cys-S-cGMP (autophagy tag). cGMP-HTL increases the K63-linked ubiquitination of mitochondria. AUTAC (autophagy-targeting chimera) is a novel targeted-clearance strategy that contains a degradation tag (guanine derivatives) and a warhead to provide target specificity.
|
-
- HY-130716
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C10-COOH (compound 6b) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based von Hippel-Lindau (VHL) ligand and a linker used in PROTAC technology.
|
-
- HY-155269
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C13-NH2 hydrochloride is a Pomalidomide (HY-10984)-based E3 ubiquitin ligase cereblon (CRBN) ligand for recruiting cereblon proteins. Pomalidomide-5-C13-NH2 hydrochloride can be connected to protein ligands through a linker to form PROTAC.
|
-
- HY-148834
-
-
- HY-114176
-
|
VH032-C4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 28
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
|
-
- HY-103604
-
|
VH032-PEG4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 4 hydrochloride; E3 ligase Ligand-Linker Conjugates 7
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
|
-
- HY-103602
-
|
VH032-PEG3-NH2 hydrochloride; VHL Ligand-Linker Conjugates 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 5
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-133486
-
-
- HY-134581A
-
|
M5049 hydrochloride
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research.
|
-
- HY-130271
-
|
VH032-PEG5-COOH; VHL Ligand-Linker Conjugates 16; E3 Ligase Ligand-Linker Conjugates 58
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology.
|
-
- HY-112600
-
|
Cereblon Ligand-Linker Conjugates 12; E3 Ligase Ligand-Linker Conjugates 23
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-P1868
-
|
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-128848
-
|
Cereblon Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 49
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-103602A
-
|
VH032-PEG3-NH2; VHL Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 5 Free Base
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-103604A
-
|
VH032-PEG4-NH2; VHL Ligand-Linker Conjugates 4 ; E3 ligase Ligand-Linker Conjugates 7 Free Base
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
|
-
- HY-W584534
-
|
|
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
-
|
|
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-138551A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-Me-C10-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC ligand, it can be used in PROTAC technology.
|
-
- HY-126458
-
|
E3 ligase Ligand-Linker Conjugates 32
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-PEG2-propargyl (E3 ligase Ligand-Linker Conjugates 32) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. Thalidomide-O-PEG2-propargyl 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-133189
-
|
|
PROTAC Linkers
|
Endocrinology
|
|
Bis-propargyl-PEG9 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG9 can be used to synthesize the bivalent estrogen receptor ligands. Bis-propargyl-PEG9 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-144456
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model.
|
-
- HY-W017424
-
|
|
Others
|
Others
|
|
Benzo[d]thiazol-2-amine is a favorable ligand to synthesize dinuclear complexes which contain nitrogen heterocycle.
|
-
- HY-W584531
-
|
|
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-W584529
-
|
|
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
-
|
|
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-W584533
-
|
|
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-148476
-
|
|
PROTACs
|
Others
|
|
Tri-GalNAc-DBCO can bind to the desialic acid glycoprotein receptor (ASGPR) to drive protein downregulation and target protein degradation, where GalNAc is a high-affinity ligand for hepatocyte-specific ASGPR.
|
-
- HY-123802
-
|
|
Integrin
|
Cancer
|
|
BIO7662 is a specific α4β1 antagonist. BIO7662 can be used to study α4β1 integrin-ligand interactions.
|
-
- HY-109176
-
|
GDC-9545; RG6171
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity.
|
-
- HY-W584532
-
|
|
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-P3136A
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV055 hydrochloride, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 hydrochloride is efficacious in stimulating cellular Gq-mediated signaling.
|
-
- HY-P3136
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV055, a G-protein-biased agonist, is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling.
|
-
- HY-P1868A
-
|
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-103603
-
|
VH032-PEG2-NH2 hydrochloride; VHL Ligand-Linker Conjugates 3 hydrochloride; E3 ligase Ligand-Linker Conjugates 6
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
|
-
- HY-103615
-
|
Cereblon Ligand-Linker Conjugates 4; E3 ligase Ligand-Linker Conjugates 18
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Thalidomide-O-amido-C4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-amido-C4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-N10634
-
|
C16 Glucosyl(β) Ceramide (d18:1/16:0)
|
Others
|
Inflammation/Immunology
|
|
D-Glucosyl-β-1,1′-N-palmitoylsphingosine (C16 Glucosyl(β) Ceramide (d18:1/16:0)) is an endogenous Mincle ligand possessing immunostimulatory activity.
|
-
- HY-112600A
-
|
Cereblon Ligand-Linker Conjugates 12 TFA; E3 Ligase Ligand-Linker Conjugates 23 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG1-(C1-PEG)2-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-W020035
-
|
|
GPR55
|
Neurological Disease
|
|
L-α-lysophosphatidylinositol Soy sodium is an endogenous ligand of GPR55. L-α-lysophosphatidylinositol Soy sodium is an endogenous lysophospholipid and endocannabinoid neurotransmitter that belongs to the class of lysophospholipids.
|
-
- HY-156726
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG4-C4-Cl (Intermediate 4d) is an E3 ligase ligand-linker conjugate containing a Pomalidomide (HY-10984) based cereblon (CRBN) ligand and a linker. Pomalidomide-amino-PEG4-C4-Cl can be used in the synthesis of PROTAC.
|
-
- HY-112617
-
-
- HY-144734
-
|
|
Others
|
Neurological Disease
|
|
Pantothenate kinase-IN-1 (Compound 1) is a pantothenate kinase (PANK) modulator with an IC50 of 0.51 µM against PANK3. Pantothenate kinase-IN-1 has a reasonable ligand efficiency (LipE = 2.8).
|
-
- HY-142952
-
-
- HY-136424
-
|
GM1485
|
Others
|
Neurological Disease
|
|
GPI-1485 (GM1485), a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke.
|
-
- HY-103603A
-
|
VH032-PEG2-NH2 ; VHL Ligand-Linker Conjugates 3 ; E3 ligase Ligand-Linker Conjugates 6 Free Base
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
|
-
- HY-N8641
-
-
- HY-128839
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
|
-
- HY-P3137
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-150202
-
|
|
Others
|
Others
|
|
L1-PEG2-TATE is a nonadentate ligand. L1-PEG2-TATE can be used for the research of imaging.
|
-
- HY-P1438
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide S (Rat) is an endogenous ligand of a previously orphan G-protein-coupled receptor now named NPS receptor. Neuropeptide S (Rat) can be used for the research of nervous system disease.
|
-
- HY-119782
-
|
|
Fluorescent Dye
|
Others
|
|
L-Argininamide is a hydrophilic amino acid derivative and can be used as a compound for ligand binding DNA aptamers. L-Argininamide has the potential for fluorescent aptasensors development.
|
-
- HY-147192
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-O-PEG1-propargyl (Compound 10b) is an E3 ligand for the synthesis of PROTAC. (S,R,S)-AHPC-O-PEG1-propargyl is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-148650
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin. Neurotensin is a sortilin ligand. Sortilin antagonist 1 can be used for the research of neurological disease.
|
-
- HY-148665
-
|
|
FABP
|
Others
|
|
FABP-IN-2 is a novel FABP3 ligand. FABP-IN-2 inhibits FABP3/FABP4 with an IC50 of 1.16 μM and 4.27 μM respectively.
|
-
- HY-138550A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-3-methylbutanyl acetate-methanesulfonothioate-PEG3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-122136
-
|
|
Melatonin Receptor
|
Neurological Disease
|
|
S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist.
|
-
- HY-150879
-
-
- HY-135903
-
|
GDC-9545 tartrate; RG6171 tartrate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Giredestrant tartrate (GDC-9545 tartrate), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant tartrate potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Anti-tumor activity.
|
-
- HY-145368
-
|
|
LYTACs
|
Others
|
|
Tri-GalNAc-NHS ester is a LYsosome TArgeting Chimera (LYTAC) and a ligand of asialoglycoprotein receptor (ASGPR). ASGPR is a lysosomal targeting receptor specifically expressed on liver cells, for the degradation of extracellular proteins including membrane proteins. Tri-GalNAc-NHS ester can be used as a protein degrader and it can be used for the research of LYTAC.
|
-
- HY-142954
-
-
- HY-114872
-
-
- HY-148070
-
|
|
FLT3
FAK
Cytochrome P450
|
Cancer
|
|
FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers.
|
-
- HY-145177
-
|
|
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-P99056
-
|
PF 05082566
|
TNF Receptor
|
Cancer
Inflammation/Immunology
|
|
Utomilumab (PF 05082566) is a fully human IgG2 mAb agonist of the T-cell costimulatory receptor 4-1BB/CD137. Utomilumab can be used for the research of relapsed/refractory follicular lymphoma (FL) and other CD20 + non-Hodgkin lymphomas (NHL).
|
-
- HY-103246
-
|
|
Androgen Receptor
|
Cancer
|
|
TFM-4AS-1 is a selective androgen receptor modulator (SARM). TFM-4AS-1 is a potent androgen receptor (AR) ligand with an IC50 of 38 nm. TFM-4AS-1 is also a gene-selective agonist.
|
-
- HY-134761
-
|
|
c-Myc
|
Cancer
|
|
EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis.
|
-
- HY-114872A
-
-
- HY-142953
-
-
- HY-126534
-
-
- HY-149935
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can enable the development of DCAF1-based PROTACs.
|
-
- HY-138965A
-
-
- HY-147559
-
|
|
Cannabinoid Receptor
|
Others
|
|
CB1R Allosteric modulator 2 (compound 18) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 2 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
|
-
- HY-147558
-
|
|
Cannabinoid Receptor
|
Others
|
|
CB1R Allosteric modulator 1 (compound 11) is a potent CB1R allosteric modulator. CB1R Allosteric modulator 1 shows negatively affects the functional activity of orthosteric ligands (NAM) at CB1Rs.
|
-
- HY-119102
-
|
|
HCN Channel
|
Inflammation/Immunology
|
|
BPU-11 is a hyperpolarization-activated cyclic nucleotide-gated (HCN) C-linker pocket (CLP) HCN4 CLP ligand. BPU-11 can be used for the research of congenital immune disease.
|
-
- HY-120842
-
|
|
mAChR
|
Neurological Disease
|
|
RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [ 3H](+)-pentazocine with a Ki of 50 pM.
|
-
- HY-130982
-
|
|
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-118438
-
|
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations.
|
-
- HY-150235
-
|
|
Galectin
|
Inflammation/Immunology
|
|
Galectin-8N-IN-1 (compound 19a) is a potent and selective galectin-8N inhibitor with a Kd value of 1.8 μM. Galectin-8N-IN-1 is a galectin-8N ligand. Galectin-8N-IN-1 can be used in research of immune system.
|
-
- HY-103599
-
|
VH032-PEG2-N3; VHL Ligand-Linker Conjugates 6; E3 ligase Ligand-Linker Conjugates 13
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-103601
-
|
VH032-PEG4-N3; VHL Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 4
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
(S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-103600
-
|
VH032-PEG1-N3; VHL Ligand-Linker Conjugates 9; E3 ligase Ligand-Linker Conjugates 3
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-103598
-
|
VH032-PEG3-N3; VHL Ligand-Linker Conjugates 8; E3 ligase Ligand-Linker Conjugates 12
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG3-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG3-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-130798
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180).
|
-
- HY-128832
-
|
MDM2 Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 48
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Nutlin-C1-amido-PEG4-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Nutlin 3 based MDM2 ligand and 4-unit PEG linker used in PROTAC technology. Nutlin-C1-amido-PEG4-C2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-P2159
-
|
|
Opioid Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- HY-W584514
-
|
|
SHP2
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN proteins. Thalidomide-NH-(CH2)2-NH2 TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules designed to synthesize small PROTAC molecules targeting SHP2 protein.
|
-
- HY-148340
-
|
|
Others
|
Others
|
|
24RBPyBC is a dinucleating macrocyclic ligand, it contains phenolate pyridine, bipyridine, and amino groups form dinuclear Fe(II) and Fe(III) complexes.
|
-
- HY-125843
-
|
Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG1-C2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology. Pomalidomide-PEG1-C2-N3 can be used to design a selective CDK6 PROTAC degrader CP-10. CP-10 induces the degradation of CDK6 with an DC50 of 2.1 nM. Pomalidomide-PEG1-C2-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-130813
-
-
- HY-103606
-
|
VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG6-C4-Cl is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG6-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-109149
-
|
KP 106
|
Others
|
Neurological Disease
|
|
Lomardexamfetamine (KP 106) is an orally active central nervous system stimulant composed of d-amphetamine and a ligand. Lomardexamfetamine can be used for the research of attention-deficit hyperactivity disorder.
|
-
- HY-123109
-
|
VH032-Boc
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology.
|
-
- HY-P1483
-
-
- HY-P1483B
-
|
|
Urotensin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
Urotensin II, mouse acetate is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse acetate is a potent vasoconstrictor. Urotensin II, mouse acetate plays a physiological role in the central nervous system.
|
-
- HY-141495A
-
|
(-)-PW0464
|
Dopamine Receptor
|
Neurological Disease
|
|
Razpipadon ((-)-PW0464), an aromatic compound, is a dopamine receptor partial agonist. Razpipadon can be used in the study of dopamine D1 ligand-mediated related psychiatric disorders.
|
-
- HY-P99021
-
|
LY 2951742
|
CGRP Receptor
|
Neurological Disease
|
|
Galcanezumab (LY 2951742) is a humanized IgG4 monoclonal antibody against the CGRP ligand. Galcanezumab can be used for migraine or cluster headaches research.
|
-
- HY-W584513
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-(CH2)2-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)2-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)2-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-107686
-
|
5-I A-85380 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
5-Iodo-A-85380 dihydrochloride is a selective ligand of nAChR. 5-Iodo-A-85380 dihydrochloride binds to α4β2 nAChRs in rat and human brain with Kds of 12 and 14 pM,respectively.
|
-
- HY-W229874
-
|
|
Others
|
Cancer
|
|
EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1.
|
-
- HY-P1483A
-
|
|
Urotensin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
Urotensin II, mouse TFA is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse TFA is a potent vasoconstrictor. Urotensin II, mouse TFA plays a physiological role in the central nervous system.
|
-
- HY-103607
-
|
VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-D1605
-
|
|
Fluorescent Dye
|
Others
|
|
BODIPY FL L-Cystine is a thiol-reactive, green-fluorescent dye. BODIPY FL L-Cystine can be the labeling of membrane proteins, proteins with hydrophobic binding sites, or hydrophobic ligands. (λex=504 nm, λem=511 nm).
|
-
- HY-148680
-
|
|
STING
|
Cancer
|
|
CL845-PAB-Ala-Val-C5-MC is a conjugatable STING ligand， it is synthesized from the proprietary cyclic dinuleotide HY-148679 CL845. CL845-PAB-Ala-Val-C5-MC can be used for bioconjugation.
|
-
- HY-133799
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C7-COOH is a synthesized E3 ligase cereblon ligand-linker conjugate. Pomalidomide-C7-COOH is an intermediate for the synthesis of PROTAC BCL-XL degraders.
|
-
- HY-W584515
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.
|
-
- HY-W584520
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-NH-PEG1-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-4-NH-PEG1-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-150029
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CB1/2 agonist 3 (compound 52), a potent non-selective cannabinoid ligand, is a CB1/CB2 (cannabinoid receptor) competitive agonist. CB1/2 agonist 3 acts on hCB1 and hCB2 with Ki values of 5.9 nM and 3.5 nM, respectively.
|
-
- HY-150734
-
|
|
Toll-like Receptor (TLR)
|
Infection
Inflammation/Immunology
|
|
ODN 2007, a class B CpG ODN (oligodeoxynucleotide), is a Toll-like receptor (TLR) ligand. ODN 2007 can be used as an immunomodulator, vaccine adjuvant, and enhance immune responses in mammals, fish, and humans. ODN 2007 sequence: 5'-TCGTCGTTGTCGTTTTGTCGTT-3'.
|
-
- HY-W584522
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-NH-PEG1-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG1-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-W584524
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-NH-PEG2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-W584516
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-NH-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-NH-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-NH-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-W584517
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-O-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-139516
-
|
AZ13040214; NAV4614
|
Amyloid-β
|
Others
|
|
AZD4694 Precursor (AZ13040214) is the precursor of [ 18F] AZD4694 for the synthesis of [ 18F] AZD4694, an amyloid-β imaging ligand with high affinity for amyloid-β plaques.
|
-
- HY-152152
-
|
|
MAGL
|
Neurological Disease
|
|
JZP-MA-13 is a selective α/β-hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 392 nM. JZP-MA-13 shows no inhibition of MAGL, ABHD12, FAAH, or other serine hydrolases. JZP-MA-13 is a positron emission tomography (PET) ligand for in vivo imaging of the ABHD6.
|
-
- HY-P10052
-
|
|
VEGFR
|
Cancer
|
|
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. CBO-P11 is modified with a nearinfrared cyanine dye bearing an alkyne function, allowing both “click” coupling on azido-modified nanoparticles and fluorescence labelling.
|
-
- HY-131028
-
|
JF646 TFA
|
Fluorescent Dye
|
Others
|
|
Janelia Fluor® 646 TFA (JF646 TFA), a red fluorogenic fluorescent dye, can be used in the synthesis of Janelia Fluor 646 HaloTag and SNAP-Tag ligands. JF646 TFA is used in live cell imaging experiments. Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
|
-
- HY-149933
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility.
|
-
- HY-131961
-
|
|
VD/VDR
HDAC
|
Cancer
|
|
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
|
-
- HY-D0020
-
|
|
Biochemical Assay Reagents
|
Infection
Endocrinology
|
|
2,2'-Bipyridine is the unique molecular scaffold of the bioactive natural products. 2,2'-Bipyridine is extensively used as the core structure of many chelating ligands by acting as a bridge in the arrangement of the catalytic center. 2,2'-Bipyridine shows robust redox stability and hyperglycemic activity.
|
-
- HY-148679
-
|
|
STING
|
Cancer
Infection
Inflammation/Immunology
|
|
CL845 is an analog of the STING agonist CL656 (HY-112878). CL845 can be used to synthesize conjugatable PRR ligands that target STING (stimulator of interferon genes). CL845 can be usexd for the research of cancers, immunological disorders or infections.
|
-
- HY-145419
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α.
|
-
- HY-145420
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α.
|
-
- HY-145418
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α.
|
-
- HY-139403
-
|
|
Target Protein Ligand-Linker Conjugates
Ras
|
Cancer
|
|
MRTX849 ethoxypropanoic acid incorporates a ligand for KRAS G12C, and a PROTAC linker. MRTX849 ethoxypropanoic acid can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC 50s between 0.25 and 0.76 μM).
|
-
- HY-136363
-
|
|
TRP Channel
|
Neurological Disease
|
|
MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
|
-
- HY-103608
-
|
VHL Ligand-Linker Conjugates 11; E3 ligase Ligand-Linker Conjugates 11
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-PEG)2-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-136277
-
|
|
Fluorescent Dye
|
Others
|
|
DFHO is a fluorogenic ligand of Corn fluorogenic aptamer. The RNA aptamer, Corn binds DFHO with a Kd value of 70 nM and converts it to a fluorescent form, enabling RNA imaging in cells.
|
-
- HY-112210
-
|
Shld1
|
FKBP
|
Others
|
|
Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD).
|
-
- HY-145399
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan is a conjugate used to synthesis ADC. Mal-PEG8-amide-Val-Ala-(4-NH2)-Exatecan comprises topoisomerase inhibitor derivative with a linker for connecting to a ligand unit (extracted from patent US20200306243A1).
|
-
- HY-108355
-
|
|
PKC
|
Cancer
|
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
|
-
- HY-101178
-
|
|
iGluR
|
Neurological Disease
|
|
L-689560 is a potent N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. L-689560 is widely used as a radiolabeled ligand in binding studies and used for study the roles of NMDA receptors in normal neurological processes as well as in diseases.
|
-
- HY-134592
-
-
- HY-151387
-
|
|
Others
|
Neurological Disease
|
|
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases.
|
-
- HY-113884B
-
|
13(S)-HODE
|
PPAR
Mitochondrial Metabolism
|
Cancer
Inflammation/Immunology
|
|
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury.
|
-
- HY-123109A
-
|
(S,S,S)-VH032-Boc
|
Others
|
Cancer
|
|
(S,S,S)-AHPC-Boc is the inactive isomer of (S,R,S)-AHPC-Boc (HY-123109), and can be used as an experimental control. (S,R,S)-AHPC-Boc (VH032-Boc) is a ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Boc is used in PROTAC technology.
|
-
- HY-151107
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC50 and a Ki of 960 nM and 970 nM, respectively. CBR Agonist-2 is a promising tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system.
|
-
- HY-103605
-
|
VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-131295
-
|
|
MEK
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
|
-
- HY-133036
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
|
-
- HY-135236
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity.
|
-
- HY-42771
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-O-CH2-COO(t-Bu) is t-Bu modified Thalidomide (HY-14658), which is the final step intermediate in the synthesis of Thalidomide-4-OH (HY-123096). Thalidomide-4-O-CH2-COO(t-Bu) acts as a Cereblon ligand to recruit CRBN proteins. The t-Bu protecting group at the end of Thalidomide-4-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules.
|
-
- HY-113330
-
|
12(S)-HHTrE
|
Leukotriene Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenous ligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity.
|
-
- HY-A0003C
-
|
CC-5013 sodium
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide (sodium), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (sodium) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (sodium) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-P1318
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-144712
-
|
|
G-quadruplex
Apoptosis
|
Cancer
|
|
L5-DA is a G-quadruplex (G4) ligand and selectively stabilized for G4s over ds26. L5-DA exhibits significant cytotoxicity against HeLa cells (IC50=4.3 μM). L5-DA stabilizes G4s in HeLa cells, induces apoptosis, and cell cycle arrest.
|
-
- HY-P1318A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-16785
-
|
INXN-1001; RG-115932
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys.
|
-
- HY-148681
-
|
|
STING
|
Cancer
|
|
CL845-PAB-Ala-Val-PEG4-Azide is a conjugatable STING ligand， it is synthesized from the proprietary cyclic dinuleotide HY-148679 CL845. CL845-PAB-Ala-Val-PEG4-Azide can be used for bioconjugation. CL845-PAB-Ala-Val-PEG4-Azide is a click chemistry reagent, itcontains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-142521
-
|
|
Leukotriene Receptor
|
Metabolic Disease
|
|
BLT2 probe 1 (compound 13) is a fluorescent probe based on the synthetic BLT2 agonist CAY10583. BLT2 is a promising target for diabetic wound healing and gastrointestinal lesions. BLT2 probe 1 is suitable to investigate the pharmacology of BLT2 receptor ligands in a variety of assay systems.
|
-
- HY-103076
-
EZ-482
1 Publications Verification
|
Others
|
Neurological Disease
|
|
EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas.
|
-
- HY-114091
-
|
|
MMP
|
Inflammation/Immunology
|
|
PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively.
|
-
- HY-150028
-
|
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand, with Ki values of 3.5 and 1.2 nM, respectively. CB1/2 agonist 2 can behave as a full CB1 agonist and CB2 competitive inverse agonist. CB1/2 agonist 2 shows antinociceptive activity.
|
-
- HY-115531
-
|
|
Others
|
Cancer
|
|
UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB).
|
-
- HY-75706
-
|
|
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-151801
-
|
|
mAChR
|
Others
|
|
DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart.
|
-
- HY-113962
-
|
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
|
-
- HY-U00228
-
-
- HY-136772
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Others
|
|
Pomalidomide-PEG1-NH2 hydrochloride is a crosslinker-E3 ligase ligand conjugate, consisting of an E3 ligase ligand pomalidomide and a PEGylated crosslinker with terminal amine for reactivity with a carboxyl group on the target ligand.
|
-
- HY-153806
-
|
ZZY05-092
|
FKBP
|
Cancer
|
|
RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand.
|
-
- HY-132944
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(R)-Pomalidomide-pyrrolidine, a CRBN ligand, can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-A0003B
-
|
CC-5013 hemihydrate
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
|
|
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-A0003
-
|
CC-5013
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-A0003A
-
|
CC-5013 hydrochloride
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
Inflammation/Immunology
|
|
Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
|
-
- HY-148152
-
|
|
PSMA
|
Others
|
|
PSMA I&S is a precursor of the 99mTc-labeled PSMA-targeting ligand.
|
-
- HY-120953
-
-
- HY-151792
-
|
|
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-114434
-
AP1867
1 Publications Verification
|
FKBP
|
Cancer
|
|
AP1867 is a synthetic FKBP12 F36V-directed ligand.
|
-
- HY-148152A
-
|
|
PSMA
|
Others
|
|
PSMA I&S (TFA) is a precursor of the 99mTc-labeled PSMA-targeting ligand.
|
-
- HY-124211
-
-
- HY-130952
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-111841
-
|
|
SNIPERs
PROTACs
|
Cancer
|
|
PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
|
-
- HY-111842
-
|
|
SNIPERs
PROTACs
|
Cancer
|
|
PROTAC CRABP-II Degrader-3 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
|
-
- HY-113534
-
|
|
IAP
Apoptosis
|
Cancer
|
|
MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
|
-
- HY-111840
-
|
|
SNIPERs
PROTACs
|
Cancer
|
|
PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on IAP ligand.
|
-
- HY-66007
-
-
- HY-133484B
-
-
- HY-136272
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
A 410099.1 amide-PEG3-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG3-amine-Boc can conjugates with target protein ligands.
|
-
- HY-136273
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
A 410099.1 amide-PEG2-amine-Boc is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-PEG3 linker with terminal amine. A 410099.1 amide-PEG2-amine-Boc can conjugates with target protein ligands.
|
-
- HY-136274
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Boc-A 410099.1 amide-alkylC4-amine is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-alkylC4 linker with terminal amine. Boc-A 410099.1 amide-alkylC4-amine can conjugates with target protein ligands.
|
-
- HY-148142
-
-
- HY-17360
-
|
BA679 BR
|
mAChR
|
Neurological Disease
|
|
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-148143
-
-
- HY-151716
-
|
|
ADC Linker
|
Others
|
|
Halo-DBCO is a click chemistry reagent containing dibenzocyclooctyne (DBCO). Halo-DBCO can be used as a ligand to react with HaloTag to form covalent HaloTag ligand couples.
|
-
- HY-139345
-
-
- HY-139549
-
|
|
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.
|
-
- HY-130295
-
-
- HY-138783
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-Piperidine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-P4715
-
|
|
PTHR
|
Endocrinology
|
|
(Tyr36)-pTH-Related Protein (1-36) (human, mouse, rat) is a peptide and can be used as a parathyroid hormone (PTH) receptor ligand.
|
-
- HY-120665
-
-
- HY-N1427A
-
-
- HY-104046
-
|
|
Others
|
Others
|
|
Octaaminocryptand 1 is an aminocryptand ligand.
|
-
- HY-141010
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-PEG4-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-141014
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-PEG4-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131185
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-134983
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine 5-fluoride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-D1027
-
|
Monodansyl cadaverine
|
Autophagy
|
Others
|
|
Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands.
|
-
- HY-138792
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Glutarimide-Isoindolinone-NH-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates a cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138783A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-Piperidine hydrochloride is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-Piperazine-Piperidine hydrochloride incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138773
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131874
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C7-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138790
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Glutarimide-Isoindolinone-NH-PEG4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates a cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138775
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138774
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131876
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C3-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138860
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C11-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131880
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C2-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131889
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138791
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Glutarimide-Isoindolinone-NH-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates a cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138771
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138782
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG1-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138780
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-141010A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-PEG4-amine hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130950
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138772
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130951
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C6-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-141887
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C6-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138781
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138784
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130965
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138784A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131888A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-141010B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-PEG4-amine TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-W076696
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-4-OH is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-OH can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-138845A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130964B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-136164
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032-OH is the VH032-based VHL ligand. VH032-OH can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-133484
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138845
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131888
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-113413
-
-
- HY-112797
-
-
- HY-133816A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-136162A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide 4'-ether-alkylC2-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-133485B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-139539
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-COOH can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-138847
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-133817
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130949
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C7-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138858A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-amido-PEG2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-134986
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138848A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-133817A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130948
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138787
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-133816
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138859
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131867
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138789
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138848
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-23095
-
|
|
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.
|
-
- HY-138846A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130708
-
UNC6852
2 Publications Verification
|
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-138858
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-amido-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-136237
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130963
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C10-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138847A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-129704B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-135250
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-117992
-
|
|
Complement System
|
Others
|
|
BR103 is a C3aR-specific small molecule ligand. BR103 can be used to measure ligand affinity for a G protein-coupled receptor for saturation and competitive binding.
|
-
- HY-138846
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-133485
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-134985
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-129704
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-136162
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide 4'-ether-alkylC2-amine hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138788
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-139547
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-103634
-
|
|
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-138859A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amino-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-W077589A
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-134985A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG1-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138853
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138882
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-4-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-138789A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG1-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138849A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138882A
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-4-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
|
-
- HY-111879
-
|
|
SNIPERs
|
Cancer
|
|
Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
|
-
- HY-W077589
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-5-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
|
-
- HY-129704A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C6-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-134984A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-134984
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138850A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131388
-
-
- HY-138850
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138881
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-6-F is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-6-F can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-W072954
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-5-Br is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-Br can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-138851
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131998
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG4-Ms is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739.
|
-
- HY-138852
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-136161
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 6-unit PEG linker used in PROTAC technology.
|
-
- HY-130639
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-NH-Boc (compound 15) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138853A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C8-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138851A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C5-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-141423
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amide-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138849
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-139540
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
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.
|
-
- HY-138852A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138788A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Piperazine-PEG2-NH2 diTFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-111878
-
|
|
SNIPERs
|
Cancer
|
|
BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
|
-
- HY-138786
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-5-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-107438A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C4-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-17360S
-
|
BA679 BR-d3
|
mAChR
|
Neurological Disease
|
|
Tiotropium-d3 (bromide) is the deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-126583
-
|
|
Calcium Channel
|
Cancer
|
|
Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca 2+ channel. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand.
|
-
- HY-136166
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-130948B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
|
|
Thalidomide-O-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-107439A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C8-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-17360S1
-
|
BA679 BR-d6
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Tiotropium-d6 (bromide) is deuterium labeled Tiotropium (Bromide). Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
|
-
- HY-136156
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG6-butyl iodide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 6-unit PEG linker used in PROTAC technology.
|
-
- HY-112618B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C6-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-W093272
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5,6-F is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-F can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-122694
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138786A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-5-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-141423A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amide-C5-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138785A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-5-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138785
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-5-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-122694A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-114420
-
-
- HY-15238
-
-
- HY-P99575
-
|
AMG-757
|
Notch
|
Cancer
Inflammation/Immunology
|
|
Tarlatamab (AMG-757) is a bispecific T-cell engager (BiTE) antibody targeting delta-like ligand 3 (DLL3). DLL3 is a target that is selectively expressed in small-cell lung cancer (SCLC) tumors, but with minimal normal tissue expression. Tarlatamab has the KDs of 0.64 nM and 0.50 nM for human and nonhuman primate (NHP) DLL3, respectively. Tarlatamab has the KDs of 14.9 nM and 12 nM for human and NHP CD3, respectively. Tarlatamab is a first-in-class HLE BiTE immuno-oncology therapy targeting DLL3 and has the potential for SCLC research.
|
-
- HY-138862
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-136163A
-
-
- HY-131159
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-O-C8-Boc is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-Boc can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-138856A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG3-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-130981
-
-
- HY-138856
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG3-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138854A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-112599B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in the synthesis of PROTACs..
|
-
- HY-138855A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-122710
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG4-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-136183
-
|
VH032 phenol-alkylC6-amine dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-phenol-alkylC6-amine dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and an alkyl linker used for PROTAC degrader.
|
-
- HY-137531
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG1-C2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 1-unit PEG linker used in PROTAC technology.
|
-
- HY-123324
-
|
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.
|
-
- HY-138854
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG1-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138855
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138857A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-138857
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-amido-PEG4-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-131308
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C2-PEG3-OH is an E3 ligase ligand-linker conjugate that incorporates Thalidomide based cereblon ligand and a linker used for PROTAC BCL-XL degrader XZ739.
|
-
- HY-123215
-
|
7-Hydroxy pomalidomide; Pomalidomide metabolite M16
|
Ligands for E3 Ligase
|
Cancer
|
|
CC-17369 (7-Hydroxy pomalidomide) is a metabolite of Pomalidomide. CC-17369 is the Pomalidomide -based cereblon (CRBN) ligand used in the recruitment of CRBN protein. CC-17369 can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-139546
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-propargyne-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-propargyne-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-114176B
-
|
VH032-C4-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C4-NH2 dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
|
-
- HY-133144
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
|
-
- HY-122710A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-138861A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-114176A
-
|
VH032-C4-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC.
|
-
- HY-138861
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-129703B
-
|
Thalidomide-NH-PEG2-C2-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG2-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
|
-
- HY-139541
-
|
|
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.
|
-
- HY-136165
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG3-propionic acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-153337
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-C11-NH2 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-C11-NH2 can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-129703
-
|
Thalidomide-NH-PEG2-C2-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
|
-
- HY-156111
-
|
|
Androgen Receptor
PROTACs
|
Cancer
|
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models.
|
-
- HY-130988A
-
|
GDC-0068-NH2 dihydrochloride; RG7440-NH2 dihydrochloride
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Ipatasertib-NH2 dihydrochloride 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-139542
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
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.
|
-
- HY-100583
-
-
- HY-75035
-
-
- HY-W011051
-
-
- HY-P0183
-
-
- HY-131959
-
-
- HY-131872
-
|
Pomalidomide 4'-PEG2-acid
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG2-COOH (Pomalidomide 4'-PEG2-acid) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
|
-
- HY-122825
-
|
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-110 consists of a IAP ligand and an estrogen ligand, connected by a linker. SNIPER(ER)-51 induces estrogen receptor (ER) protein degradation with DC50s of <3 nM and 7.7 nM after 4 h and 48 h, respectively.
|
-
- HY-131912
-
-
- HY-110392
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
|
-
- HY-129703A
-
|
Thalidomide-NH-PEG2-C2-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG2-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
|
-
- HY-131318
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
|
-
- HY-139543
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
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.
|
-
- HY-130648
-
-
- HY-107440A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-111663
-
-
- HY-106547
-
-
- HY-152270
-
-
- HY-15265
-
|
|
VD/VDR
|
Cancer
|
|
Impurity F of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
|
-
- HY-131717
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
|
-
- HY-130269
-
|
β-NF-CH2-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
|
-
- HY-122725B
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader.
|
-
- HY-131190
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
N-Boc-SBP-0636457-OH is a synthesized E3 ligase ligand-linker conjugate that incorporates IAP ligand and a linker. N-Boc-SBP-0636457-OH can be used to design a PROTAC Bcl-xL degrader-1 (HY-131188).
|
-
- HY-N2388
-
|
|
MMP
|
Inflammation/Immunology
Cancer
|
|
Auraptene is the most abundant naturally occurring geranyloxycoumarin. Auraptene decreases the secretion of matrix metalloproteinase 2 (MMP-2) as well as key inflammatory mediators, including IL-6, IL-8, and chemokine (C-C motif) ligand-5(CCL5).
|
-
- HY-130737
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-alkylC5-acid (Example 3) is an E3 ligase ligand-linker conjugate containing a Pomalidomide (HY-10984) based cereblon (CRBN) ligand and a linker. Pomalidomide 4'-alkylC5-acid can be used in the synthesis of PROTAC.
|
-
- HY-131646
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-C3-PEG3-C1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-43722
-
|
|
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-122725A
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs, such as MDM2 PROTAC degrader.
|
-
- HY-100486
-
BTTAA
1 Publications Verification
|
Others
|
Others
|
|
BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
|
-
- HY-114229
-
-
- HY-W129872
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-CH2-NH2 (hydrochloride) is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-CH2-NH2 (hydrochloride) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-132288
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pom-8PEG, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and an 8-unit PEG linker. Pom-8PEG can be used in the synthesis of PROTAC, such as IDO1 PROTAC degrader.
|
-
- HY-131647
-
|
Pomalidomide-PEG5-CO2H
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-PEG5-acid (Pomalidomide-PEG5-CO2H) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 5-unit PEG linker used in PROTAC technology.
|
-
- HY-139545
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-4-C3-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-P1380A
-
|
|
Apoptosis
|
Cancer
|
|
Difopein (TFA), a specific and competitive inhibitor of 14-3-3 protein (a highly conserved eukaryotic regulatory molecule), blocking the ability of 14-3-3 to bind to target proteins and inhibits 14-3-3/Ligand interactions. Difopein (TFA) leads to induction of apoptosis and enhances the ability of cisplatin to kill cells.
|
-
- HY-D1643
-
|
|
Biochemical Assay Reagents
|
Others
|
|
5,5'-Dinitro BAPTA AM is a membrane-permeant, high-affinity calcium chelator, it can be used for investigation of the role of cytosolic Ca 2+. 5,5'-Dinitro BAPTA AM can be loaded by incubation into live cells, and is cleaved by cytosolic esterases to liberate the active tetra-carboxylate ligand.
|
-
- HY-156568A
-
|
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models.
|
-
- HY-131189
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
N-Boc-SBP-0636457-OH, a ligand for E3 ubiquitin ligase, is used in the recruitment of IAP E3 ligases. N-Boc-SBP-0636457-OH can be connected to the ligand for Bcl-xL by a linker to form PROTAC Bcl-xL degrader-1 (HY-131188).
|
-
- HY-130849
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-C5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C5-COOH can be used in PROTAC DT2216 (HY-130604).
|
-
- HY-131186
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C3-piperazine-N-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in the synthesis of PROTAC PD-1/PD-L1 degrader-1 (HY-131183).
|
-
- HY-133699
-
|
|
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-143499
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-3 (Compound 15) is a potent inhibitor of hMAO-B with an IC50 of 47.4 nM. hMAO-B-IN-3 is playing favourable agent-like properties and a broad safety window. hMAO-B-IN-3 is thus a suitable candidate for lead optimization and the development of multitarget-directed ligands.
|
-
- HY-101909
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAF is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAF contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF (HY-15579)
|
-
- HY-P1205A
-
|
Melanin-concentrating hormone(human, mouse, rat) TFA
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively.
|
-
- HY-135572
-
|
|
Others
|
Cancer
Neurological Disease
|
|
TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity.
|
-
- HY-44177
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Cit-PAB-MMAF sodium is a agent-linker conjugate for ADC. Val-Cit-PAB-MMAF sodium contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin polymerization inhibitor MMAF (HY-15579)
|
-
- HY-110399
-
-
- HY-A0266
-
-
- HY-P99723
-
|
BCD-135
|
PD-1/PD-L1
|
Cancer
|
|
Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 (PD-L1).
|
-
- HY-116677
-
|
TBTA
|
Others
|
Others
|
|
Tris(benzyltriazolylmethyl)amine (TBTA) is a ligand that acts as a biochemical tool for the tagging of proteins and enzymes.
|
-
- HY-N3171A
-
|
Wikstromol
|
Apoptosis
PI3K
|
Cancer
|
|
(+)-Nortrachelogenin (Wikstromol), a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity.
|
-
- HY-136006B
-
|
VH032-C6-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C6-NH2 (VH032-C6-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-136186
-
|
VH032-C7-amine
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
|
-
- HY-126457
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs. Thalidomide-propargyl 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-130711B
-
|
VH032-C3-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-136008
-
|
VH032-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-125845A
-
|
(S,S,S)-VH032-NH2 hydrochloride
|
Ligands for E3 Ligase
|
Cancer
|
|
(S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
|
-
- HY-130641
-
|
|
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.
|
-
- HY-133487A
-
|
VH032-C8-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-144768
-
|
|
Liposome
|
Others
|
|
(R)-Chol-TPP a mitochondria targeting liposome ligand could be used in pH-redox responsive.
|
-
- HY-135324
-
-
- HY-32339
-
|
22-Oxacalcitriol
|
VD/VDR
|
Metabolic Disease
|
|
Maxacalcitol (22-Oxacalcitriol) is non-calcemic vitamin D3 analog and ligand of VDR-like receptors.
|
-
- HY-155378
-
-
- HY-N0277
-
-
- HY-W127822
-
|
(1Z,4Z,10Z,15Z)-5,10,15-Triphenyl-22,24-dihydro-21H-corri
|
Biochemical Assay Reagents
|
Others
|
|
5,10,15-tris(phenyl)corrole is a corrole derivative used as a trianionic ligand for transition metals.
|
-
- HY-142240
-
-
- HY-145938
-
|
|
FAP
|
Cancer
|
|
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
|
-
- HY-112609
-
-
- HY-148556
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugates) that incorporates the Thalidomide (Thalidomide (HY-14658)) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-C6-azide is a click chemistry reagent, itcontains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-129941
-
|
VH032-C10-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.
|
-
- HY-129941A
-
|
VH032-C10-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-C10-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.
|
-
- HY-155264
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C8-NH2 hydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C8-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155260
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C4-NH2 hydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155262
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C6-NH2 hydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155259
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C3-NH2 hydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-155261
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-C5-NH2 hydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-C5-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-P3676
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (3-36) (porcine) is an agonist of neuropeptide Y (NPY) receptor subtype Y2, and stimulates feeding in rats. Neuropeptide Y (3-36) (porcine) is a highly Y2 selective ligand compared with nselective Y1/Y2 receptor ligand, Neuropeptide Y 1-36.
|
-
- HY-131178
-
|
|
Others
|
Others
|
|
HG-7-85-01-NH2 is the ligand of SNIPER(ABL)-033. SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 value of 0.3 μM.
|
-
- HY-130847
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-C10-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-C10-NH2 can be used in PROTAC MS432 (HY-130602).
|
-
- HY-P99325
-
|
IDEC-131; Anti-Human CD40 Ligand Recombinant Antibody
|
TNF Receptor
|
Inflammation/Immunology
|
|
Toralizumab (IDEC-131) is a humanized monoclonal antibody (mAb) against CD40L (CD154) comprised of human gamma 1 heavy chains and human kappa light chains. Toralizumab binds specifically to human CD40L on T cells, thereby preventing CD40 signaling. Toralizumab, a immunosuppressive agent, has the potential for active systemic lupus erythematosus (SLE) research.
|
-
- HY-112398
-
-
- HY-103628
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 Degrader-1 is a PROTAC connected by ligands for Cereblon and CDK as a selective CDK9 degrader.
|
-
- HY-101861
-
|
CPHPC; Ro63-8695; GSK2315698
|
Others
|
Neurological Disease
|
|
Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
|
-
- HY-19945
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
|
-
- HY-P4803
-
-
- HY-108515
-
|
JO1784
|
Sigma Receptor
|
Neurological Disease
|
|
(+)-Igmesine hydrochloride (JO1784) is an orally active and selective σ receptor ligand with neuroprotective and anti-amnesic activities.
|
-
- HY-139620
-
|
|
PROTACs
|
Cancer
|
|
MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
|
-
- HY-W343750
-
-
- HY-P4198
-
-
- HY-15264
-
MC 1046
1 Publications Verification
Impurity A of Calcipotriol
|
VD/VDR
|
Cancer
|
|
MC 1046(Impurity A of Calcipotriol) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
|
-
- HY-136184
-
|
VH032-phenol-C4-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-phenol-C4-NH2 (VH032-phenol-C4-NH2) dihydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-129652
-
|
|
AUTACs
|
Cancer
|
|
Halo PROTAC 1 is a conjugate of ligands for E3 and 22-atom-length linker. The connector of linker is Halogen group. Halo PROTAC 1 is a ligand having activity to bind to an intracellular proteins fused with HaloTag and a structure having activity to induce autophagy of an intracellular molecule are linked via a PEG linker. Halo PROTAC 1 can be uesd for the synthesis of AUTAC.
|
-
- HY-136187
-
|
VH032-C5-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
|
-
- HY-111844
-
|
|
SNIPERs
PROTACs
RAR/RXR
|
Cancer
|
|
PROTAC RAR Degrader-1 comprises a IAP ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
|
-
- HY-156162
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-C14-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-NH-C14-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
|
-
- HY-103603B
-
|
VH032-PEG2-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-NH2 dihydrochloride (VH032-PEG2-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.
|
-
- HY-132938
-
-
- HY-111850
-
|
PROTAC IAP binding moiety 1
|
Ligands for E3 Ligase
|
Cancer
|
|
Bestatin-amido-Me, the Bestatin-based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
|
-
- HY-139548
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.
|
-
- HY-139482
-
|
|
LYTACs
|
Cancer
|
|
tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.
|
-
- HY-15266
-
|
PRI 2202; Impurity D of Calcipotriol
|
VD/VDR
|
Cancer
|
|
24R-Calcipotriol(PRI 2202) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
|
-
- HY-111519
-
-
- HY-D1288A
-
-
- HY-139544
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-propoxyethanamine is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.
|
-
- HY-153855
-
|
RXC004
|
Wnt
Acyltransferase
Porcupine
|
Cancer
|
|
Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research.
|
-
- HY-130988
-
|
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-400685
-
|
|
Others
|
Cancer
|
|
SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models.
|
-
- HY-130854
-
|
|
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-111254
-
|
|
PPAR
|
Metabolic Disease
|
|
GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain.
|
-
- HY-130853
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.
|
-
- HY-140055
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-PEG4-Propargyl is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-PEG4-Propargyl 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-103223
-
|
NSC 710305
|
Cytochrome P450
|
Cancer
|
|
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.
|
-
- HY-N2540
-
|
(±)-5,7-Dihydroxyflavanone; NSC 43318
|
Free Fatty Acid Receptor
|
Others
|
|
(±)-Pinocembrin ((±)-5,7-Dihydroxyflavanone) is a GPR120 ligand able to promote wound healing in HaCaT cell line.
|
-
- HY-112588
-
-
- HY-P2277
-
-
- HY-16785A
-
|
INXN-1001 racemate; RG-115932 racemate
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Veledimex racemate (INXN-1001 racemate) is the racemate of veledimex. Veledimex is an orally available, small-molecule activator ligand for the RheoSwitch Therapeutic System.
|
-
- HY-107444
-
-
- HY-W127824
-
|
(5Z,9Z,14Z)-5,10,15-Tris(4-nitrophenyl)-22,24-dihydro-21H-corri
|
Biochemical Assay Reagents
|
Others
|
|
5,10,15-tris(4-nitrophenyl)corrole is a corrole derivative used as a trianionic ligand for transition metals.
|
-
- HY-103555
-
-
- HY-P2278
-
-
- HY-46340
-
-
- HY-D1288
-
-
- HY-U00250
-
-
- HY-P99966
-
|
|
RANKL/RANK
|
Cancer
|
|
Narlumosbart (JMT103) is an IgG4κ antibody targeting receptor activator of nuclear factor-κB ligand (RANKL).
|
-
- HY-101601
-
-
- HY-114907
-
|
Eosinic acid; Solvent Red 72
|
Fluorescent Dye
|
Others
|
|
4',5'-Dibromofluorescein (Eosinic acid) is a fluorescein derivative that can used as a ligand for studying of protein properties by spectral analysis.
|
-
- HY-156568
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models.
|
-
- HY-138778
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Propargyne-PEG1-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-Propargyne-PEG1-COOH is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-138776
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Propargyne-PEG3-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-Propargyne-PEG3-COOH is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-138678
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669).
|
-
- HY-138777
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-Propargyne-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-Propargyne-PEG2-COOH is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-108652
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene-ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene-ATP trisodium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.
|
-
- HY-134440
-
|
|
P2X Receptor
|
Inflammation/Immunology
|
|
α,β-Methylene ATP dilithium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand. α,β-Methylene ATP dilithium is a highly selective agonist for P2X1 and P2X3, with practically no activity at P2X2,4-7.
|
-
- HY-P2277A
-
-
- HY-P1186
-
|
Eledoisin-Related Peptide; Eledoisin RP
|
Neurokinin Receptor
|
Neurological Disease
|
|
Eledoisin Related Peptide is a Substance P analog that excites neurons and triggers behavioral responses. Eledoisin Related Peptide is also a tachykinin receptor ligand.
|
-
- HY-147311
-
-
- HY-112156
-
-
- HY-112376
-
-
- HY-P5054
-
-
- HY-112377
-
-
- HY-112155
-
-
- HY-A0077AS
-
-
- HY-107471
-
|
GP2a
|
Cannabinoid Receptor
|
Cancer
|
|
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.
|
-
- HY-147239
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-VA-PABC-MMAE is a agent-linker conjugate for ADC. MC-VA-PABC-MMAE contains the ADCs linker (peptide MC-VA-PABC) and a potent tubulin polymerization inhibitor MMAE (HY-15162).
|
-
- HY-108258
-
|
|
GPR119
|
Endocrinology
|
|
PSN 375963 is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
|
-
- HY-128128
-
|
|
Others
|
Neurological Disease
|
|
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
|
-
- HY-18370
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent.
|
-
- HY-108258A
-
|
|
GPR119
|
Endocrinology
|
|
PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
|
-
- HY-131029
-
|
JF646, Maleimide
|
Fluorescent Dye
|
Others
|
|
Janelia Fluor® 646, Maleimide (JF646, Maleimide) is a red fluorescent dye that contains a maleimide group. JF646, Maleimide can be used in cellular imaging. Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
|
-
- HY-35261A
-
|
|
PROTAC Linkers
|
Cancer
|
|
Mal-PEG2-NH2 (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-130197
-
|
|
PROTAC Linkers
|
Cancer
|
|
Lipoamido-PEG4-azide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Lipoamido-PEG4-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-141481
-
|
|
PROTACs
EGFR
PARP
|
Cancer
|
|
DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP.
|
-
- HY-129774
-
|
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH 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.
|
-
- HY-156164
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-NH-PEG2-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG2-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
|
-
- HY-146812
-
|
|
G-quadruplex
|
Cancer
|
|
DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells.
|
-
- HY-130617
-
|
|
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-130715
-
|
|
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.
|
-
- HY-156163
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-NH-PEG1-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG1-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
|
-
- HY-114407
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
|
-
- HY-156165
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-NH-PEG3-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG3-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
|
-
- HY-129773
-
|
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS 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.
|
-
- HY-111872
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
|
-
- HY-103333
-
-
- HY-P99408
-
-
- HY-100930
-
-
- HY-111857
-
|
BMS-354825 carbaldehyde; PROTAC ABL binding moiety 4
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
|
-
- HY-111556
-
|
|
PROTACs
CDK
|
Cancer
|
|
BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.
|
-
- HY-P0031
-
|
|
Integrin
|
Others
|
|
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.
|
-
- HY-143346
-
|
|
Others
|
Cancer
|
|
CCW16 is the covalent ligand for the E3 ubiquitin ligase RNF4. CCW16 can be used in the synthesis of protein degraders.
|
-
- HY-136269A
-
-
- HY-136269
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
A 410099.1, amine-Boc hydrochloride is a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5).
|
-
- HY-P1037
-
|
|
Motilin Receptor
|
Others
|
|
Motilin (26-47), human, porcine is an endogenous motilin receptor ligand with Ki and EC50 of 2.3 nM and 0.3 nM in a Chinese hamster ovary cell line.
|
-
- HY-N11494
-
|
|
NF-κB
|
Others
|
|
Dauricumine is a chlorinated alkaloid that inhibits NF-κB ligand-induced differentiation of mouse bone marrow-derived macrophages into multinucleated osteoclasts.
|
-
- HY-148362
-
-
- HY-128767
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-PEG3-acetylene is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. VH032-PEG3-acetylene 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-111593
-
|
|
PROTACs
|
Cancer
|
|
Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC, consists of two ligands of von Hippel-Lindau.
|
-
- HY-100275
-
-
- HY-112895A
-
|
|
Androgen Receptor
|
Cancer
|
|
(R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.
|
-
- HY-132858
-
-
- HY-153419
-
|
|
Others
|
Others
|
|
BTTES is a tris(triazolylmethyl)amine-based ligand for Cu(I) without apparent toxicity. BTTES IMPROVES the cycloaddition reaction rapidly in living systems.
|
-
- HY-133137A
-
|
|
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-135558
-
-
- HY-133137
-
|
|
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-112375
-
|
|
PROTACs
|
Cancer
|
|
AT6 is a PROTAC AT1 analogue, which is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 with highly selectivity to bromodomain (Brd4).
|
-
- HY-15420
-
|
Indomethacin morpholinylamide; IMMA
|
Cannabinoid Receptor
|
Cancer
|
|
BML-190(IMMA) is a potent and selective CB2 receptor ligand (Ki values are 435 nM and > 2 μM for CB2 and CB1 respectively).
|
-
- HY-144323
-
|
|
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-143418
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-17 (Compound 16) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-17 exhibits potent anti-viral activity with the EC50 of 2.18 μM. SARS-CoV-2-IN-17 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-17 is a potent NPro ligand.
|
-
- HY-107442
-
|
|
Epigenetic Reader Domain
Ligands for Target Protein for PROTAC
|
Cancer
|
|
PROTAC BRD4-binding moiety 1 is a ligand for BRD4. PROTAC BRD4-binding moiety 1 binds to cereblon ligand via a linker to form PROTAC to degrade BRD4 (HY-133136). PROTAC BRD4-binding moiety 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-136055
-
|
VH032-C5-COOH
|
E3 Ligase Ligand-Linker Conjugates
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
|
-
- HY-125876
-
|
|
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.
|
-
- HY-134581
-
|
M5049
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
|
-
- HY-144825
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function.
|
-
- HY-143417
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-16 (Compound 12) is a potent SARS-CoV-2 nucleocapsid protein (NPro) inhibitor. SARS-CoV-2-IN-16 exhibits potent anti-viral activity with the EC50 of 3.69 μM. SARS-CoV-2-IN-16 binds to NPro with the low KD value of 7.82 μM, suggesting that SARS-CoV-2-IN-16 is a potent NPro ligand.
|
-
- HY-N4194
-
|
|
PPAR
|
Metabolic Disease
|
|
Glabrone is an isoflavone isolated from Glycyrrhiza glabra roots. Glabrone exhibits anti-influenza activity and significant PPAR-γ ligand-binding activity.
|
-
- HY-111858
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-050, conjugating Imatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
|
-
- HY-111852
-
-
- HY-103633
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BET Degrader-1 is a PROTAC connected by ligands for Cereblon and BET, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
|
-
- HY-129405
-
|
|
Bacterial
|
Infection
|
|
N-(Ketocaproyl)-DL-homoserine lactone is a natural, very active ligand of LuxR. N-(Ketocaproyl)-DL-homoserine lactone is a quorum sensing (QS) autoinducer.
|
-
- HY-P9904
-
|
MPDL3280A
|
PD-1/PD-L1
Apoptosis
Autophagy
|
Cancer
|
|
Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
|
-
- HY-W011051S1
-
-
- HY-P99641
-
|
|
PD-1/PD-L1
|
Cancer
|
|
Gilvetmab is a potent caninized antiPD-1 monoclonal antibody. gilvetmab blocks the interaction between PD-1 and its ligand PDL-1.
|
-
- HY-111853
-
|
PROTAC IAP binding moiety 2
|
Ligands for E3 Ligase
|
Cancer
|
|
MV-1-NH-Me, the MV-1 based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
|
-
- HY-13751
-
|
|
Sigma Receptor
|
Inflammation/Immunology
|
|
SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
|
-
- HY-122577
-
-
- HY-W011051S
-
-
- HY-124625
-
-
- HY-141495
-
-
- HY-133136
-
-
- HY-155698
-
|
|
Others
|
Others
|
|
Mz438 is high-affinity and selective fluorescent CXCR2 ligand. Mz438 is a small-molecule-based fluorescent probe targeting the IABS of CXCR2.
|
-
- HY-111758
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.
|
-
- HY-149307
-
|
|
Others
|
Others
|
|
CYCA-117-70 is a DCAF1 ligand (KD: 70 μM). CYCA-117-70 is an ideal chemical handles for PROTACs recruiting DCAF1.
|
-
- HY-132939
-
-
- HY-111849
-
|
CGP-57148B carbaldehyde; STI571 carbaldehyde; PROTAC ABL binding moiety 1
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
|
-
- HY-N8460A
-
|
Cortisol 21-sulfate sodium
|
Endogenous Metabolite
|
Endocrinology
|
|
Cortisol sulfate sodium (Cortisol 21-sulfate) is a metabolite of Cortisol (HY-N0583). Cortisol sulfate sodium is a specific ligand for intracellular transcortin.
|
-
- HY-P99625
-
|
SAR441344; INX-021
|
TNF Receptor
|
Inflammation/Immunology
|
|
Frexalimab (SAR441344; INX-021) is a monoclonal antibody targeting the CD40 ligand (CD40L). Frexalimab has the potential for multiple sclerosis research.
|
-
- HY-N8460
-
|
Cortisol 21-sulfate
|
Endogenous Metabolite
|
Endocrinology
|
|
Cortisol sulfate (Cortisol 21-sulfate) is a metabolite of Cortisol (HY-N0583). Cortisol sulfate is a specific ligand for intracellular transcortin.
|
-
- HY-W615104
-
|
|
Others
|
Others
|
|
BTTP is a tris(triazolylmethyl)amine-based ligand. BTTP can accelerate the copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), the prototypical reaction in click chemistry.
|
-
- HY-15329
-
|
|
VD/VDR
|
Metabolic Disease
|
|
Maxacalcitol-d66 is the deuterated form of Maxacalcitol (22-Oxacalcitriol), which is a non-calcemic vitamin D3 analog and VDR ligand of VDR-like receptors.
|
-
- HY-130640
-
-
- HY-121738
-
-
- HY-N12335
-
|
|
Others
|
Others
|
|
Desacetylxanthanol (Compound 4) is a sesquiterpenoid derived from Xanthium strumarium. Desacetylxanthanol has anti-tumor necrosis factor-associated apoptosis-inducing ligand (TRAIL) activity.
|
-
- HY-W584518
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-5-O-CH2-COOH is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-5-O-CH2-COOH acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-5-O-CH2-COOH is a key intermediate in the synthesis of PROTAC molecules designed based on CRBN.
|
-
- HY-139344
-
|
|
PROTACs
FAK
|
Cancer
|
|
FC-11 is a PROTAC FAK degrader (DC90: 1 nM) . FC-11 contains CRBN ligand Pomalidomide (HY-10984), linker and FAK ligand PF562271 (HY-10459). FC-11 degrades FAK in various cells, with DC50s of 310 pM in TM3, 80 pM in PA1, 330 pM in MDA-MB-436, 370 pM in LNCaP, and 40 pM in Ramos cells.
|
-
- HY-129772
-
|
|
PROTAC Linkers
|
Cancer
|
|
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs 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.
|
-
- HY-40178
-
|
|
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.
|
-
- HY-131030
-
|
JF669, SE; JF669, NHS
|
Fluorescent Dye
|
Others
|
|
Janelia Fluor 669, SE (JF669, SE), a red fluorescent dye, can be directly reacted with the available thiol-containing HaloTag ligand under mild conditions (DIEA, DMF) to afford a JF669HaloTag ligand in a single step (Ex = 669 nm; Em = 682 nm). Janelia Fluor products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
|
-
- HY-140844
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-PEG4-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-PEG4-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-P99437
-
|
KN-026
|
EGFR
|
Cancer
|
|
Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting the extracellular domains II and IV of the human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathway. The IgG1 Fc fragment of Anbenitamab binds FcRγIIIa mediates potent antibody dependent cell-mediated cytotoxicity (ADCC) and inhibits tumor cell proliferation. Anbenitamab has the potential for HER2-positive metastatic breast cancer (MBC) research.
|
-
- HY-108496
-
|
S1P
|
Endogenous Metabolite
LPL Receptor
|
Endocrinology
|
|
Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
|
-
- HY-69220
-
|
|
PROTAC Linkers
|
Cancer
|
|
7-Octynoic acid (compound 42) is a PROTAC linker and 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. 7-Octynoic acid is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-141015
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG4-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. Pomalidomide-PEG4-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-W048671
-
|
|
Amino Acid Derivatives
|
Others
|
|
Fmoc-Thr(TBDMS)-OH is a Threonine derivative. Fmoc-Thr(TBDMS)-OH can be used for the preparation of sugar ligand-tethered functional nucleic acid conjugates for targeted research.
|
-
- HY-N3960
-
|
|
PPAR
Bacterial
|
Infection
Metabolic Disease
|
|
Glycyrin is a PPAR-γ ligand of licorice. Glycyrin can decrease the blood glucose levels of genetically diabetic mice. Glycyrin also shows antibacterial activity.
|
-
- HY-16954
-
-
- HY-115568
-
|
|
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-139309
-
|
|
Bcl-2 Family
PROTACs
|
Cancer
|
|
PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.
|
-
- HY-136280
-
|
EMD 57445
|
Sigma Receptor
|
Neurological Disease
|
|
Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent.
|
-
- HY-139680
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-1 is a dopamine D3 receptor-selective or multitarget bitopic ligand (Ki = 1.58 nM) potentially useful for central nervous system disorders.
|
-
- HY-107737
-
|
1,2-Dilauroyl-sn-glycero-3-phosphocholine
|
Liposome
|
Metabolic Disease
|
|
DLPC (1,2-Dilauroyl-sn-glycero-3-phosphocholine) is an LRH-1 agonist ligand.
DLPC is a phospholipid for biological study.
|
-
- HY-139681
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-2 is a dopamine D3 receptor-selective (Ki = 2.16 nM) or multitarget bitopic ligand potentially useful for central nervous system disorders.
|
-
- HY-N10062
-
|
|
RANKL/RANK
|
Others
|
|
Amakusamine inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced formation of multinuclear osteoclasts with an IC50 value of 10.5 μM in RAW264.7 cells.
|
-
- HY-13751A
-
|
|
Sigma Receptor
|
Inflammation/Immunology
|
|
SR-31747 free base is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase.
|
-
- HY-111851
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-049, conjugating Imatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 100 μM.
|
-
- HY-114616
-
|
|
Others
|
Neurological Disease
|
|
PBB3, a selective PET ligand, recognizes tau pathology in Alzheimer's disease brains, where dystrophic neurites and diffuse neurofibrils are more clearly detected Tangles with calcification.
|
-
- HY-P0272
-
|
|
HIV
|
Infection
|
|
Peptide T is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-111433
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 degrader AT1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4 as a highly selective Brd4 degrader, with a Kd of 44 nM for Brd4 BD2 in cells.
|
-
- HY-P1464
-
|
Amylin (rat)
|
Amylin Receptor
|
Metabolic Disease
|
|
Amylin, amide, rat is a potent and high affinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
|
-
- HY-15527
-
|
AC-5216; XBD-173
|
Others
|
Metabolic Disease
Neurological Disease
|
|
Emapunil (AC-5216), an orally active and selective TSPO (a mitochondrial benzodiazepine receptor) ligand, produces anti-anxiety and antidepressant-like effects in various animal models.
|
-
- HY-U00180
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors. KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM).
|
-
- HY-N6253
-
|
(+)-Pinoresinol
|
Apoptosis
|
Cancer
|
|
Pinoresinol is a lignol of plant origin serving for defense in a caterpillar. Pinoresinol drastically sensitizes cancer cells against TNF-related apoptosis-inducing ligand (TRAIL) -induced apoptosis.
|
-
- HY-15594
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Phen-DC3 is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
|
-
- HY-111860
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 20 μM.
|
-
- HY-P99188
-
|
CNTO 888
|
CCR
|
Cancer
|
|
Carlumab (CNTO 888) is a humanised anti-CCL2 (chemokine ligand 2) antibody with high affinity. Carlumab can be used in cancer research, particularly in prostate cancer.
|
-
- HY-103029
-
|
|
Wee1
|
Cancer
|
|
Bosutinib isomer is a ligand or inhibitor with high binding affinity for both Wee1 and Wee2, with Kd values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively.
|
-
- HY-W011051S2
-
-
- HY-12452
-
-
- HY-111855
-
-
- HY-148896
-
-
- HY-153917
-
|
|
Others
|
Cancer
Metabolic Disease
|
|
CRT0063465 is a Ligand of HumanPGK1andStress Sensor DJ1, with theKdof 24 μM ofPGK1. CRT0063465 modulates the shelterin complex composition
and telomere Length.
|
-
- HY-122246
-
|
|
GPR55
PKC
ERK
Arrestin
|
Metabolic Disease
|
|
ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.
|
-
- HY-116918
-
|
N-Acetyldiphenylamine
|
Others
|
Others
|
|
N,N-Diphenylacetamide (N-Acetyldiphenylamine) has N,N-disubstituted amide group and can be used as a mono- as well as a bidentate ligand generating four-membered chelate rings.
|
-
- HY-141729
-
|
|
Fluorescent Dye
|
Cancer
|
|
Biotin-NH-PSMA-617 is a biotin-tagged PSMA-617. PSMA-617 is a small molecule targeting the prostate-specific membrane antigen (PSMA), which is directly expressed by the tumor cells .
|
-
- HY-139402
-
|
|
Ras
|
Cancer
|
|
MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2 (HY-137516). LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC 50s between 0.25 and 0.76 μM).
|
-
- HY-144272
-
-
- HY-P5064
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide that was first isolated from the porcine hypothalamus. Galanin-Like Peptide (porcine) has a high affinity for the GALR2 receptor (IC50 of 0.24 nM) and a lower affinity for the GALR1 receptor (IC50 of 4.3 nM).
|
-
- HY-P2543
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Neuropeptide Y (3-36) (human, rat), a neuropeptide Y (NPY) metabolite formed from dipeptidyl peptidase-4 (DPP4), is a selective Y2 receptor agonist. Neuropeptide Y (3-36) (human, rat) is a NPY metabolite formed from dipeptidyl peptidase-4 (DPP4). Neuropeptide Y (3-36) (human, rat) decreases release of norepinephrine via the Y2 receptor.
|
-
- HY-P0262
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
Endocrinology
|
|
Galantide, a non-specific galanin receptor antagonist, is a peptide consisting of fragments of galanin and substance P. Galantide recognizes two classes of galanin binding sites (KD<0.1 nM and ~6 nM) in the rat hypothalamus. Galantide dose dependently (IC50=1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. Galantide appears to bind to a single population of SP receptors (KD~40 nM).
|
-
- HY-108509
-
|
BMY-14802-1; BMS 181100 hydrochloride
|
Sigma Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.
|
-
- HY-34544
-
|
|
Others
|
Others
|
|
2-Hexylthiophene is an extremely weak basic heteroaromatic compound. 2-Hexylthiophene can be used to modify and improve the molar absorption coefficient of ruthenium sensitizer
|
-
- HY-132208
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-PEG2-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology. Pomalidomide 4'-PEG2-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-P4990A
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
Pro8-Oxytocin TFA is a a modified oxytocin (OXT) ligand. Pro8-Oxytocin produces more potent and efficacious responses at primate OXTR and stronger behavioral effects than the consensus mammalian OXT ligand (Leu8-Oxytocin). Pro8-Oxytocin TFA produce a less efficacious response than Vasopressin (HY-B1811) (AVP) at human AVPR1a and higher efficacious response than AVP at marmoset AVPR1a.
|
-
- HY-137538
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology. Pomalidomide-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-131168
-
|
VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) is a E3 ligase ligand-linker conjugate that contains on one end a VHL ligand. (S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH is used in PROTAC technology.
|
-
- HY-P4990
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
Pro8-Oxytocin is a a modified oxytocin (OXT) ligand. Pro8-Oxytocin produces more potent and efficacious responses at primate OXTR and stronger behavioral effects than the consensus mammalian OXT ligand (Leu8-Oxytocin). Pro8-Oxytocin produce a less efficacious response than Vasopressin (HY-B1811) (AVP) at human AVPR1a and higher efficacious response than AVP at marmoset AVPR1a.
|
-
- HY-W584523
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-4-NH-PEG1-COOH TFA is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-4-NH-PEG1-COOH TFA acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-4-NH-PEG1-COOH TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-137537
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG2-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology. Pomalidomide-PEG2-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-129619
-
|
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
|
-
- HY-117726
-
-
- HY-B2087
-
|
HPN-100
|
Sigma Receptor
|
Cardiovascular Disease
|
|
Glycerol phenylbutyrate is a sigma-2 (σ2) receptor ligand, with a pKi of 8.02. Glycerol phenylbutyrate (GPB) is a new generation ammonia scavenger agent.
|
-
- HY-130852
-
-
- HY-153550
-
|
|
PSMA
|
Others
|
|
PSMA-1007 is a prostate-specific membrane antigen (PSMA) ligand. 18F-labeled PSMA-1007 can be used as a PET tracer for prostate cancer imaging.
|
-
- HY-111413
-
|
|
Integrin
|
Cancer
|
|
c(phg-isoDGR-(NMe)k) is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
|
-
- HY-147354
-
|
|
LYTACs
|
Cardiovascular Disease
|
TriGalNAc CBz is a GalNAc derivative and tri-GalNAc is an asialoglycoprotein receptor (ASGPR) ligand. TriGalNAc CBz can be used for mRNA drug delivery as well as lysosomal targeted chimerism (LYTAC) studies.
|
-
- HY-124673
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
AF40431, the first reported small-molecule ligand of sortilin, has an IC50 of 4.4 µM and a Kd of 0.7 µM . AF40431 is bound in the neurotensin-binding site of sortilin.
|
-
- HY-106025
-
|
AC-3933
|
GABA Receptor
|
Neurological Disease
|
|
Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist. AC-3933 binds to GABA(-) and GABA(+) ligand with Kis of 5.15 and 6.11 nM, respectively.
|
-
- HY-129180
-
|
|
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-P0272A
-
|
|
HIV
|
Infection
|
|
Peptide T (TFA) is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a ligand for the CD4 receptor and prevents binding of HIV to the CD4 receptor.
|
-
- HY-15594A
-
|
Phen-DC3 Triflate
|
G-quadruplex
|
Cancer
|
|
Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
|
-
- HY-D1398
-
|
|
nAChR
|
Neurological Disease
|
|
LtIA-F, a novel fluorescent analogue of LtIA, provides a wealth of pharmacological tools to explore the structure–function relationship, distribution, and ligand binding domain of the α3β2 nAChR subtype.
|
-
- HY-114306
-
|
|
Antifolate
|
Cancer
|
|
EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor. Small molecule-agent conjugate (SMDC).
|
-
- HY-130850
-
-
- HY-111859
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.
|
-
- HY-111854
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM .
|
-
- HY-P99307
-
|
AMG-203; Anti-Human CSF2 Recombinant Antibody
|
c-Fms
|
Inflammation/Immunology
|
|
Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with high affinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis.
|
-
- HY-138865
-
|
|
Others
|
Infection
|
|
BiCAPPA is the first bivalent antiprion ligand. BiCAPPA can decrease infectious conformational form of prion protein (PrP Sc) from scrapie-infected cells, with an EC50 of 0.32 μM.
|
-
- HY-P3279
-
|
|
Src
|
Cancer
|
|
EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.
|
-
- HY-N11773
-
|
|
PPAR
|
Metabolic Disease
|
|
Gancaonin L is an isoflavone, that can be isolated from Glycyrrhiza glabra roots. Gancaonin L exhibits significant PPAR-γ ligand-binding activity. Gancaonin L can be used for anti-diabetes and anti-obesity research.
|
-
- HY-111876A
-
|
|
SNIPERs
|
Cancer
|
|
SNIPERTACC3-1 hydrochloride targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPERTACC3-1 hydrochloride induces cancer cell death.
|
-
- HY-101380A
-
|
|
Imidazoline Receptor
|
Neurological Disease
|
|
BU226 hydrochloride is a selective imidazoline 2 (I2) receptors ligand with an Ki of 1.4 nM for I2 and an IC50 of 534.5 nM for I1. BU226 hydrochloride can be used for researching antidepressant.
|
-
- HY-P99852
-
|
ABT165; PR1283233
|
VEGFR
|
Cancer
|
|
Dilpacimab (ABT165) is a potent dual-variable domain immunoglobulin, targets both delta-like ligand 4 (DLL4) and VEGF pathways.. Dilpacimab can be used in research of cancer.
|
-
- HY-103148
-
-
- HY-147021A
-
-
- HY-114228
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
|
-
- HY-112617B
-
-
- HY-111413A
-
|
|
Integrin
|
Cancer
|
|
c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
|
-
- HY-111873
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-019, conjugating Dasatinib (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM.
|
-
- HY-12809
-
Optovin
1 Publications Verification
|
TRP Channel
|
Neurological Disease
|
|
Optovin is a reversible photoactivated TRPA1 ligand that enables light-mediated neuronal excitation. Optovin activates TRPA1 via structure-dependent photochemical reactions with redox-sensitive cysteine residues.
|
-
- HY-P99475
-
|
MSB-2311
|
PD-1/PD-L1
|
Cancer
|
|
Betifisolimab (MSB-2311) is a humanized monoclonal antibody directed against the immunosuppressive ligand PD-L1. Betifisolimab has the potential for advanced solid tumors and hematological malignancies research.
|
-
- HY-136006
-
|
VH032-C6-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
Inflammation/Immunology
|
|
(S,R,S)-AHPC-C6-NH2 dihydrochloride (VH032-C6-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 dihydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
|
-
- HY-133487B
-
|
VH032-C8-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
Inflammation/Immunology
|
|
(S,R,S)-AHPC-C8-NH2 (VH032-C8-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
|
-
- HY-136006A
-
|
VH032-C6-NH2 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
Inflammation/Immunology
|
|
(S,R,S)-AHPC-C6-NH2 hydrochloride (VH032-C6-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C6-NH2 hydrochloride is XF038-161A, example 6, extracted from patent WO2019173516A1.
|
-
- HY-130618
-
|
|
PROTAC Linkers
|
Cancer
|
|
Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH 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.
|
-
- HY-133487
-
|
VH032-C8-NH2 dihydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
Inflammation/Immunology
|
|
(S,R,S)-AHPC-C8-NH2 dihydrochloride (VH032-C8-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for AKT PROTAC degrader. (S,R,S)-AHPC-C8-NH2 is XF038-164A, example 8, extracted from patent WO2019173516A1.
|
-
- HY-130711A
-
|
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-154857
-
|
|
Others
|
Cancer
|
|
1-Palmitoyl-2-succinyl-sn-glycerophosphorylcholine is a glycerophosphorylcholine, consisting of glycerol phosphate, choline and palmitic acid. It accumulates in vivo at sites of oxidative stress. 1-Palmitoyl-2-succinyl-sn-glycerophosphorylcholine may be a ligand of scavenger receptors class B, while oxidized phospholipids oxPC(CD36) are potent ligands of scavenger receptors class B (CD36 and SR-BI). Oxidized phospholipids (oxPLs) also play an important role in tumor apoptosis, may be elevated in malignant biliary strictures.
|
-
- HY-W584521
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-4-NH-PEG1-NH2 TFA is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-4-NH-PEG1-NH2 TFA acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-4-NH-PEG1-NH2 TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
|
-
- HY-130711
-
|
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-P3108
-
-
- HY-P3099
-
|
|
Guanylate Cyclase
|
Cancer
|
|
Uroguanylin (human) is a natural ligand for the Guanylyl Cyclase (GCC) receptor expressed in metastatic colorectal cancer tumors. Uroguanylin (human) has anti-tumor actions in an animal model for human colon cancer.
|
-
- HY-111861
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
|
-
- HY-102023
-
GNF351
3 Publications Verification
|
Aryl Hydrocarbon Receptor
|
Others
|
|
GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. GNF351 competes with a photoaffinity AHR ligand for binding to the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in mouse or human keratinocytes.
|
-
- HY-139620A
-
|
|
PROTACs
|
Others
|
|
MS83 epimer 1 is the epimer of MS83 (HY-139620). MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
|
-
- HY-149097
-
|
|
Phosphatase
|
Neurological Disease
|
|
ITH12711 is a PP2A ligand. ITH12711 is able to cross the blood-brain barrier (BBB). ITH12711 exerts neuroprotection via restoration of PP2A-phosphatase activity.
|
-
- HY-111862
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-044, conjugating HG-7-85-01 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.
|
-
- HY-124382
-
|
|
TRP Channel
|
Neurological Disease
|
|
AS1928370 is a novel and central nervous system (CNS) penetrant TRPV1 antagonist and can prevent ligand-induced activation in vivo. AS1928370 is a promising agent for neuropathic pain treatment research.
|
-
- HY-16785B
-
|
INXN-1001 (S enantiomer); RG-115932 (S enantiomer)
|
Interleukin Related
|
Cancer
|
|
Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
|
-
- HY-101026
-
|
|
HSP
|
Cancer
|
|
CCT251236 is an orally available pirin ligand from a heat shock transcription factor 1 (hsf1) phenotypic screen with an IC50 of 19 nM for inhibition of HSF1-mediated HSP72 induction.
|
-
- HY-155033
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Others
|
|
SSI-4 is an inhibitor of Stearoyl CoA desaturase 1 (SCD1) , which can be modified with 11C, used as a ligand to in vivo small animal PET/CT imaging of SCD1.
|
-
- HY-135345
-
|
|
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-150158
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research.
|
-
- HY-15238A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ST-836 hydrochloride (compound 34) is a potent dopamine receptor ligand with Ki values of 4.5 nM, 132 nM for D3 and D2, respectively. ST-836 hydrochloride has the potential for Parkinson’s disease.
|
-
- HY-122562
-
MT-802
1 Publications Verification
|
PROTACs
Btk
|
Cancer
Inflammation/Immunology
|
|
MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).
|
-
- HY-123937
-
|
|
PROTACs
CDK
|
Cancer
|
|
THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
|
-
- HY-111866
-
|
|
PROTACs
RIP kinase
|
Inflammation/Immunology
|
|
PROTAC RIPK degrader-2 is a nonpeptidic PROTAC based on von Hippel-Lindau ligand which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
|
-
- HY-111876
-
|
|
SNIPERs
|
Cancer
|
|
SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-1 induces cancer cell death.
|
-
- HY-P0224
-
|
fMLP; N-Formyl-MLF
|
TNF Receptor
|
Inflammation/Immunology
|
|
N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
|
-
- HY-130845
-
-
- HY-130714
-
|
|
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-100686
-
|
|
GABA Receptor
|
Neurological Disease
|
|
U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.
|
-
- HY-P99736
-
|
BI-754111
|
LAG-3
|
Cancer
|
|
Miptenalimab (BI-754111) is an anti-human LAG-3 antibody (KD: 88.6 nM for h LAG-3). Miptenalimab blocks the interaction of LAG-3 with its ligand MHC-II.
|
-
- HY-146180
-
|
|
FAP
|
Cancer
|
|
FSDD0I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD0I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-19567
-
|
RP 52028
|
Parasite
|
Infection
|
|
PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
|
-
- HY-146181
-
|
|
FAP
|
Cancer
|
|
FSDD1I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD1I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-134977
-
|
|
Ras
|
Cancer
|
|
Atrovastatin-PEG3-FITC (compound S31) is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay.
|
-
- HY-110213
-
|
|
Fluorescent Dye
|
Others
|
|
BODIPY 630/650X is a fluorescent conjugate of the adenosine receptor ligand N-ethylcarboxamido-adenosine (NECA). BODIPY 630/650X displays excitation/emission maxima of 630/650 nm, respectively.
|
-
- HY-146436
-
|
|
Angiotensin Receptor
|
Others
|
|
AT1R antagonist 2 (compound 6) is a potent AT1R selective ligand. AT1R antagonist 2 exhibits a fair AT1R affinity, with a Ki of 26 nM.
|
-
- HY-149934
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
DCAF1 binder 1 is a selective for the CRL4 DCAF1 E3 ligase complex. DCAF1 binder 1 is a ligands for E3 Ligase, involving in targeted protein degradation (TPD).
|
-
- HY-111877
-
|
|
SNIPERs
|
Cancer
|
|
SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-2 induces cancer cell death.
|
-
- HY-15839
-
UNC 669
2 Publications Verification
|
Epigenetic Reader Domain
|
Cancer
|
|
UNC 669, a ligand for a methyl-lysine binding domain, is a potent L3MBTL1 (IC50=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor.
|
-
- HY-W595340
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
E3 ubiquitin ligase binder-1 (compound 11) is a potent E3 ubiquitin ligase binder. E3 ubiquitin ligase binder-1 is a ligand for E3 Ligase.
|
-
- HY-128845
-
|
|
PROTACs
|
Cancer
|
|
PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader.
|
-
- HY-111877A
-
|
|
SNIPERs
|
Cancer
|
|
SNIPER(TACC3)-2 hydrochloride targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway based on IAP ligand. SNIPER(TACC3)-2 hydrochloride induces cancer cell death.
|
-
- HY-136257
-
|
|
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-101838
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC50 of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.
|
-
- HY-146182
-
|
|
FAP
|
Cancer
|
|
FSDD3I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD3I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-108496S
-
|
S1P-d7
|
Endogenous Metabolite
LPL Receptor
|
Endocrinology
|
|
Sphingosine-1-phosphate-d7 is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2].
|
-
- HY-130814
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C4-NH2 TFA (compound 29c) is an E3 ligase ligand-linker conjugate, and incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-NH-C4-NH2 TFA is used in PROTAC BRD2/BRD4 degrader-1 (HY-130612). PROTAC BRD2/BRD4 degrader-1 is a potent and selective BET protein BRD4 and BRD2 degrader.
|
-
- HY-124619
-
|
|
FKBP
HIV
|
Infection
Neurological Disease
|
|
GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models. GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models. GPI-1046 improves HIV-associated injury of peripheral nerves.
|
-
- HY-131387
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the a VHL ligand and a linker. (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 can be used in PROTAC BRD4 Degrader-5 (HY-133737) and PROTAC BRD4 Degrader-5-CO-PEG3-N3 (HY-133736).
|
-
- HY-130816
-
|
VH032-O-Ph-PEG1-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02.
|
-
- HY-130709
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with Cereblon ligand.
|
-
- HY-13992
-
|
B/B Homodimerizer
|
FKBP
|
Metabolic Disease
|
|
AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
|
-
- HY-146431
-
|
|
Angiotensin Receptor
|
Others
|
|
AT1R antagonist 1 (compound 10) is a potent AT1R selective ligand. AT1R antagonist 1 exhibits a fair AT1R affinity, with a Ki of 8.5 nM.
|
-
- HY-111863
-
|
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM.
|
-
- HY-P2112
-
|
DOTA-Nal3-octreotide
|
Somatostatin Receptor
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Others
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DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging.
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- HY-22024
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Others
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Cancer
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5-Hydroxyflavone, a flavonoid ligand, shows no cytotoxic activity against MCF-7, FaDU, MDA-MB-435S, U87, RPE-1, and HEK293 cells.
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- HY-101622
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5-HT Receptor
Dopamine Receptor
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5-HT6/7 antagonist 1 is a multifunctional ligand that antagonizes 5-HT6/7/2A and D2 receptors, without interacting with M1 receptors and hERG channels.
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- HY-103632
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PROTACs
Epigenetic Reader Domain
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Cancer
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PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
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- HY-130845A
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