Search Result
Results for "
ligand
" in MCE Product Catalog:
1164
Inhibitors & Agonists
3
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-145484
-
|
PROTAC IRAK4 ligand-3
|
PROTACs
|
Cancer
|
|
PROTAC IRAK4 ligand-3 is a ligand of PROTAC IRAK4 degrader-7 (HY-145483). PROTAC IRAK4 ligand-3 can be used for the research of cancer.
|
-
- HY-146441
-
-
- HY-133045
-
|
VHL Ligand 8
|
Ligands for E3 Ligase
|
Cancer
|
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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.
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-
- HY-147366
-
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RBP4 ligand-1
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Others
|
Metabolic Disease
|
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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.
|
-
- HY-150407
-
|
TSPO ligand-1
|
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.
|
-
- HY-151479
-
|
GID4 Ligand 3
|
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.
|
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- HY-43869
-
|
Vipivotide tetraxetan Ligand-Linker Conjugate
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-126456
-
-
- HY-145308
-
-
- HY-133073
-
|
CCR7 Ligand 1
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-P1840A
-
-
- HY-P1840
-
-
- HY-133046
-
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VHL Ligand-Linker Conjugates 17
|
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.
|
-
- HY-115953
-
-
- HY-128808
-
|
cIAP1 ligand 1
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.
|
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- HY-128809
-
|
cIAP1 ligand 2
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.
|
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- HY-103597
-
|
Thalidomide-O-COOH
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-103596
-
|
Thalidomide-4-OH
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.
|
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- HY-128837
-
|
Nutlin carboxylic acid
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.
|
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- HY-41547
-
|
Thalidomide 4-fluoride
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).
|
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- HY-139656
-
-
- HY-146102
-
|
M1 ligand 1
|
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.
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- HY-128807
-
|
E3 ligase Ligand 10
|
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.
|
-
- HY-129653
-
|
E3 ligase Ligand 18
|
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.
|
-
- HY-128811
-
|
E3 ligase Ligand 14
|
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
-
|
E3 ligase Ligand 8
|
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
-
|
E3 ligase Ligand 13
|
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-141724
-
|
PCSK9 ligand 1
|
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-128806
-
|
E3 ligase Ligand 9
|
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-114399
-
-
- HY-146125
-
|
CGCG/CGG ligand 1
|
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.
|
-
- HY-150410
-
|
TSPO ligand-3
|
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.
|
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- HY-125905
-
|
VH032-cyclopropane-F
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-146081
-
|
CD22 ligand-1
|
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-128836
-
-
- HY-150409
-
|
TSPO ligand-2
|
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-145990
-
|
FABPs ligand 6
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.
|
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- HY-111823
-
-
- HY-115729
-
-
- HY-151476
-
-
- HY-139304
-
-
- HY-132942
-
-
- HY-129967
-
-
- HY-138539
-
-
- HY-141486
-
|
(Rac)-PROTAC PARP/EGFR ligand 1
|
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.
|
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- HY-147810
-
-
- HY-139660
-
-
- HY-145922
-
-
- HY-U00126
-
-
- HY-111845
-
-
- HY-111839
-
-
- HY-115968
-
|
Dopamine D3 receptor ligand-4
|
Dopamine Receptor
|
Neurological Disease
|
|
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). Dopamine D3 receptor ligand-4 can be used for the research of Cocaine use disorder.
|
-
- HY-129939
-
-
- HY-115955
-
|
Dopamine D3 receptor ligand-3
|
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). Dopamine D3 receptor ligand-3 has the potential for Cocaine use disorder (CUD) research.
|
-
- HY-115954
-
|
Dopamine D3 receptor ligand-2
|
Dopamine Receptor
|
Neurological Disease
|
|
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). Dopamine D3 receptor ligand-2 has the potential for Cocaine use disorder (CUD) research.
|
-
- HY-132970
-
-
- HY-101626A
-
-
- HY-101626
-
|
Sigma-LIGAND-1
|
Sigma Receptor
|
Neurological Disease
|
|
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.
|
-
- HY-126351
-
|
PROTAC ERRα ligand 2
|
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
-
-
- HY-111843
-
-
- HY-130270
-
-
- HY-130296
-
-
- HY-130297
-
|
PROTAC BCR-ABL1 ligand 1
|
Bcr-Abl
|
Cancer
|
|
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-125906
-
-
- HY-P99133
-
-
- HY-144983
-
-
- HY-144980
-
-
- HY-144985
-
-
- HY-128822
-
-
- HY-128813A
-
-
- HY-128815
-
-
- HY-128816A
-
-
- HY-128820
-
-
- HY-128819
-
-
- HY-128826
-
-
- HY-128812A
-
-
- HY-128813
-
-
- HY-128824
-
-
- HY-128812
-
-
- HY-128817
-
-
- HY-128825
-
-
- HY-128823
-
-
- HY-128818
-
-
- HY-128821
-
-
- HY-128816
-
-
- HY-128814
-
-
- HY-141486A
-
-
- HY-44012
-
-
- HY-44012A
-
-
- HY-P1887
-
|
p5 Ligand for Dnak and DnaJ
|
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-U00425
-
-
- HY-42424
-
|
(S,R,S)-AHPC-Me hydrochloride
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
-
|
(S,R,S)-AHPC-Me dihydrochloride
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-148179
-
-
- HY-44148
-
-
- HY-KT001
-
-
- HY-132943
-
-
- HY-136306
-
-
- HY-139655
-
-
- HY-152538
-
|
Antitumor agent-85
|
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-152537
-
|
Antitumor agent-84
|
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-139707
-
-
- HY-112078
-
|
(S,R,S)-AHPC-Me
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-107439
-
|
Thalidomide-O-amido-C8-NH2
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
-
|
Thalidomide-O-amido-C4-NH2
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.
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- HY-111824
-
|
VH032-thiol-C6-NH2
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.
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-
- HY-112618
-
|
Thalidomide-O-amido-C6-NH2
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.
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-
- HY-129608
-
|
Lenalidomide-acetylene-C5-COOH
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.
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-
- HY-115446A
-
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Lenalidomide-C4-NH2 hydrochloride
Cereblon ligand 1 hydrochloride; E3 ligase ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
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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.
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-
- HY-128716B
-
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Pomalidomide-PEG3-C2-NH2 hydrochloride
Cereblon ligand-Linker Conjugates 5 hydrochloride; E3 ligase ligand-Linker Conjugates 30 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
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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-130499
-
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ERRα Ligand-Linker Conjugates 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
|
-
- HY-P4205
-
-
- HY-147225
-
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TSPO Ligand-Linker Conjugates 1
|
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-103612
-
-
- HY-21930
-
|
Pomalidomide-PEG4-C-COOH
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-103614
-
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Thalidomide-O-amido-C8-NH2 TFA
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
-
|
Thalidomide-O-amido-C4-NH2 TFA
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-146077
-
-
- HY-146076
-
-
- HY-130521
-
|
Pomalidomide-amido-PEG3-C2-NH2
Cereblon ligand-Linker Conjugates 22; E3 ligase ligand-Linker Conjugates 55
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
|
-
- HY-129776
-
|
K-Ras ligand-Linker Conjugate 2
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-129775
-
|
K-Ras ligand-Linker Conjugate 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-148406
-
-
- HY-112618A
-
|
Thalidomide-O-amido-C6-NH2 TFA
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
-
|
Thalidomide-O-amido-PEG3-C2-NH2
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
-
-
- HY-103615
-
-
- HY-133189
-
-
- HY-130822
-
|
K-Ras ligand-Linker Conjugate 4
|
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
-
|
K-Ras ligand-Linker Conjugate 5
|
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
-
|
K-Ras ligand-Linker Conjugate 6
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-130707
-
|
K-Ras ligand-Linker Conjugate 3
|
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-41549
-
|
Pomalidomide-PEG4-Ph-NH2
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-128941
-
-
- HY-120217
-
|
VH032
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kdligand for protein by a linker to form PROTACs.
|
-
- HY-125554
-
-
- HY-125845
-
|
(S,R,S)-AHPC
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-101763A
-
|
(S,R,S)-AHPC hydrochloride
VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride
|
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
-
|
Methyl 3-aminopropanoate hydrochloride
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-147192
-
-
- HY-132856
-
-
- HY-128716
-
|
Pomalidomide-PEG3-C2-NH2
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
-
|
Pomalidomide-PEG4-C2-NH2
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-115560A
-
-
- HY-125884
-
-
- HY-N0927
-
|
(-)-Isocorypalmine
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-128846A
-
-
- HY-W087383
-
-
- HY-128846
-
-
- HY-130979
-
-
- HY-126458
-
-
- HY-148834
-
-
- HY-130716
-
-
- HY-128716A
-
|
Pomalidomide-PEG3-C2-NH2 TFA
Cereblon ligand-Linker Conjugates 5 TFA; E3 ligase ligand-Linker Conjugates 30 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-PEG3-C2-NH2 TFA (Cereblon Ligand-Linker Conjugates 5 (TFA)) is a synthetic E3 ligase ligand-linker conjugate comprising a Pomalidomide (HY-10984)-based cereblon ligand and a 3-unit PEG linker. Pomalidomide-PEG3-C2-NH2 TFA can be used for the synthesis of PROTACs.
|
-
- HY-133486
-
-
- HY-110402
-
|
(S,R,S)-AHPC TFA
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-134581A
-
|
Enpatoran hydrochloride
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-125846
-
|
(S,R,S)-AHPC-PEG1-OTs
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-125883
-
-
- HY-112617A
-
-
- HY-103611
-
-
- HY-138551A
-
-
- HY-144456
-
|
Xanthine oxidase-IN-5
|
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 drug-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
-
-
- HY-128832
-
-
- HY-114176
-
-
- HY-148476
-
|
Tri-GalNAc-DBCO
|
Others
|
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-103599
-
|
(S,R,S)-AHPC-PEG2-N3
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.
|
-
- HY-103604
-
|
(S,R,S)-AHPC-PEG4-NH2 hydrochloride
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-103601
-
|
(S,R,S)-AHPC-PEG4-N3
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.
|
-
- HY-103600
-
|
(S,R,S)-AHPC-PEG1-N3
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.
|
-
- HY-103598
-
|
(S,R,S)-AHPC-PEG3-N3
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.
|
-
- HY-103602
-
|
(S,R,S)-AHPC-PEG3-NH2 hydrochloride
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-133869
-
|
cGMP-HTL
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-109176
-
|
Giredestrant
GDC-9545
|
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-P3136A
-
-
- HY-P3136
-
-
- HY-W020035
-
-
- HY-N10634
-
-
- HY-130271
-
|
(S,R,S)-AHPC-PEG5-COOH
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-103602A
-
|
(S,R,S)-AHPC-PEG3-NH2
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
-
|
(S,R,S)-AHPC-PEG4-NH2
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-112600
-
-
- HY-128848
-
-
- HY-144734
-
-
- HY-142952
-
-
- HY-136424
-
|
GPI-1485
GM1485
|
Others
|
Neurological Disease
|
|
GPI-1485 (GM1485), a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke.
|
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
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-N8641
-
-
- HY-150202
-
-
- HY-P1438
-
-
- HY-128839
-
-
- HY-P3137
-
|
TRV056
|
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-103603
-
|
(S,R,S)-AHPC-PEG2-NH2 hydrochloride
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-112600A
-
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
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-112617
-
-
- HY-125843
-
|
Pomalidomide-PEG1-C2-N3
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.
|
-
- HY-148650
-
|
Sortilin antagonist 1
|
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-IN-2
|
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-122136
-
|
S26131
|
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-145368
-
|
Tri-GalNAc-NHS ester
|
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-103603A
-
|
(S,R,S)-AHPC-PEG2-NH2
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-138550A
-
-
- HY-135903
-
|
Giredestrant tartrate
GDC-9545 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-142954
-
-
- HY-114872
-
-
- HY-134761
-
|
EN4
|
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-148070
-
|
FLT3-IN-17
|
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
-
|
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc incorporates the Thalidomide based cereblon ligand and a linker. Thalidomide-O-amido-CH2-PEG3-CH2-NH-Boc can be used for the synthesis of PROTAC BET degrader. (From patent WO2017180417A1 compound s7).
|
-
- HY-126534
-
-
- HY-147559
-
-
- HY-147558
-
-
- HY-119102
-
|
BPU-11
|
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-130982
-
|
Lenalidomide-PEG3-iodine
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-PEG3-iodine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a 3-unit PEG linker. Lenalidomide-PEG3-iodine can be used in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
|
-
- HY-150235
-
|
Galectin-8N-IN-1
|
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-130798
-
-
- HY-P2159
-
-
- HY-148340
-
|
24RBPyBC
|
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-130813
-
-
- HY-109149
-
|
Lomardexamfetamine
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
-
-
- HY-P99021
-
-
- HY-141495A
-
|
Razpipadon
(-)-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-P1483
-
-
- HY-P1483B
-
-
- HY-W229874
-
|
EN106
|
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
-
-
- HY-148680
-
|
CL845-PAB-Ala-Val-C5-MC
|
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-148681
-
|
CL845-PAB-Ala-Val-PEG4-Azide
|
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.
|
-
- HY-D1605
-
|
BODIPY FL L-Cystine
|
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-133799
-
-
- HY-103606
-
|
(S,R,S)-AHPC-PEG6-C4-Cl
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-150029
-
|
CB1/2 agonist 3
|
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
-
|
ODN 2007
|
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-152152
-
|
JZP-MA-13
|
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-139516
-
|
AZD4694 Precursor
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-131028
-
|
Janelia Fluor® 646 TFA
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-131961
-
|
Triciferol
|
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
-
|
2,2'-Bipyridine
|
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
-
|
CL845
|
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-103607
-
|
(S,R,S)-AHPC-PEG2-C4-Cl
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-139403
-
-
- HY-145419
-
|
IRE1α kinase-IN-4
|
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
-
|
IRE1α kinase-IN-5
|
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
-
|
IRE1α kinase-IN-3
|
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-136363
-
|
MDR-652
|
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-136277
-
|
DFHO
|
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
-
|
Shield-1
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
-
-
- HY-108355
-
|
R59949
|
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
-
|
L-689560
|
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
-
|
A2AAR antagonist 1
|
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
-
|
(S)-Coriolic acid
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-151107
-
|
CBR Agonist-2
|
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-131295
-
-
- HY-133036
-
|
APJ receptor agonist 1
|
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-103608
-
|
(S,R,S)-AHPC-(C3-PEG)2-C6-Cl
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-135236
-
|
OXFBD04
|
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-113330
-
|
12S-HHT
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-103605
-
|
(S,R,S)-AHPC-C6-PEG3-C4-Cl
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-P1318
-
|
Ac-RYYRIK-NH2
|
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
-
|
L5-DA
|
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
-
|
Ac-RYYRIK-NH2 TFA
|
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
-
|
Veledimex
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-142521
-
|
BLT2 probe 1
|
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
|
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
-
|
PF-00356231 hydrochloride
|
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
-
|
CB1/2 agonist 2
|
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
-
|
UNC-2170
|
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
-
|
N-Descyclopropanecarbaldehyde Olaparib
|
E3 Ligase Ligand-Linker Conjugates
PARP
|
Cancer
|
|
N-Descyclopropanecarbaldehyde Olaparib is an analogue of Olaparib containing DOTA moiety. N-Descyclopropanecarbaldehyde Olaparib is a CRBN-based ligand for synthesizing novel dual EGFR and PARP PROTAC, DP-C-4. N-Descyclopropanecarbaldehyde Olaparib can be radiolabeled F-18 or fluorophore for positron emission tomography (PET) or optical imaging in several types of tumor.
|
-
- HY-151801
-
|
DIBA-Cy5
|
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-Dihydroxycholesterol
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
-
-
- HY-A0003B
-
|
Lenalidomide hemihydrate
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
-
|
Lenalidomide
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
-
|
Lenalidomide hydrochloride
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-151792
-
|
Pomalidomid-C6-PEG3-butyl-N3
|
PROTACs
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.
Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader.
|
-
- HY-132944
-
-
- HY-148152
-
-
- HY-120953
-
-
- HY-114434
-
-
- HY-148152A
-
-
- HY-130952
-
|
Thalidomide-O-C8-COOH
|
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
-
-
- HY-111842
-
-
- HY-113534
-
|
MV1
|
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
-
-
- HY-66007
-
-
- HY-148556
-
-
- HY-133484B
-
-
- HY-148142
-
-
- HY-17360
-
|
Tiotropium Bromide
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
-
|
Halo-DBCO
|
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-136272
-
-
- HY-136273
-
-
- HY-136274
-
-
- HY-N1427A
-
-
- HY-104046
-
-
- HY-139345
-
-
- HY-139549
-
|
Thalidomide-benzo
|
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
-
-
- HY-126457
-
|
Thalidomide-propargyl
|
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.
|
-
- HY-140844
-
-
- HY-141010
-
-
- HY-141014
-
-
- HY-131185
-
-
- HY-134983
-
-
- HY-D1027
-
|
Dansylcadaverine
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
-
-
- HY-138783A
-
-
- HY-138773
-
-
- HY-131874
-
-
- HY-138790
-
-
- HY-141015
-
-
- HY-138775
-
-
- HY-138774
-
-
- HY-131876
-
-
- HY-138860
-
-
- HY-131880
-
-
- HY-131889
-
-
- HY-138791
-
-
- HY-140055
-
-
- HY-113413
-
-
- HY-112797
-
-
- HY-138771
-
-
- HY-138782
-
-
- HY-138778
-
-
- HY-138776
-
-
- HY-138780
-
-
- HY-141010A
-
-
- HY-130950
-
-
- HY-138777
-
-
- HY-138772
-
-
- HY-130951
-
-
- HY-141887
-
-
- HY-138781
-
-
- HY-101909
-
-
- HY-P1205A
-
|
MCH(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
-
-
- HY-44177
-
-
- HY-P99575
-
|
Tarlatamab
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-132208
-
-
- HY-138784
-
-
- HY-130965
-
-
- HY-138784A
-
-
- HY-131888A
-
-
- HY-141010B
-
-
- HY-W076696
-
|
Lenalidomide-4-OH
|
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
-
-
- HY-130964B
-
-
- HY-136164
-
-
- HY-133484
-
-
- HY-138845
-
-
- HY-131888
-
-
- HY-133816A
-
-
- HY-136162A
-
-
- HY-133485B
-
-
- HY-139539
-
|
Thalidomide-5-COOH
|
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
-
-
- HY-133817
-
-
- HY-130949
-
-
- HY-138858A
-
-
- HY-134986
-
-
- HY-138848A
-
-
- HY-133817A
-
-
- HY-130948
-
-
- HY-138787
-
-
- HY-133816
-
-
- HY-138859
-
-
- HY-131867
-
-
- HY-138789
-
-
- HY-138848
-
-
- HY-23095
-
|
Thalidomide-5-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-138846A
-
-
- HY-130708
-
|
UNC6852
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
UNC6852 is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, with an IC50 of 247 nM for EED.
|
-
- HY-138858
-
-
- HY-136237
-
-
- HY-130963
-
-
- HY-138847A
-
-
- HY-129704B
-
-
- HY-135250
-
-
- HY-138846
-
-
- HY-133485
-
-
- HY-134985
-
-
- HY-129704
-
-
- HY-136162
-
-
- HY-138788
-
-
- HY-139547
-
|
Thalidomide-5,6-Cl
|
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
-
|
dFKBP-1
|
PROTACs
FKBP
|
Cancer
|
|
dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker.
|
-
- HY-138859A
-
-
- HY-W077589A
-
|
Lenalidomide-5-aminomethyl
|
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-138853
-
-
- HY-138882
-
|
Lenalidomide-4-aminomethyl
|
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-137538
-
-
- HY-138789A
-
-
- HY-138849A
-
-
- HY-138882A
-
-
- HY-111879
-
|
Biotin-BS
|
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
-
-
- HY-129704A
-
-
- HY-134984A
-
-
- HY-134984
-
-
- HY-138850A
-
-
- HY-131388
-
-
- HY-138850
-
-
- HY-138881
-
|
Lenalidomide-6-F
|
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
-
|
Lenalidomide-5-Br
|
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
-
-
- HY-131998
-
-
- HY-138852
-
-
- HY-136161
-
-
- HY-130639
-
-
- HY-137537
-
-
- HY-138853A
-
-
- HY-128767
-
-
- HY-138851A
-
-
- HY-141423
-
-
- HY-138849
-
-
- HY-139540
-
|
Pomalidomide-6-OH
|
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
-
-
- HY-138788A
-
-
- HY-15238
-
-
- HY-111878
-
|
BzNH-BS
|
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
-
-
- HY-107438A
-
-
- HY-17360S
-
|
Tiotropium-d3 bromide
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
-
|
Nemadipine-A
|
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
-
-
- HY-130948B
-
-
- HY-107439A
-
-
- HY-17360S1
-
|
Tiotropium-d6 bromide
BA679 BR-d6
|
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
-
-
- HY-112618B
-
-
- HY-W093272
-
|
Thalidomide-5,6-F
|
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
-
-
- HY-138786A
-
-
- HY-141423A
-
-
- HY-138785A
-
-
- HY-138785
-
-
- HY-122694A
-
-
- HY-114420
-
-
- HY-138862
-
-
- HY-136163A
-
-
- HY-131159
-
|
Thalidomide-O-C8-Boc
|
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
-
-
- HY-130981
-
-
- HY-138856
-
-
- HY-138854A
-
-
- HY-112599B
-
-
- HY-138855A
-
-
- HY-122710
-
-
- HY-136183
-
-
- HY-137531
-
-
- HY-123324
-
|
Pomalidomide-5-OH
5-Hydroxy pomalidomide; CC-17368
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-OH (5-hydroxy pomalidomide) is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-138854
-
-
- HY-138855
-
-
- HY-138857A
-
-
- HY-138857
-
-
- HY-131308
-
-
- HY-100583
-
-
- HY-75035
-
-
- HY-W011051
-
-
- HY-P0183
-
-
- HY-123215
-
|
CC-17369
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
-
-
- HY-114176B
-
-
- HY-133144
-
|
Lenalidomide-OH
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
|
-
- HY-122710A
-
-
- HY-107442
-
-
- HY-138861A
-
-
- HY-114176A
-
-
- HY-138861
-
-
- HY-129703B
-
-
- HY-139541
-
|
Pomalidomide-5-O-CH3
|
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-5-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-136165
-
-
- HY-129703
-
-
- HY-130988A
-
-
- HY-139542
-
|
Pomalidomide-6-O-CH3
|
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-107471
-
|
CB2 receptor agonist 3
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
-
-
- HY-108258
-
|
PSN 375963
|
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
-
|
ASN04421891
|
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
-
-
- HY-108258A
-
|
PSN 375963 hydrochloride
|
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
-
|
Janelia Fluor® 646, Maleimide
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
-
-
- HY-130197
-
-
- HY-141481
-
-
- HY-111663
-
-
- HY-106547
-
-
- HY-152270
-
-
- HY-15265
-
-
- HY-131959
-
-
- HY-131872
-
-
- HY-122825
-
|
SNIPER(ER)-110
|
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
-
|
CMP8
|
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
-
-
- HY-131318
-
|
Lenalidomide-I
|
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
-
|
Thalidomide-5-PEG2-Cl
|
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
-
-
- HY-100486
-
|
BTTAA
|
Others
|
Others
|
|
BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
|
-
- HY-114229
-
-
- HY-131717
-
|
Thalidomide-NH-CH2-COOH
|
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-P99325
-
|
Toralizumab
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 drug, has the potential for active systemic lupus erythematosus (SLE) research.
|
-
- HY-122725B
-
-
- HY-131190
-
-
- HY-N2388
-
|
Auraptene
|
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
-
-
- HY-131646
-
-
- HY-43722
-
|
Lenalidomide-Br
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
|
-
- HY-122725A
-
-
- HY-130269
-
|
β-Naphthoflavone-CH2-OH
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-110399
-
-
- HY-A0266
-
-
- HY-P99723
-
-
- HY-144768
-
|
Chol-TPP
|
Liposome
|
Others
|
|
Chol-TPP, a mitochondria targeting liposome ligand could be used in pH-redox responsive.
|
-
- HY-116677
-
-
- HY-N3171A
-
-
- HY-W129872
-
-
- HY-132288
-
|
Pom-8PEG
|
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
-
-
- HY-139545
-
-
- HY-P1380A
-
|
Difopein TFA
|
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
-
|
5,5'-Dinitro BAPTA AM
|
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-69220
-
|
7-Octynoic acid
|
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.
|
-
- HY-131189
-
|
N-Boc-SBP-0636457-OH
|
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
-
-
- HY-131186
-
-
- HY-133699
-
|
Pomalidomide-PEG4-COOH
|
Ligands for E3 Ligase
|
Others
|
|
Pomalidomide-PEG4-COOH is a E3 ligase ligand-linker conjugate. Pomalidomide-PEG4-COOH contains the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology (extracted from patent WO2017184995A1).
|
-
- HY-143499
-
|
hMAO-B-IN-3
|
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 drug-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-135324
-
-
- HY-32339
-
-
- HY-N0277
-
-
- HY-142240
-
-
- HY-145938
-
|
OncoFAP
|
FAP
|
Cancer
|
|
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
|
-
- HY-112609
-
-
- HY-136006B
-
-
- HY-136186
-
-
- HY-130711B
-
-
- HY-136008
-
-
- HY-125845A
-
|
(S,S,S)-AHPC hydrochloride
(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
-
|
Br-C10-methyl ester
|
PROTAC Linkers
|
Cancer
|
|
Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432). PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein.
|
-
- HY-133487A
-
-
- HY-112398
-
-
- HY-103628
-
-
- HY-101861
-
|
Miridesap
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
-
|
DAA-1106
|
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-139620
-
|
MS83
|
PROTACs
|
Cancer
|
|
MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
|
-
- HY-P4198
-
-
- HY-15264
-
|
MC 1046
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-141729
-
|
Biotin-NH-PSMA-617
|
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
-
|
MRTX849 acid
|
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-P2543
-
|
Neuropeptide Y (3-36) (human, rat)
|
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
-
|
Galantide
|
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
-
-
- HY-34544
-
|
2-Hexylthiophene
|
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-129941
-
-
- HY-129941A
-
-
- HY-P3676
-
-
- HY-131178
-
|
HG-7-85-01-NH2
|
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
-
-
- HY-132938
-
-
- HY-111850
-
-
- HY-139548
-
-
- HY-139482
-
|
tri-GalNAc-COOH
|
LYTACs
|
Cancer
|
|
tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.
|
-
- HY-100275
-
-
- HY-15266
-
|
24R-Calcipotriol
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
-
-
- HY-136184
-
-
- HY-129652
-
|
Halo PROTAC 1
|
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
-
-
- HY-108374
-
|
4-Azidobutylamine
|
PROTAC Linkers
|
Cancer
|
|
4-Azidobutylamine is a PROTAC linker, which refers to the alkyl chain composition. 4-Azidobutylamine 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-111844
-
|
PROTAC RAR Degrader-1
|
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-103603B
-
-
- HY-103223
-
|
Phortress
NSC 710305
|
Cytochrome P450
|
Cancer
|
|
Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1.
|
-
- HY-N2540
-
-
- HY-112588
-
-
- HY-P2277
-
-
- HY-16785A
-
-
- HY-107444
-
-
- HY-P2278
-
-
- HY-D1288
-
-
- HY-U00250
-
-
- HY-101601
-
-
- HY-114907
-
|
4',5'-Dibromofluorescein
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-130988
-
|
Ipatasertib-NH2
GDC-0068-NH2; RG7440-NH2
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
|
-
- HY-130854
-
|
Thalidomide-NH-C6-NH-Boc
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
|
-
- HY-111254
-
|
GQ-16
|
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
-
|
Thalidomide-NH-PEG2-C2-NH-Boc
|
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-P1186
-
-
- HY-147311
-
-
- HY-112156
-
-
- HY-112376
-
-
- HY-112377
-
-
- HY-112155
-
-
- HY-A0077AS
-
-
- HY-108652
-
-
- HY-134440
-
-
- HY-111872
-
|
SNIPER(ABL)-020
|
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-111857
-
-
- HY-111556
-
|
BSJ-03-123
|
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
-
|
Cyclo(RADfK)
|
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
-
|
CCW16
|
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
-
-
- HY-P1037
-
-
- HY-129774
-
|
Phthalimide-PEG4-MPDM-OH
|
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-130617
-
|
Pomalidomide-amido-C1-Br
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity.
|
-
- HY-130715
-
|
tert-Butyl 11-aminoundecanoate
|
PROTAC Linkers
|
Cancer
|
|
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-114407
-
|
TD-428
|
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-129773
-
|
Phthalimide-PEG4-PDM-OTBS
|
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-D1441
-
-
- HY-P1123
-
|
MEDICA16
|
ATP Citrate Lyase
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120.
|
-
- HY-P0023
-
|
Cyclo(-RGDfK)
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-P1299A
-
|
UFP-101 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pKi of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect.
|
-
- HY-120738
-
|
p-MPPI hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
|
-
- HY-P1299
-
|
UFP-101
|
Opioid Receptor
|
Neurological Disease
|
|
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pKi of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect.
|
-
- HY-117829
-
-
- HY-P0023A
-
|
Cyclo(-RGDfK) TFA
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-12436
-
|
NTRC-824
|
Neurotensin Receptor
|
Neurological Disease
|
|
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC50 of 38 nM and a Ki of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM).
|
-
- HY-111593
-
-
- HY-112895A
-
-
- HY-132858
-
-
- HY-133137A
-
|
SJF620 hydrochloride
|
PROTACs
Btk
|
Cancer
|
|
SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
|
-
- HY-135558
-
-
- HY-133137
-
|
SJF620
|
PROTACs
Btk
|
Cancer
|
|
SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.
|
-
- HY-112375
-
|
AT6
|
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
-
|
BML-190
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-148362
-
-
- HY-N4194
-
|
Glabrone
|
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
-
-
- HY-111852
-
-
- HY-103633
-
-
- HY-129405
-
-
- HY-P9904
-
-
- HY-W011051S1
-
-
- HY-P99641
-
|
Gilvetmab
|
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
-
-
- HY-13751
-
-
- HY-N10062
-
|
Amakusamine
|
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 cells.
|
-
- HY-122577
-
-
- HY-W011051S
-
-
- HY-124625
-
-
- HY-141495
-
-
- HY-144323
-
|
YF135
|
PROTACs
PERK
|
Cancer
|
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
|
-
- HY-143418
-
|
SARS-CoV-2-IN-17
|
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-136055
-
-
- HY-125876
-
|
PROTAC Bcl2 degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
|
-
- HY-134581
-
|
Enpatoran
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-130652
-
|
Pomalidomide 4'-PEG3-azide
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient PARP1 degrader based on Rucaparib by using the PROTAC approach.
|
-
- HY-144825
-
|
Chol-CTPP
|
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-2-IN-16
|
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-133136
-
-
- HY-111758
-
|
PROTAC B-Raf degrader 1
|
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-132939
-
-
- HY-111849
-
-
- HY-N8460A
-
-
- HY-P99625
-
-
- HY-N8460
-
-
- HY-15329
-
|
Maxacalcitol-d6
|
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-W048671
-
-
- HY-16954
-
-
- HY-115568
-
|
BETd-246
|
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
-
-
- HY-136280
-
|
Panamesine
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
-
-
- HY-139681
-
-
- HY-13751A
-
-
- HY-111851
-
|
SNIPER(ABL)-049
|
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-129772
-
|
Phthalimide-PEG3-C2-OTs
|
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
-
|
NH2-C4-NH-Boc
|
PROTAC Linkers
|
Cancer
|
|
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-P99437
-
|
Anbenitamab
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
-
|
Sphingosine-1-phosphate
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-P0272
-
|
Peptide T
|
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
-
-
- HY-P1464
-
|
Amylin, amide, rat
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
-
|
Emapunil
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
-
-
- HY-N6253
-
|
Pinoresinol
(+)-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
-
|
Phen-DC3
|
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
-
|
SNIPER(ABL)-013
|
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
-
|
Carlumab
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-W011051S2
-
-
- HY-12452
-
-
- HY-111855
-
-
- HY-122246
-
-
- HY-148272
-
-
- HY-143315
-
-
- HY-P1125
-
-
- HY-150537
-
|
AChE/GSK-3β-IN-1
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research.
|
-
- HY-121295
-
|
Roseoflavin
|
Bacterial
|
Infection
|
|
Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties.
|
-
- HY-100552
-
|
VUF10166
|
5-HT Receptor
|
Neurological Disease
|
|
VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM.
|
-
- HY-117726
-
-
- HY-B2087
-
-
- HY-130852
-
-
- HY-111413
-
-
- HY-147354
-
|
TriGalNAc CBz
|
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
-
-
- HY-106025
-
|
Radequinil
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
-
|
XY028-133
|
PROTACs
CDK
|
Cancer
|
|
XY028-133 (example 14) is a PROTAC-based CDK4/6 degrader with anti-tumor activity, which consists of ligands for von Hippel-Lindau and CDK.
|
-
- HY-P0272A
-
|
Peptide T TFA
|
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
-
-
- HY-D1398
-
|
LtIA-F
|
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
-
|
EC0489
|
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-drug conjugate (SMDC).
|
-
- HY-130850
-
-
- HY-111859
-
|
SNIPER(ABL)-058
|
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
-
|
SNIPER(ABL)-015
|
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-131030
-
|
Janelia Fluor® 669, SE
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 JF669−HaloTag 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-131168
-
-
- HY-129619
-
|
SNIPER(ER)-87
|
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-P99307
-
|
Namilumab
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
-
|
BiCAPPA
|
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
-
|
EPQpYEEIPIYL
|
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-101380A
-
-
- HY-P99852
-
|
Dilpacimab
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-147021A
-
-
- HY-114228
-
-
- HY-112617B
-
-
- HY-111413A
-
-
- HY-111873
-
|
SNIPER(ABL)-019
|
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
|
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
-
|
Betifisolimab
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-P3108
-
-
- HY-111861
-
|
SNIPER(ABL)-024
|
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
|
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-P99375
-
|
Narnatumab
IMC-RON8; LY3012219; Anti-MSPR/RON/CD136 Reference Antibody (narnatumab)
|
Others
|
Cancer
|
|
Narnatumab (IMC-RON8) is a neutralizing human monoclonal antibody that blocks RON binding to its ligand, macrophage-stimulating protein (MSP), with a Kd of 32 pM. Narnatumab can be used for the research of cancer.
|
-
- HY-111862
-
|
SNIPER(ABL)-044
|
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-16785B
-
|
Veledimex (S enantiomer)
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
-
|
CCT251236
|
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-135345
-
|
PROTAC FKBP Degrader-3
|
PROTACs
FKBP
|
Cancer
|
|
PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.
|
-
- HY-150158
-
|
TMX-201
|
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-136006
-
-
- HY-133487B
-
-
- HY-136006A
-
-
- HY-130618
-
|
Boc-C1-PEG3-C4-OH
|
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
-
-
- HY-130711A
-
|
(S,R,S)-AHPC-C3-NH2 TFA
VH032-C3-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
|
-
- HY-130711
-
|
(S,R,S)-AHPC-C3-NH2
VH032-C3-NH2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader.
|
-
- HY-15238A
-
-
- HY-139999
-
|
LCL-PEG3-N3
|
Ligands for E3 Ligase
|
Cancer
|
|
LCL-PEG3-N3 is a decoy oligonucleotide ligand for E3 ligase which can be used for developing chimeric molecules LCL-ER(dec), degrading the estrogen receptor.
|
-
- HY-122562
-
-
- HY-123937
-
|
THAL-SNS-032
|
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
-
-
- HY-111876
-
|
SNIPER(TACC3)-1
|
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
-
-
- HY-130845
-
-
- HY-130714
-
|
TD-165
|
PROTACs
|
Cancer
|
|
TD-165 is a PROTAC-based cereblon (CRBN) degrader. TD-165 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.
|
-
- HY-100686
-
|
U93631
|
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-146180
-
|
FSDD0I
|
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
-
|
PK 11195
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
-
|
FSDD1I
|
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
-
|
Atrovastatin-PEG3-FITC
|
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
-
|
BODIPY 630/650X
|
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
-
-
- HY-139999A
-
-
- HY-111877
-
|
SNIPER(TACC3)-2
|
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
-
-
- HY-128845
-
|
PROTAC CRBN Degrader-1
|
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-136257
-
|
CMP98
|
PROTACs
|
Others
|
|
CMP98, a PROTAC, is unable to induce degradation of VHL. CMP98 can be used as a negative control compound for CM11. CMP98 consists of two von Hippel-Lindau ligands on their active domain.
|
-
- HY-101838
-
|
dBET1
|
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
-
|
FSDD3I
|
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-148137
-
-
- HY-147532
-
|
CB2R probe 1
|
Cannabinoid Receptor
|
Cancer
|
|
CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells.
|
-
- HY-N10526
-
|
Isoglobotriaose
Gala-3Galb-4Glc
|
Others
|
Others
|
|
Isoglobotriaose (Gala-3Galb-4Glc) is a glycosphingolipid found in mammalian tissues. Isoglobotriaose is an analogue of Globotriaose, the ganglioside derivatives of them locate in difference position of small intestine, isoglobotriaosylceramide is restricted to the nonepithelial residue, while globotriaosylceramide is in both compartments.
|
-
- HY-13992
-
|
AP20187
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
-
-
- HY-111863
-
|
SNIPER(ABL)-047
|
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-22024
-
|
5-Hydroxyflavone
|
Others
|
Cancer
|
|
5-Hydroxyflavone, a flavonoid ligand, shows no cytotoxic activity against MCF-7, FaDU, MDA-MB-435S, U87, RPE-1, and HEK293 cells.
|
-
- HY-101622
-
-
- HY-103632
-
-
- HY-103222
-
|
DiMNF
3',4'-Dimethoxy-αNF
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent.
|
-
- HY-138946
-
|
XY028-140
|
CDK
PROTACs
|
Cancer
|
|
XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells.
|
-
- HY-108496S
-
|
Sphingosine-1-phosphate-d7
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
-
|
Thalidomide-NH-C4-NH2 TFA
|
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
-
|
GPI-1046
|
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
-
-
- HY-130816
-
|
(S,R,S)-AHPC-O-Ph-PEG1-NH2
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
-
|
PROTAC CDK2/9 Degrader-1
|
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-135250B
-
-
- HY-114305
-
|
A1874
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
A1874 is a nutlin-based (MDM2 ligand) and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
|
-
- HY-P2267
-
|
LDV
|
Integrin
|
Others
|
|
LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC. LDV is a α4β1 integrin (VLA-4) ligand, and binds α4β1 integrin in leukemia cells.
|
-
- HY-P1166
-
|
UFP-803
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
UFP-803 is a potent urotensin-II receptor (UT) ligand. UFP-803 has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.
|
-
- HY-112718
-
-
- HY-103691
-
|
ARN5187
|
Autophagy
Apoptosis
|
Cancer
|
|
ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis.
|
-
- HY-N6777
-
|
Penicillic acid
|
Caspase
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8.
|
-
- HY-111871
-
|
SNIPER(ABL)-033
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
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 of 0.3 μM.
|
-
- HY-103691A
-
|
ARN5187 trihydrochloride
|
Autophagy
Apoptosis
|
Cancer
|
|
ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.
|
-
- HY-101059
-
|
FGIN 1-27
|
Others
|
Neurological Disease
|
|
FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions.
|
-
- HY-134184
-
-
- HY-131232
-
-
- HY-129363
-
-
- HY-W013788
-
-
- HY-103025
-
|
Methylprednisolone aceponate
ZK 91588; MPA
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Methylprednisolone aceponate (ZK 91588) is a glucocorticoid and anti-inflammatory agent with weak systemic effects. Methylprednisolone aceponate is a selective glucocorticoid receptor Ligand.Methylprednisolone aceponate can be used for research of eczema and other inflammatory skin disorders.
|
-
- HY-132603
-
|
AB-729
|
Small Interfering RNA (siRNA)
HBV
|
Infection
|
|
AB-729 is a siRNA specifically designed to inhibit viral replication and reduces HBV antigens. AB-729 conjugates to a trimer of N-acetylgalactosamine (GalNAc) ligand that promotes uptake into hepatocytes via the asialoglycoprotein receptor (ASGR).
|
-
- HY-104006
-
|
CYM51010
|
Opioid Receptor
|
Neurological Disease
|
|
CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC50 of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms.
|
-
- HY-N0499
-
|
Cyanidin Chloride
IdB 1027
|
RANKL/RANK
|
Cancer
|
|
Cyanidin Chloride (IdB 1027), a subclass of anthocyanin, displays antioxidant and anti-carcinogenesis properties. Cyanidin Chloride (IdB 1027) inhibits osteoclast formation, hydroxyapatite resorption, and receptor activator of NF-κB ligand (RANKL)-induced osteoclast marker gene expression.
|
-
- HY-115715
-
|
EN219
|
E1/E2/E3 Enzyme
|
Cancer
|
|
EN219 is a moderately selective synthetic covalent ligand against an N-terminal cysteine (C8) of RNF114 with an IC50 of 470 nM. EN219 inhibits RNF114-mediated autoubiquitination and p21 ubiquitination.
|
-
- HY-148859
-
-
- HY-112495
-
|
VH032-PEG5-C6-Cl
HaloPROTAC 2
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-130619
-
|
Boc-C1-PEG3-C4-OBn
|
PROTAC Linkers
|
Cancer
|
|
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-136163
-
-
- HY-148118
-
|
Tri-GalNAc(OAc)3
|
LYTACs
|
Cancer
|
|
Tri-GalNAc(OAc)3 is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera.
|
-
- HY-P99480
-
|
Bintrafusp alfa
M 7824; MSB0011359C
|
TGF-β Receptor
|
Cancer
|
|
Bintrafusp alfa (M 7824) is a first-in-class bifunctional fusion protein composed of the extracellular domain of TGF-βRII fused to a human IgG1 mAb blocking programmed cell death ligand. Bintrafusp alfa can be used for the research of cancer.
|
-
- HY-109155
-
|
Paltusotine
CRN00808
|
Somatostatin Receptor
|
Endocrinology
|
|
Paltusotine (CRN00808) is an orally active, nonpeptide selective somatostatin type 2 (SST2) receptor agonist. Paltusotine has the potential for maintaining GH and IGF-1 levels after depot somatostatin receptor ligand therapy.
|
-
- HY-138665
-
|
HHS-0701
|
Prostaglandin Receptor
|
Endocrinology
|
|
HHS-0701, a sulfur-triazole exchange (SuTEx) ligand, is a potent tyrosine-reactive prostaglandin reductase 2 (PTGR2) inhibitor. HHS-0701 blocks PTGR2 metabolism of the lipid substrate 15-Keto-PGE2.
|
-
- HY-128605
-
|
PD-1-IN-22
|
PD-1/PD-L1
|
Cancer
|
|
PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM.
|
-
- HY-148103
-
|
SR12418
|
REV-ERB
|
Inflammation/Immunology
|
|
SR12418 is a REV-ERB-specific synthetic ligand with IC50s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research.
|
-
- HY-107737
-
-
- HY-108372
-
|
Boc-C5-O-C5-O-C6-Cl
PROTAC Linker 2
|
PROTAC Linkers
|
Cancer
|
|
Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
|
-
- HY-P99936
-
|
Elgemtumab
LJM716
|
EGFR
|
Cancer
|
|
Elgemtumab(LJM716) is a fully human IgG monoclonal antibody. Elgemtumab can specifically bind to HER3, block ligand-dependent and independent HER3 signal transduction and cell proliferation, and has good anti-tumor potential.
|
-
- HY-P1166A
-
|
UFP-803 TFA
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
UFP-803 TFA is a potent urotensin-II receptor (UT) ligand. UFP-803 TFA has lower residual agonist activity, so it may be an important tool for the investigations on the role played by the UT system in physiology and pathology.
|
-
- HY-B2078A
-
|
Eprazinone dihydrochloride
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.
|
-
- HY-N2078
-
|
Yamogenin
Neodiosgenin
|
LXR
|
Metabolic Disease
|
|
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
|
-
- HY-P3440
-
|
WL12
|
PD-1/PD-L1
|
Cancer
|
|
WL12 is a specifically targeting programmed death ligand 1 (PD-L1) binding peptide. WL12 can be radiolabeled by different radionuclides, generating radiotracers, which can assess the tumor PD-L1 expression.
|
-
- HY-107447S
-
-
- HY-44432
-
-
- HY-141550
-
|
BPK-25
|
Others
|
Inflammation/Immunology
|
|
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
|
-
- HY-148118A
-
|
Tri-GalNAc(OAc)3 TFA
|
LYTACs
|
Cancer
|
|
Tri-GalNAc(OAc)3 TFA is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera.
|
-
- HY-128842
-
-
- HY-W040270
-
|
Amino-PEG10-amine
|
PROTAC Linkers
|
Cancer
|
|
Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
|
-
- HY-128843
-
-
- HY-128840
-
-
- HY-151515
-
-
- HY-23999
-
|
BI-0115
|
LOX-1
|
Cardiovascular Disease
|
|
BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain.
|
-
- HY-146020
-
|
Topoisomerase IIα-IN-1
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines.
|
-
- HY-128841
-
-
- HY-P1197
-
-
- HY-148671
-
-
- HY-101310
-
|
SYM 2081
|
iGluR
|
Neurological Disease
|
|
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively.
|
-
- HY-120210
-
|
XY018
|
ROR
|
Cancer
Inflammation/Immunology
|
|
XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
|
-
- HY-108571
-
|
CP-775146
|
PPAR
|
Metabolic Disease
|
|
CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway.
|
-
- HY-108813
-
|
Belatacept
BMS 224818; LEA 29Y
|
Others
|
Inflammation/Immunology
|
|
Belatacept (BMS 224818) is a selective T-cell costimulation blocker. Belatacept binds to CD 80/86 ligands and thereby inhibits the CD-28-mediated T-cell costimulation. Belatacept can be used in the research of Immunosuppression in organ transplants.
|
-
- HY-130612
-
|
PROTAC BRD2/BRD4 degrader-1
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.
|
-
- HY-103235
-
|
NPEC-caged-(S)-AMPA
|
iGluR
|
Neurological Disease
|
|
NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor.
|
-
- HY-13682B
-
|
Mifamurtide sodium
MTP-PE sodium; L-MTP-PE sodium; CGP 19835 sodium
|
NOD-like Receptor (NLR)
|
Cancer
Inflammation/Immunology
|
|
Mifamurtide sodium (MTP-PE sodium), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide sodium, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide sodium has the potential for osteosarcoma research.
|
-
- HY-135034
-
|
UMB68 sodium
|
Others
|
Neurological Disease
|
|
UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [ 3H]NCS-382 with an IC50 of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds.
|
-
- HY-126534A
-
-
- HY-13682
-
|
Mifamurtide
MTP-PE; L-MTP-PE; CGP 19835
|
NOD-like Receptor (NLR)
|
Cancer
Inflammation/Immunology
|
|
Mifamurtide (MTP-PE), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide has the potential for osteosarcoma research.
|
-
- HY-135250A
-
-
- HY-129523
-
|
PROTAC K-Ras Degrader-1
|
PROTACs
Ras
|
Cancer
|
|
PROTAC K-Ras Degrader-1 (Compound 518) is a PROTAC. PROTAC K-Ras Degrader-1 can effectively degrades K-Ras based on Cereblon E3 ligand, exhibits ≥70% degradation efficacy in SW1573 cells.
|
-
- HY-D1092
-
|
DiBAC4(5)
|
Fluorescent Dye
|
Neurological Disease
|
|
DiBaC4(5) is a fluorescent voltage-sensitive dye that can be used to monitor the transmembrane potentials when Papain-dissociated retinal cells from adult zebrafish were exposed to GABAergic ligands. DiBaC4(5) is a potential-sensitive fluorescence dye.
|
-
- HY-107443
-
-
- HY-118998
-
|
TX2-121-1
|
EGFR
|
Cancer
|
|
TX2-121-1, a potent and selective Her3 (ErbB3) bivalent ligand, can induce degradation of Her3 with an IC50 of 49 nM. TX2-121-1 can inhibit Her3-dependent signaling.
|
-
- HY-136160
-
-
- HY-130411
-
|
Amino-PEG11-amine
|
PROTAC Linkers
|
Cancer
|
|
Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
|
-
- HY-139831
-
|
Galectin-8-IN-1
|
Galectin
|
Cancer
|
|
Galectin-8-IN-1 is a selective ligand for the galectin-8 N-terminal domain (galectin-8N), with a Kd of 48 μM and 15-fold selectivity over galectin-3 and even better selectivity over the other mammalian galectins.
|
-
- HY-128838
-
-
- HY-122826
-
-
- HY-P9977
-
|
Amivantamab
JNJ-61186372
|
EGFR
|
Cancer
|
|
Amivantamab (JNJ-61186372) is a human EGFR-MET bispecific antibody with immune anticancer activity. Amivantamab inhibits ligand binding, promotes endocytosis and degradation of receptor-antibody complexes, and induces Fc-dependent cytokinesis in macrophages and antibody-dependent cytotoxicity in natural killer cells.
|
-
- HY-133737
-
-
- HY-134582
-
|
dCBP-1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
|
-
- HY-17537
-
|
APY29
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
|
-
- HY-147619
-
|
FGFR-IN-4
|
FGFR
|
Cancer
|
|
FGFR-IN-4 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-4 has the potential for the research of cancer diseases (extracted from patent WO2022033532A1, compound 20).
|
-
- HY-P99114
-
|
Sugemalimab
|
PD-1/PD-L1
|
Cancer
|
|
Sugemalimab is a fully human, full length, anti-programmed death ligand 1 (PD-L1) immunoglobulin G4 (IgG4) monoclonal antibody (mAb). Sugemalimab shows anticancer activities and can be used for non-small cell lung cancer research.
|
-
- HY-P1197A
-
-
- HY-13956S
-
|
Pioglitazone-d4
U 72107-d4
|
PPAR
Ferroptosis
|
Cancer
Metabolic Disease
|
|
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
|
-
- HY-147620
-
|
FGFR-IN-5
|
FGFR
|
Cancer
|
|
FGFR-IN-5 is a potent inhibitor of FGFR. Fibroblast growth factor receptor (FGFR) is a tyrosine kinase receptor that binds to fibroblast growth factor ligands. FGFR-IN-5 has the potential for the research of cancer diseases (extracted from patent WO2022042612A1, compound 3).
|
-
- HY-130835
-
|
FKBP12 PROTAC RC32
RC32
|
PROTACs
FKBP
|
Cancer
|
|
FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an Cereblon E3 ubiquitin ligase (Pomalidomide; HY-10984).
|
-
- HY-134591
-
-
- HY-N0368
-
|
Linalool
|
iGluR
Apoptosis
Endogenous Metabolite
|
Cancer
Cardiovascular Disease
|
|
Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity.Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome.
|
-
- HY-108822
-
|
Rilonacept
Arcalyst; IL 1 Trap; Interleukin 1 Trap
|
Interleukin Related
|
Inflammation/Immunology
|
|
Rilonacept (Arcalyst), a dimeric fusion protein, is a interleukin 1 inhibitor. Rilonacept consists of the ligand-binding domains of the extracellular portions of the IL-1R components linked to the Fc portion of human IgG1. Rilonacept can be used for the research of cryopyrin-associated periodic syndromes.
|
-
- HY-130257
-
|
CP5V
|
PROTACs
|
Cancer
|
|
CP5V is a PROTAC connected by ligands for von Hippel-Lindau and CDK, which specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. CP5V induces mitotic inhibition and suppresses cancer cell proliferation.
|
-
- HY-114405
-
|
SJFδ
|
PROTACs
p38 MAPK
Autophagy
|
Cancer
|
|
SJFδ is a 10-atom linker PROTAC based on von Hippel-Lindau ligand. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ.
|
-
- HY-101043
-
|
4-PPBP maleate
|
Sigma Receptor
iGluR
|
Neurological Disease
|
|
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection.
|
-
- HY-P4095
-
|
NoxaBH3
|
CXCR
|
Cancer
|
|
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitory activity against Mcl-1. NoxaBH3 binds to the endogenous CXCR4 ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells.
|
-
- HY-P1366
-
|
des-Gln14-Ghrelin
|
GHSR
|
Metabolic Disease
|
|
des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
|
-
- HY-P99274
-
|
Xentuzumab
BI 836845; Anti-Human IGF1 and IGF2 Recombinant Antibody
|
IGF-1R
|
Cancer
|
|
Xentuzumab (Anti-Human IGF1 and IGF2 Recombinant Antibody; BI836845) is a recombinant a humanized monoclonal antibody that targets IGF ligands IGF1 and IGF2. Xentuzumab inhibits both of IGF1 and IGF2 growth-promoting signalling and suppresses AKT activation.
|
-
- HY-N0443
-
|
N-Methylcytisine
Caulophylline
|
nAChR
|
Inflammation/Immunology
|
|
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia.
|
-
- HY-12650
-
|
Mirogabalin
DS5565
|
Calcium Channel
|
Neurological Disease
|
|
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
|
-
- HY-141799
-
-
- HY-136406
-
|
Bongkrekic acid
|
ATP Synthase
|
Cancer
Infection
|
|
Bongkrekic acid is a mitochondrial toxin secreted by the bacteria Pseudomonas cocovenenans. Bongkrekic acid specific ligand for mitochondrial adenine nucleotide translocase (ANT) rather than the electron transport chain. Bongkrekic acid has to cross the mitochondrial inner membrane to produce its inhibitory effect on ADP/ATP transport.
|
-
- HY-W013754
-
|
S-Hexylglutathione
|
Others
|
Others
|
|
S-Hexylglutathione is an S-substituted glutathione in which the hydrogen of the thiol has been replaced by a hexyl group. S-Hexylglutathione is also an competitive inhibitor against glutathione-S-transferase. S-Hexylglutathione can be used as an affinity chromatographic ligand for glutathione-S-transferase and glutathione peroxidase.
|
-
- HY-146035
-
|
AChE-IN-14
|
Cholinesterase (ChE)
Histamine Receptor
|
Neurological Disease
|
|
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease.
|
-
- HY-133131
-
-
- HY-120879
-
|
PF2562
|
Dopamine Receptor
|
Neurological Disease
|
|
PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a Ki of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC50 of 568 nM in HTRF assay.
|
-
- HY-44103
-
|
Desmethyl-QCA276
PROTAC BRD4-binding moiety 4
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Desmethyl-QCA276 (PROTAC BRD4-binding moiety 4), the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM.
|
-
- HY-132992
-
-
- HY-13682C
-
|
Mifamurtide TFA
MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA
|
NOD-like Receptor (NLR)
|
Cancer
Inflammation/Immunology
|
|
Mifamurtide TFA (MTP-PE TFA), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide TFA, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide TFA has the potential for osteosarcoma research.
|
-
- HY-P1366A
-
|
des-Gln14-Ghrelin TFA
|
GHSR
|
Metabolic Disease
|
|
des-Gln14-Ghrelin TFA is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
|
-
- HY-P99823
-
|
Recifercept
TA-46; sFGFR3
|
FGFR
|
Others
|
|
Recifercept (TA-46) is a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule. Recifercept can be used as a decoy/ligand trap to decrease the amount of fibroblast growth factors that can bind to mutant FGFR3 receptors. Recifercept can be used for the research of achondroplasia.
|
-
- HY-130683
-
-
- HY-130638
-
-
- HY-P99836
-
|
Cudarolimab
IBI101
|
Orexin Receptor (OX Receptor)
|
Cancer
Inflammation/Immunology
|
|
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research.
|
-
- HY-111848A
-
|
PROTAC AR Degrader-4 TFA
|
SNIPERs
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
|
-
- HY-136281
-
|
DuP 734
|
Sigma Receptor
|
Neurological Disease
|
|
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.
|
-
- HY-100723
-
|
THK-523
|
Amyloid-β
|
Neurological Disease
|
|
THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease.
|
-
- HY-111848
-
|
PROTAC AR Degrader-4
|
SNIPERs
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-4 comprises a IAP ligand binding group, a linker and an Androgen Receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
|
-
- HY-147541
-
-
- HY-D0142
-
|
Pyrene-1,3,6,8-tetrasulfonic acid tetrasodium
|
Fluorescent Dye
|
Others
|
|
Pyrene-1,3,6,8-tetrasulfonic acid tetrasodium is a fluorescent dye and pH indicator, also as a ligand of multifunctional metal-organic framework. Pyrene-1,3,6,8-tetrasulfonic acid tetrasodium has been used to detect CO2 release.
|
-
- HY-111874
-
|
SNIPER(ABL)-039
|
SNIPERs
Bcr-Abl
|
Cancer
|
|
SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively.
|
-
- HY-132605
-
|
SLN124
|
Small Interfering RNA (siRNA)
Ser/Thr Protease
|
Metabolic Disease
|
|
SLN124 is a GalNac-siRNA targeting transmembrane serine protease 6 (Tmprss6). SLN124 is composed of a trimeric GalNAc ligand conjugated to TMPRSS6‐siRNA. SLN124 has the potential for an siRNA to restore hepcidin expression and normalise iron homeostasis in β‐thalassaemia.
|
-
- HY-N11386
-
|
Harpactira Hamiltoni Venom
Highveld Baboon Spider Venom
|
Others
|
Neurological Disease
|
|
Harpactira Hamiltoni Venom (Highveld Baboon Spider Venom) is a venom that can be obtained from baboon spider. Spider venoms are complex mixtures of neurotoxic peptides, proteins and low molecular mass organic molecules. Spider venoms have proven to be a rich source of highly specific peptide ligands for selected subtypes of potassium, sodium and calcium channels.
|
-
- HY-111905
-
|
BRD7-IN-1
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
|
-
- HY-148100
-
|
Emapticap pegol
NOX-E36
|
Others
|
Cancer
Inflammation/Immunology
|
|
Emapticap pegol is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36).
|
-
- HY-P1297
-
|
CRF(6-33)(human)
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect.
|
-
- HY-130245
-
|
PCSK9 degrader 1
|
Ser/Thr Protease
|
Metabolic Disease
|
|
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.
|
-
- HY-130842
-
-
- HY-P99720
-
|
Luspatercept
ACE-536; luspatercept–aamt
|
TGF-beta/Smad
|
Metabolic Disease
|
|
Luspatercept (ACE-536) is a recombinant modified ActRIIB fusion protein that binds with transforming growth factor β superfamily ligands. Luspatercept increases the erythrocyte numbers and promotes maturation of erythroid precursors. Luspatercept binds with GDF11 and inhibits Smad2/3 signaling. Luspatercept can be used for the research of anemia.
|
-
- HY-B1322A
-
-
- HY-P9920
-
|
Ramucirumab
|
VEGFR
|
Cancer
|
|
Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D. Ramucirumab is also an angiogenesis inhibitor.
|
-
- HY-P3839
-
|
Nocistatin
|
Opioid Receptor
|
Neurological Disease
|
|
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia.
|
-
- HY-147091
-
-
- HY-125835
-
|
CP-10
|
PROTACs
CDK
|
Cancer
|
|
CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.
|
-
- HY-P1039
-
|
R18
PHCVPRDLSWLDLEANMCLP
|
Raf
|
Cancer
|
|
R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.
|
-
- HY-107452
-
-
- HY-123921
-
|
Gefitinib-based PROTAC 3
|
PROTACs
EGFR
|
Cancer
|
|
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
|
-
- HY-13956
-
|
Pioglitazone
U 72107
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.
|
-
- HY-P99934
-
|
Eftozanermin alfa
ABBV-621
|
Apoptosis
|
Cancer
|
|
Eftozanermin alfa (ABBV-621) is a second-generation tumor necrosis factor-related apoptosis-inducing ligand receptor (TRAIL-R) agonist. Eftozanermin alfa induces apoptosis in tumor cells by activation of death receptors 4/5. Eftozanermin alfa can be used for the research of multiple solid and heme malignancies.
|
-
- HY-15615A
-
|
TIC10
ONC-201
|
TNF Receptor
Apoptosis
|
Cancer
|
|
TIC10 (ONC-201) is a potent, orally active, and stable tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) inducer which acts by inhibiting Akt and ERK, consequently activating Foxo3a and significantly inducing cell surface TRAIL. TIC10 can cross the blood-brain barrier.
|
-
- HY-145696
-
|
SJ10542
|
PROTACs
JAK
|
Cancer
Inflammation/Immunology
|
|
SJ10542 is a potent and selective JAK2/3 directing phenyl glutarimide (PG)-PROTAC with DC50s of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. SJ10542 utilizes a PG ligand as the cereblon (CRBN) recruiter.
|
-
- HY-114324
-
|
PROTAC PARP1 degrader
|
PROTACs
PARP
|
Cancer
|
|
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-P3130
-
|
Stresscopin-related peptide (human)
|
CRFR
|
Inflammation/Immunology
Neurological Disease
|
|
Stresscopin-related peptide (human) is a specific ligand for the type 2 CRH receptor. Stresscopin-related peptide (human) suppresses food intake, delayed gastric emptying and decreases heat-induced edema. Stresscopin-related peptide (human) maintains homeostasis after stress, and can be used in the research of stress-related diseases.
|
-
- HY-130654
-
|
(S,R,S)-AHPC-C2-PEG4-N3
VH032-C2-PEG4-N3
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-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-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC50) of 82 nM.
|
-
- HY-P1846
-
|
Jagged-1 (188-204)
|
Notch
|
Cancer
|
|
Jagged-1 (188-204) is a fragment of the Jagged-1 (JAG-1) protein with Notch agonist activity. JAG-1 is a Notch ligand highly expressed in cultured and primary multiple myeloma (MM) cells. JAG-1 induces maturation of monocyte-derived human dendritic cells.
|
-
- HY-101519
-
|
BETd-260
ZBC 260
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-P1039A
-
|
R18 TFA
PHCVPRDLSWLDLEANMCLP TFA
|
Raf
|
Cancer
|
|
R18 TFA is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.
|
-
- HY-P9968
-
|
Nimotuzumab
|
EGFR
|
Cancer
|
|
Nimotuzumab is a humanized IgG1 monoclonal antibody targeting EGFR with a KD of 0.21 nM. Nimotuzumab is directed against the extracellular domain of the EGFR blocking the binding to its ligands. Nimotuzumab, a strong antitumor drug, is cytolytic on target tumors by its capacity to cause antibody dependent cell mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC).
|
-
- HY-112811
-
|
PROTAC CDK9 degrader-2
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC.
|
-
- HY-130682
-
-
- HY-P1846A
-
|
Jagged-1 (188-204) (TFA)
|
Notch
|
Cancer
|
|
Jagged-1 (188-204) TFA is a fragment of the Jagged-1 (JAG-1) protein with Notch agonist activity. JAG-1 is a Notch ligand highly expressed in cultured and primary multiple myeloma (MM) cells. JAG-1 induces maturation of monocyte-derived human dendritic cells.
|
-
- HY-111905A
-
|
BRD7-IN-1 free base
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
|
-
- HY-P1525
-
-
- HY-134823
-
|
MD-222
|
MDM-2/p53
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
|
-
- HY-132308
-
|
DYRK1-IN-1
|
DYRK
|
Neurological Disease
|
|
DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
|
-
- HY-13956B
-
|
Pioglitazone potassium
U 72107 potassium
|
PPAR
Ferroptosis
|
Cancer
Metabolic Disease
|
|
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research.
|
-
- HY-118482
-
|
Sauristolactam
Saurolactam
|
Others
|
Neurological Disease
|
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-139218
-
-
- HY-D0939
-
|
Direct Blue 1
Chicago Sky Blue 6B
|
Amyloid-β
Others
|
Neurological Disease
|
|
Direct Blue 1 (Chicago Sky Blue 6B) is a counterstain for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1, structurally related to glutamate, is a potent and competitive VGLUT inhibitor without affecting plasma membrane transporters. Direct Blue 1 is the first small molecule PrP ligand capable of inhibiting Aβ binding.
|
-
- HY-P99345
-
|
Dostarlimab
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively.
|
-
- HY-107453
-
|
SirReal1-O-propargyl
PROTAC Sirt2-binding moiety 1
|
Ligands for Target Protein for PROTAC
|
Cancer
|
|
SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2.
|
-
- HY-144204
-
|
Estrogen receptor antagonist 5
|
Estrogen Receptor/ERR
|
Cancer
Endocrinology
|
|
Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165).
|
-
- HY-145615
-
-
- HY-P2264
-
|
KYL peptide
|
Ephrin Receptor
|
Inflammation/Immunology
|
|
KYL peptide, an antagonistic peptide, selectively targets EphA4 receptor. KYL peptide binds to the ligand-binding domain of EphA4, effectively alleviates Aβ-induced synaptic dysfunction and synaptic plasticity defects in AD mice. KYL peptide can promote nerve regeneration after injury and modulating immune responses.
|
-
- HY-P1297A
-
|
CRF(6-33)(human) TFA
|
CRFR
|
Neurological Disease
|
|
CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect.
|
-
- HY-144206
-
|
Estrogen receptor antagonist 6
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166).
|
-
- HY-112752
-
|
Gal-C4-Chol
|
Others
|
Others
|
|
Gal-C4-Chol is a glycosylated cholesterol derivative. Gal-C4-Chol can be used as a ligand for asialoglycoprotein receptors (ASGPR) to prepare Galactosylated (Gal) liposomes. Gal-C4-Chol can be used to prepare simple lipid-based nanoparticles.
|
-
- HY-133139
-
-
- HY-137818
-
-
- HY-146383
-
|
H3R antagonist 2
|
Histamine Receptor
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor (H3R) antagonist with a Ki of 170 nM for hH3R . H3R antagonist 2 shows inhibitory effects with IC50 values of 180, 880 and 775 nM for acetylcholinesterase, butyrylcholinesterase and human monoamine oxidase B (hMAO B), respectively. H3R antagonist 2 shows favorable anti-neuropathic pain and memory-enhancing effects. H3R can across BBB.
|
-
- HY-130642
-
-
- HY-103336
-
|
Tocrifluor 1117
T1117
|
GPR55
Cannabinoid Receptor
|
Cardiovascular Disease
|
|
Tocrifluor 1117 (T1117), a fluorescent form of the cannabinoid CB1 receptor antagonist AM251 (HY-15443), is a selective fluorescent GPR55 ligand. Tocrifluor 1117 is a potent tool for identifying the cellular location of cannabinoid receptors (including GPR55 in living tissues) (Ex/Em=543/590 nm).
|
-
- HY-B1322
-
-
- HY-125693
-
|
L685818
|
Fungal
|
Infection
Neurological Disease
|
|
L685818 is a specific immunophilin ligand. L685818 was neuroregenerative and non-neuroprotective in primary brain cultures. L685818 protects dopaminergic neurons from toxic inhibition of MPP+ and 6-OHDA, reduces tyrosine hydroxylase (TH) loss, and promotes neuronal process regeneration. L685818 is also an antifungal reagent for Cryptococcus neoformans.
|
-
- HY-P99667
-
|
Ipafricept
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is the first class of recombinant fusion proteins, consisting of the extracellular portion of the human fried-8 receptor fused to the Fc fragment of human IgG1 binding to the Wnt ligand. Ipafricept shows solid tumor inhibition activity, with well tolerance.
|
-
- HY-135881
-
|
OMDM-5
|
TRP Channel
Endogenous Metabolite
|
Neurological Disease
|
|
OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM).
|
-
- HY-W020790
-
|
Sialyl-Lewis X
sLeX
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin). Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation.
|
-
- HY-107656
-
|
PTAC oxalate
|
mAChR
|
Neurological Disease
|
|
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects.
|
-
- HY-14422
-
|
SR1078
|
ROR
|
Cancer
|
|
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.
|
-
- HY-130713
-
-
- HY-P1306
-
|
Obestatin(rat)
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-122054
-
|
BPK-29
|
Others
|
Cancer
|
|
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
|
-
- HY-P2268
-
|
RAGE antagonist peptide
|
Amyloid-β
|
Cancer
Inflammation/Immunology
|
|
RAGE antagonist peptide is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide (RAP) possesses anti-tumor and anti-inflammatory activities.
|
-
- HY-122080
-
|
Memoquin
|
Cholinesterase (ChE)
Beta-secretase
Amyloid-β
|
Neurological Disease
|
|
Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-134653
-
|
5-Ph-IAA
|
Others
|
Cancer
|
|
5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.
|
-
- HY-N11387
-
|
Harpactira Pulchripes Venom
Golden Blue-Legged Venom
|
Others
|
Neurological Disease
|
|
Harpactira Pulchripes Venom (Golden Blue-Legged Venom) is a venom that can be obtained from golden blue-legged baboon spider. Spider venoms are complex mixtures of neurotoxic peptides, proteins and low molecular mass organic molecules. Spider venoms have proven to be a rich source of highly specific peptide ligands for selected subtypes of potassium, sodium and calcium channels.
|
-
- HY-133138
-
-
- HY-147102
-
|
tri-GalNAc biotin
|
LYTACs
|
Cancer
|
|
tri-GalNAc biotin is a small molecule lysosome targeting degrader. tri-GalNAc is a ligand of ASGPR (asialoglycoprotein receptor). tri-GalNAc biotin can facilitate the uptake of NeutrAvidin (NA) through ASGPR in liver cells. tri-GalNAc biotin delivers NeutrAvidin to lysosome for degradation. tri-GalNAc biotin can be used for research of LYsosome TArgeting Chimera (LYTAC).
|
-
- HY-B1322B
-
-
- HY-108512
-
|
PD 144418
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 shows potential antipsychotic activity.
|
-
- HY-108460
-
|
A-784168
|
TRP Channel
|
Neurological Disease
|
|
A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.
|
-
- HY-122054A
-
|
BPK-29 hydrochloride
|
Others
|
Cancer
|
|
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
|
-
- HY-P2518
-
-
- HY-13956S1
-
|
Pioglitazone-d4 (alkyl)
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
|
-
- HY-132998
-
|
HDAC6 degrader-1
|
PROTACs
|
Others
|
|
HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation.
|
-
- HY-138555
-
|
PROTAC BRD4 Degrader-8
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
|
-
- HY-124984
-
|
ML353
|
mGluR
|
Neurological Disease
|
|
ML353 is a selective ligand of mGlu5 silent allosteric modulator (SAM) with an Ki value of 18.2 nM. ML353 improves the affinity of common allosteric sites, 20-fold higher than the previous mGlu5 SAM tool compound 5mpep. ML353 has potential applications in solving the intrinsic activity of SAM in vivo or as a drug blocker.
|
-
- HY-P1525A
-
-
- HY-B0131S2
-
-
- HY-15523A
-
|
Braco-19 trihydrochloride
|
DNA/RNA Synthesis
CMV
|
Cancer
Infection
|
|
Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor.
|
-
- HY-138634
-
-
- HY-125877
-
|
PROTAC Mcl1 degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC50 of 0.54 μM.
|
-
- HY-108512A
-
|
PD 144418 oxalate
|
Sigma Receptor
|
Neurological Disease
|
|
PD 144418 oxalate is a highly affinity, potent and selective sigma 1 (σ1) receptor ligand (Ki values of 0.08 nM and 1377 nM for σ1 and σ2 respectively). PD 144418 oxalate devoids of any significant affinity for other receptors, ion channels and enzymes. PD 144418 oxalate shows potential antipsychotic activity.
|
-
- HY-P2518A
-
-
- HY-138632
-
-
- HY-P1022
-
|
Kisspeptin-54(human)
Metastin(human)
|
GnRH Receptor
|
Cancer
Endocrinology
|
|
Kisspeptin-54(human) (Metastin(human)) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) hinders tumor metastasis and stimulates gonadotropin secretion.
|
-
- HY-141798
-
-
- HY-107676
-
|
SIB-1553A
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-105115
-
|
Abecarnil
ZK 112119
|
GABA Receptor
|
Neurological Disease
|
|
Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.
|
-
- HY-138637
-
|
PROTAC BRD4 Degrader-14
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-14 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.8 nM and 1.7 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-14 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
|
-
- HY-138633
-
-
- HY-139185
-
|
PROTAC ERRα Degrader-3
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
|
-
- HY-139294
-
|
PROTAC BRD4 Degrader-15
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-15 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 7.2 nM and 8.1 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-15 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
|
-
- HY-122607
-
|
DPA-714
|
Others
|
Cancer
Inflammation/Immunology
|
|
DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.
|
-
- HY-131385
-
|
KB02-COOH
|
Ligands for E3 Ligase
|
Cancer
|
|
KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610).
|
-
- HY-112603A
-
|
AP5 sodium
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 sodium is a potent, orall active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 sodium demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 sodium has the potential for type II diabetes research.
|
-
- HY-W019787
-
|
BAM-12P
|
Opioid Receptor
CXCR
|
Neurological Disease
|
|
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC50 of 101 nM and a pEC50 of 6.99. BAM-12P is a ligand for CXCR7 with an EC50 of 175 nM.
|
-
- HY-P2268A
-
|
RAGE antagonist peptide TFA
|
Amyloid-β
|
Cancer
Inflammation/Immunology
|
|
RAGE antagonist peptide TFA is an advanced glycation end products (RAGE) antagonist. RAGE antagonist peptide TFA prevents RAGE from binding with several of its most important ligands, including HMGB-1, S100P, and S100A4. RAGE antagonist peptide TFA possesses anti-tumor and anti-inflammatory activities.
|
-
- HY-15523
-
|
Braco-19
|
CMV
DNA/RNA Synthesis
|
Cancer
|
|
Braco-19 is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor.
|
-
- HY-134440A
-
-
- HY-112603
-
|
AP5
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research.
|
-
- HY-145708
-
-
- HY-110358
-
|
QAQ dichloride
|
Sodium Channel
|
Inflammation/Immunology
|
|
QAQ dichloride, a photoswitchable voltage-gated Nav and Kv channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain.
|
-
- HY-N0990
-
|
1,5,15-Trimethylmorindol
|
Others
|
Cancer
|
|
1,5,15-Trimethylmorindol is an anthraquinone isolated from the leaves of Morinda citrifolia. 1,5,15- trimethylmorindol (25 μg/mL) does not show significant cytotoxic activity on the human T-cell leukemia cell line, Jurkat, by itself but it shows cytotoxicity (IC50 14.5-15.0 μg/mL) when combined with 0.5-1.5 μg/mL of TRAIL in the cell proliferation assay.
|
-
- HY-B1322AS
-
-
- HY-13912G
-
|
IWP-2
|
Wnt
|
Cancer
|
|
IWP-2 (GMP) is IWP-2 (HY-13912) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and blocks Wnt ligand palmitoylation.
|
-
- HY-111518
-
|
JH-XI-10-02
|
PROTACs
CDK
|
Cancer
|
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JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader |
