Search Result
Results for "
4-1BB Ligand Inhibitors
" in MCE Product Catalog:
9867
Inhibitors & Agonists
20
Biochemical Assay Reagents
249
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-133045
-
|
VHL Ligand 8
|
Ligand for E3 Ligase
|
Cancer
|
|
VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
|
-
- HY-126456
-
-
- HY-133073
-
|
CCR7 Ligand 1
CCR7-Cmp2105
|
CCR
Ligand 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.
|
-
- HY-U00439
-
-
- HY-P1840A
-
-
- HY-P1840
-
-
- HY-133046
-
|
VHL Ligand-Linker Conjugates 17
|
E3 Ligase Ligand-Linker Conjugate
|
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-128808
-
|
cIAP1 ligand 1
E3 ligase Ligand 12
|
Ligand for E3 Ligase
|
Cancer
|
|
cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-128809
-
|
cIAP1 ligand 2
E3 ligase Ligand 11
|
Ligand for E3 Ligase
|
Cancer
|
|
cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-128837
-
|
Nutlin carboxylic acid
MDM2 Ligand 1; E3 ligase Ligand 16
|
Ligand for E3 Ligase
|
Cancer
|
|
Nutlin carboxylic acid (MDM2 ligand 1) is the Nutlin 3-based MDM2 ligand. Nutlin carboxylic acid (MDM2 ligand 1) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-103597
-
|
Thalidomide-O-COOH
Cereblon Ligand 3; E3 ligase Ligand 3
|
Ligand 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-111823
-
-
- HY-103596
-
|
Thalidomide-4-OH
Cereblon Ligand 2; E3 ligase Ligand 2
|
Ligand for E3 Ligase
|
Cancer
|
|
Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-41547
-
|
Thalidomide 4-fluoride
Cereblon Ligand 4; E3 ligase Ligand 4
|
Ligand for E3 Ligase
|
Cancer
|
|
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
|
-
- HY-128807
-
|
E3 ligase Ligand 10
|
Ligand 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
|
Ligand 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
|
Ligand 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
|
Ligand 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
|
Ligand for E3 Ligase
|
Cancer
|
|
E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-128806
-
|
E3 ligase Ligand 9
|
Ligand 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-114399
-
-
- HY-129939
-
-
- HY-130245
-
|
PCSK9 ligand 1
|
Ser/Thr Protease
|
Metabolic Disease
|
|
PCSK9 ligand 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 ligand 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.
|
-
- HY-125905
-
|
VH032-cyclopropane-F
VHL Ligand 3; E3 ligase Ligand 19
|
Ligand 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-128836
-
-
- HY-139304
-
-
- HY-138539
-
-
- HY-129967
-
-
- HY-136306
-
-
- HY-U00126
-
-
- HY-111839
-
-
- 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).
|
-
- HY-111845
-
-
- HY-111843
-
-
- 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.
|
-
- HY-130296
-
-
- HY-130270
-
-
- HY-101626
-
-
- HY-125906
-
-
- HY-U00425
-
-
- 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-44012
-
-
- HY-44012A
-
-
- HY-42424
-
|
(S,R,S)-AHPC-Me hydrochloride
VHL Ligand 2 hydrochloride; E3 ligase Ligand 1
|
Ligand 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
|
Ligand 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-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-120217
-
|
VH032
|
Ligand 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-44148
-
-
- HY-KT001
-
-
- HY-141486
-
|
Dual PARP EGFR ligand for PROTAC
|
Target Protein Ligand-Linker Conjugate
|
Cancer
|
|
Dual PARP EGFR ligand for PROTAC incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). Dual PARP EGFR ligand for PROTAC can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP.
|
-
- HY-112078
-
|
(S,R,S)-AHPC-Me
VHL Ligand 2; E3 ligase Ligand 1A
|
Ligand 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-12512
-
|
cGAMP
Cyclic GMP-AMP; 3',3'-cGAMP
|
STING
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMP; 3',3'-cGAMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.
|
-
- HY-130499
-
|
ERRα Ligand-Linker Conjugates 1
|
Target Protein Ligand-Linker Conjugate
|
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-115446A
-
|
Lenalidomide-C4-NH2 hydrochloride
Cereblon Ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
|
-
- HY-129608
-
|
Lenalidomide-acetylene-C5-COOH
Cereblon Ligand-linker Conjugate
|
E3 Ligase Ligand-Linker Conjugate
|
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.
|
-
- HY-107439
-
|
Thalidomide-O-amido-C8-NH2
Cereblon Ligand-Linker Conjugates 2; E3 Ligase Ligand-Linker Conjugates 20
|
E3 Ligase Ligand-Linker Conjugate
|
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 Conjugate
|
Cancer
|
|
Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-111824
-
|
VH032-thiol-C6-NH2
VHL Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 29
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
|
-
- HY-112618
-
|
Thalidomide-O-amido-C6-NH2
Cereblon Ligand-Linker Conjugates 11; E3 Ligase Ligand-Linker Conjugates 25
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Thalidomide-O-amido-C6-NH2 (Cereblon Ligand-Linker Conjugates 11), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
|
-
- HY-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-128716B
-
|
Pomalidomide-PEG3-C2-NH2 hydrochloride
Cereblon Ligand-Linker Conjugates 5 hydrochloride; E3 ligase Ligand-Linker Conjugates 30 hydrochloride
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Pomalidomide-PEG3-C2-NH2 (Cereblon Ligand-Linker Conjugates 5) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
|
-
- HY-133189
-
-
- HY-103612
-
-
- HY-129776
-
|
K-Ras ligand-Linker Conjugate 2
|
Target Protein Ligand-Linker Conjugate
|
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 Conjugate
|
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-21930
-
|
Pomalidomide-PEG4-C-COOH
Cereblon Ligand -Linker Conjugates 1; E3 Ligase Ligand-Linker Conjugates 1
|
E3 Ligase Ligand-Linker Conjugate
|
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-130822
-
|
K-Ras ligand-Linker Conjugate 4
|
Target Protein Ligand-Linker Conjugate
|
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 Conjugate
|
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 Conjugate
|
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 Conjugate
|
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-101763A
-
|
(S,R,S)-AHPC hydrochloride
VH032-NH2 hydrochloride; VHL Ligand 1 hydrochloride
|
Ligand for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC 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-103614
-
|
Thalidomide-O-amido-C8-NH2 TFA
Cereblon Ligand -Linker Conjugates 2 TFA; E3 Ligase Ligand-Linker Conjugates 20 TFA
|
E3 Ligase Ligand-Linker Conjugate
|
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 Conjugate
|
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-128941
-
-
- 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-130521
-
|
Pomalidomide-amido-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 22; E3 ligase Ligand-Linker Conjugates 55
|
E3 Ligase Ligand-Linker Conjugate
|
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-125845
-
|
(S,R,S)-AHPC
VH032-NH2; VHL Ligand 1
|
Ligand 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-115560
-
-
- HY-103615
-
-
- 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 Conjugate
|
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 Conjugate
|
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-41549
-
|
Pomalidomide-PEG4-Ph-NH2
Cereblon Ligand-Linker Conjugates 9; E3 Ligase Ligand-Linker Conjugates 2
|
E3 Ligase Ligand-Linker Conjugate
|
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-126534A
-
-
- HY-126534
-
-
- 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-W087383
-
-
- HY-131005
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-130979
-
-
- HY-128716
-
|
Pomalidomide-PEG3-C2-NH2
Cereblon Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 30
|
E3 Ligase Ligand-Linker Conjugate
|
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 Conjugate
|
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-122725
-
|
Lenalidomide-C5-NH2
Cereblon Ligand-Linker Conjugates 19; E3 ligase Ligand-Linker Conjugates 31
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTAC, such as MDM2 PROTAC degrader.
|
-
- HY-128846A
-
-
- HY-125884
-
-
- HY-115560A
-
-
- HY-130716
-
-
- HY-128846
-
-
- HY-133486
-
-
- HY-126458
-
-
- 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-110402
-
|
(S,R,S)-AHPC TFA
VH032-NH2 TFA; VHL Ligand 1 TFA
|
Ligand for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC TFA (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-128716A
-
|
Pomalidomide-PEG3-C2-NH2 TFA
Cereblon Ligand-Linker Conjugates 5 TFA; E3 ligase Ligand-Linker Conjugates 30 TFA
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Pomalidomide-PEG3-C2-NH2 TFA 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-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-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 Conjugate
|
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-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-130813
-
-
- HY-125883
-
-
- HY-112617A
-
-
- HY-103611
-
-
- HY-136424
-
|
GPI-1485
GM1485
|
Others
|
Neurological Disease
|
|
GPI-1485 (GM1485), a nonimmunosuppressive immunophilin ligand, promotes neurofunctional improvement and neural regeneration following stroke.
|
-
- HY-128832
-
-
- HY-114176
-
-
- 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 Conjugate
|
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 Conjugate
|
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 Conjugate
|
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 Conjugate
|
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 Conjugate
|
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 Conjugate
|
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-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-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 Conjugate
|
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-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-P3136
-
|
TRV055
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-112600
-
-
- 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 Conjugate
|
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 Conjugate
|
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-128848
-
-
- 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-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-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-121879
-
-
- 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-114872
-
-
- HY-112617
-
-
- 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 Conjugate
|
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-125843
-
|
Pomalidomide-PEG1-C2-N3
Cereblon Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 50
|
E3 Ligase Ligand-Linker Conjugate
|
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-112600A
-
-
- HY-114872A
-
-
- 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 Conjugate
|
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-130982
-
|
Lenalidomide-PEG3-iodine
|
E3 Ligase Ligand-Linker Conjugate
|
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-130798
-
-
- 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-P2159
-
|
Dynorphin A (1-8)
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- HY-131295
-
-
- HY-D0020
-
|
2,2'-Bipyridine
|
Others
|
Infection
|
|
2,2'-Bipyridine is the unique molecular scaffold of the bioactive natural products represented by caerulomycins (CAEs) and collismycins (COLs). 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.
|
-
- 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-P1483
-
-
- HY-P1483B
-
-
- HY-122098
-
-
- HY-19373
-
-
- HY-P1483A
-
-
- HY-133799
-
-
- 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-139516
-
|
[18F]AZD4694 Precursor
|
Others
|
Others
|
|
[18F]AZD4694 Precursor 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-139403
-
-
- 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-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- 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-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-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-133036
-
|
APJ receptor agonist 1
|
Others
|
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-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-113330
-
|
12S-HHT
12(S)-HHTrE
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H 2 (PGH 2) 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-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- 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 Conjugate
|
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-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-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- 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-B1287
-
|
Citalopram hydrobromide
(±)-Citalopram hydrobromide; Lu 10-171
|
Serotonin Transporter
Autophagy
|
Neurological Disease
Cancer
|
|
Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
|
-
- 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-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-103606
-
|
(S,R,S)-AHPC-PEG6-C4-Cl
VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9
|
PROTACs
|
Cancer
|
|
(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that 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-103607
-
|
(S,R,S)-AHPC-PEG2-C4-Cl
VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10
|
PROTACs
|
Cancer
|
|
(S,R,S)-AHPC-PEG2-C4-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-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-18728
-
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-113534
-
|
MV1
|
IAP
Apoptosis
|
Others
|
|
MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
|
-
- HY-A0003B
-
|
Lenalidomide hemihydrate
CC-5013 hemihydrate
|
Ligand for E3 Ligase
Molecular Glue
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
|
Ligand for E3 Ligase
Molecular Glue
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
|
Ligand for E3 Ligase
Molecular Glue
|
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-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-15583
-
-
- 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
|
PROTACs
|
Cancer
|
|
(S,R,S)-AHPC-C6-PEG3-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
|
-
- HY-75706
-
|
N-Descyclopropanecarbaldehyde Olaparib
|
E3 Ligase Ligand-Linker Conjugate
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-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-131976
-
|
BVDV-IN-1
|
DNA/RNA Synthesis
|
Infection
|
|
BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. BVDV-IN-1 directly binds to a hydrophobic pocket of the BVDV RdRp. BVDV-IN-1 has antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC).
|
-
- 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-111879
-
|
Biotin-BS
|
SNIPER
|
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-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-111878
-
|
BzNH-BS
|
SNIPER
|
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-110399
-
-
- 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-N0277
-
-
- HY-18370
-
-
- 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-111850
-
-
- HY-101601
-
-
- HY-130952
-
|
Thalidomide-O-C8-COOH
|
Ligand 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-111872
-
|
SNIPER(ABL)-020
|
SNIPER
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-111857
-
-
- HY-111847
-
-
- 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-N1427A
-
-
- HY-104046
-
-
- HY-136272
-
-
- HY-136273
-
-
- HY-136274
-
-
- HY-139549
-
|
Thalidomide-benzo
|
Ligand 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-111858
-
-
- HY-111852
-
-
- HY-111853
-
-
- HY-13751
-
-
- HY-122577
-
-
- HY-124625
-
-
- HY-126457
-
|
Thalidomide-propargyl
|
Ligand 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-138773
-
-
- HY-130737
-
-
- 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-111849
-
-
- HY-P1123
-
|
MEDICA16
|
ATP Citrate Lyase
GPR40
GPR120
|
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-138771
-
-
- HY-138782
-
-
- HY-138778
-
-
- HY-138776
-
-
- HY-138780
-
-
- 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 VHL ligand, with an IC50 of 247 nM for EED.
|
-
- HY-141010A
-
-
- HY-130950
-
-
- HY-138777
-
-
- HY-138772
-
-
- HY-130951
-
-
- HY-138781
-
-
- 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-15839
-
-
- HY-130854
-
|
Thalidomide-NH-C6-NH-Boc
|
E3 Ligase Ligand-Linker Conjugate
|
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-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-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-132208
-
-
- HY-138784
-
-
- HY-130965
-
-
- HY-131888A
-
-
- HY-141010B
-
-
- HY-W076696
-
|
Lenalidomide-4-OH
|
Ligand 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-13751A
-
-
- HY-111851
-
|
SNIPER(ABL)-049
|
SNIPER
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-133816A
-
-
- HY-136162A
-
-
- HY-133485B
-
-
- HY-139539
-
|
Thalidomide-5-COOH
|
Ligand 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
|
Ligand 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-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
|
Ligand 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-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
|
SNIPER
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-111855
-
-
- HY-W077589A
-
|
Lenalidomide-5-aminomethyl
|
Ligand 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-131872
-
-
- HY-138853
-
-
- HY-138882
-
|
Lenalidomide-4-aminomethyl
|
Ligand 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-138849A
-
-
- HY-138882A
-
-
- HY-W077589
-
-
- HY-129704A
-
-
- HY-134984A
-
-
- HY-134984
-
-
- HY-138850A
-
-
- HY-131388
-
-
- HY-138850
-
-
- HY-138881
-
|
Lenalidomide-6-F
|
Ligand 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
|
Ligand 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
|
Ligand 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-15238
-
-
- HY-108477
-
|
TMPyP4 tosylate
TMP 1363
|
G-quadruplex
Telomerase
|
Cancer
|
|
TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
|
-
- HY-138786
-
-
- HY-107438A
-
-
- HY-136166
-
-
- HY-130948B
-
-
- HY-107439A
-
-
- HY-136156
-
-
- HY-112618B
-
-
- HY-122694
-
-
- HY-141423A
-
-
- HY-138785
-
-
- HY-130852
-
-
- HY-15594A
-
-
- HY-15043
-
-
- HY-130850
-
-
- HY-111859
-
|
SNIPER(ABL)-058
|
SNIPER
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
|
SNIPER
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-122694A
-
-
- HY-114420
-
-
- HY-106547
-
-
- HY-111873
-
|
SNIPER(ABL)-019
|
SNIPER
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-138862
-
-
- HY-136163A
-
-
- HY-131159
-
|
Thalidomide-O-C8-Boc
|
Ligand 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
|
Ligand 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-111861
-
|
SNIPER(ABL)-024
|
SNIPER
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-N0596
-
|
Panaxadiol
20(R)-Panaxadiol
|
Others
|
Cancer
|
|
Panaxadiol is found in the roots of Panax ginseng, activities neuroprotective and anti-tumour functions. Panaxadiol inhibits programmed cell death-ligand 1(PD-L1) expression and tumour proliferation.
|
-
- HY-111862
-
|
SNIPER(ABL)-044
|
SNIPER
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
Cytochrome P450
|
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-136055
-
-
- 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-123215
-
|
CC-17369
7-Hydroxy pomalidomide; Pomalidomide metabolite M16
|
Ligand 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
|
Ligand 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-P0224
-
-
- 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-129703B
-
-
- HY-139541
-
|
Pomalidomide-5-O-CH3
|
Ligand 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
|
Ligand 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
|
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-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-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-35261A
-
-
- HY-130197
-
-
- HY-141481
-
-
- HY-111663
-
-
- HY-U00228
-
-
- HY-15265
-
-
- HY-131959
-
-
- 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
|
Ligand 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
|
Ligand 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-111863
-
|
SNIPER(ABL)-047
|
SNIPER
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-122825
-
|
SNIPER(ER)-110
|
SNIPER
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-110 consists of a cIAP1 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-130648
-
-
- HY-107440A
-
-
- HY-114434
-
-
- HY-100486
-
|
BTTAA
|
Others
|
Others
|
|
BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
|
-
- HY-13723
-
-
- 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-131717
-
|
Thalidomide-NH-CH2-COOH
|
Ligand 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-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
|
SNIPER
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-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-131646
-
-
- HY-43722
-
|
Lenalidomide-Br
|
Ligand 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-116677
-
-
- HY-N3171A
-
-
- HY-130269
-
|
β-Naphthoflavone-CH2-OH
β-NF-CH2-OH
|
Ligand 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-131232
-
-
- HY-N0499
-
|
Cyanidin Chloride
IdB 1027
|
Others
|
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-W129872
-
-
- HY-131647
-
-
- HY-129619
-
|
SNIPER(ER)-87
|
SNIPER
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-69220
-
|
7-Octynoic acid
|
PROTAC Linker
|
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
|
Ligand 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-135324
-
-
- HY-32339
-
-
- 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-108372
-
|
Boc-C5-O-C5-O-C6-Cl
PROTAC Linker 2
|
PROTAC Linker
|
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-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-128842
-
-
- HY-128843
-
-
- HY-128840
-
-
- HY-128841
-
-
- 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-136006B
-
-
- HY-136186
-
-
- HY-130711B
-
-
- HY-136008
-
-
- HY-125845A
-
|
(S,S,S)-AHPC hydrochloride
(S,S,S)-VH032-NH2 hydrochloride
|
Ligand 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 Linker
|
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-114169
-
|
WRG-28
|
Discoidin Domain Receptor
|
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC50 of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.
|
-
- HY-112398
-
-
- 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-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
|
Others
|
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-110385
-
|
cGAMP disodium
Cyclic GMP-AMP disodium; 3',3'-cGAMP disodium
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP disodium (Cyclic GMP-AMP disodium) is the third cyclic dinucleotide (CDN) to be discovered in bacteria. cGAMP disodium is an effective adjuvant for sublingual vaccination capable of promoting broad immunity including serum anti-PA neutralizing and anti-PA SIgA responses in airway secretions.
|
-
- 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-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- 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-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-129941
-
-
- HY-129941A
-
-
- HY-130847
-
-
- HY-139482
-
|
tri-GalNAc-COOH
|
LYTAC
|
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-D1288
-
|
Tris-NTA
|
Others
|
Others
|
|
Tris-NTA is a His-tagged protein ligand, which can be used to bind His-tagged proteins.
|
-
- 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-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-107443
-
-
- HY-136184
-
-
- HY-131231
-
|
Thalidomide-NH-PEG3-CH2CHO
|
Ligand for E3 Ligase
|
Cancer
|
|
Thalidomide-NH-PEG3-CH2CHO is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-PEG3-CH2CHO can be connected to the ligand for protein by a linker to form PROTAC BCL-XL degrader XZ739 (HY-133557).
|
-
- HY-136187
-
-
- HY-103603B
-
-
- HY-P2277
-
-
- HY-16785A
-
-
- HY-107444
-
-
- HY-P2278
-
-
- HY-U00250
-
-
- HY-A0077AS
-
-
- 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 CRBN ligand.
|
-
- HY-130988
-
|
Ipatasertib-NH2
GDC-0068-NH2; RG7440-NH2
|
Ligand 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-130853
-
|
Thalidomide-NH-PEG2-C2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugate
|
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-111844
-
|
PROTAC RAR Degrader-1
|
SNIPER
PROTACs
RAR/RXR
|
Cancer
|
|
PROTAC RAR Degrader-1 comprises a cIAP1 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-P1740
-
|
RGD peptide (GRGDNP)
|
Integrin
Apoptosis
|
Inflammation/Immunology
|
|
RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-P1186
-
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-44103
-
|
Desmethyl-QCA276
PROTAC BRD4-binding moiety 4
|
Ligand 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-108652
-
-
- HY-134440
-
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- 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-136269A
-
-
- HY-136269
-
-
- HY-P1037
-
-
- HY-P1740A
-
|
RGD peptide (GRGDNP) (TFA)
|
Integrin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
RGD peptide (GRGDNP) (TFA) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) (TFA) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-111874
-
|
SNIPER(ABL)-039
|
SNIPER
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-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
-
|
UNC9994
|
Dopamine Receptor
5-HT Receptor
Histamine Receptor
|
Neurological Disease
|
|
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
|
-
- 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-129774
-
|
Phthalimide-PEG4-MPDM-OH
|
PROTAC Linker
|
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 Conjugate
|
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 Linker
|
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-129773
-
|
Phthalimide-PEG4-PDM-OTBS
|
PROTAC Linker
|
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-112895A
-
-
- 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-129603
-
|
SI-109
|
STAT
Ligand for Target Protein for PROTAC
|
Cancer
|
|
SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36.
|
-
- 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-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-B1322A
-
-
- 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-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-129405
-
-
- HY-P9904
-
-
- HY-141495
-
-
- HY-13912
-
|
IWP-2
|
Wnt
Porcupine
Casein Kinase
|
Cancer
|
|
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 thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ.
|
-
- 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-114407
-
|
TD-428
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
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-107453
-
|
SirReal1-O-propargyl
PROTAC Sirt2-binding moiety 1
|
Ligand 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-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-130652
-
|
Pomalidomide 4'-PEG3-azide
|
E3 Ligase Ligand-Linker Conjugate
|
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-107447
-
-
- HY-N8460
-
-
- HY-15329
-
|
Maxacalcitol-D6
|
VD/VDR
|
Metabolic Disease
|
|
Maxacalcitol-D6 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-110287
-
|
Apcin
|
APC
|
Cancer
|
|
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis.
|
-
- 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-130642
-
-
- HY-B1322
-
-
- 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
|
Others
|
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-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-B1322B
-
-
- HY-129772
-
|
Phthalimide-PEG3-C2-OTs
|
PROTAC Linker
|
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 Linker
|
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-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-111413
-
-
- 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-12452
-
-
- HY-P1125
-
|
4-CMTB
|
Others
|
Others
|
|
4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
|
-
- 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-B2087
-
-
- 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-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-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-111413A
-
-
- 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 VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.
|
-
- HY-125877
-
|
PROTAC Mcl1 degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity.
|
-
- HY-100560
-
|
Abscisic acid
(S)-(+)-Abscisic acid; ABA
|
Endogenous Metabolite
Proton Pump
|
Metabolic Disease
|
|
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.
|
-
- HY-15614A
-
|
SC144 hydrochloride
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
|
-
- HY-15614
-
|
SC144
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
|
-
- HY-131168
-
-
- 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-129652
-
|
Halo PROTAC 1
|
PROTACs
Autophagy
|
Cancer
|
|
Halo PROTAC 1 is a PROTAC, which 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.
|
-
- HY-112617B
-
-
- 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-101849
-
|
Fasentin
|
GLUT
|
Cancer
Cardiovascular Disease
|
|
Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
|
-
- HY-12028
-
|
PD98059
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
|
PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits autophagy.
|
-
- HY-10046
-
-
- HY-110135A
-
|
NBI-31772 hydrate
|
IGF-1R
|
Neurological Disease
|
|
NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects.
|
-
- HY-19578B
-
|
Isamoltane hemifumarate
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [ 125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity.
|
-
- HY-B0131
-
-
- HY-P1306A
-
|
Obestatin(rat) TFA
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA 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) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-135691
-
|
hnRNPK-IN-1
|
c-Myc
Apoptosis
|
Cancer
|
|
hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities.
|
-
- HY-P3108
-
-
- 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-13956
-
|
Pioglitazone
U 72107
|
PPAR
Ferroptosis
|
Metabolic Disease
Cancer
|
|
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.
|
-
- 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-136006
-
-
- HY-133487B
-
-
- HY-136006A
-
-
- HY-130618
-
|
Boc-C1-PEG3-C4-OH
|
PROTAC Linker
|
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 Conjugate
|
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 Conjugate
|
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-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-130845
-
|
AR antagonist 1
|
Ligand for E3 Ligase
|
Cancer
|
|
AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).
|
-
- 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-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-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-13001
-
|
Quizartinib
AC220
|
FLT3
Ligand for Target Protein for PROTAC
Apoptosis
Autophagy
|
Cancer
|
|
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
|
-
- HY-116624
-
|
MAZ51
|
VEGFR
Apoptosis
|
Cancer
|
|
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
|
-
- HY-A0009
-
|
Galanthamine hydrobromide
Galantamine hydrobromide
|
AChE
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
|
-
- 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-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-130814
-
|
Thalidomide-NH-C4-NH2 TFA
|
E3 Ligase Ligand-Linker Conjugate
|
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 Conjugate
|
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-135250B
-
-
- 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-129363
-
-
- HY-W013788
-
-
- HY-130619
-
|
Boc-C1-PEG3-C4-OBn
|
PROTAC Linker
|
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-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-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-112603
-
|
AP5
|
GPR40
|
Metabolic Disease
|
|
AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor.
|
-
- HY-111546
-
|
BI-3663
|
PROTACs
FAK
|
Cancer
|
|
BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.
|
-
- HY-100848
-
|
TX1-85-1
|
EGFR
|
Cancer
|
|
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling.
|
-
- HY-125876
-
|
PROTAC Bcl2 degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC, 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-130983
-
|
N-piperidine Ibrutinib hydrochloride
|
Btk
Ligand for Target Protein for PROTAC
|
Cancer
|
|
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
|
-
- HY-123919
-
|
TL13-112
|
PROTACs
ALK
|
Cancer
|
|
TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the cereblon ligand of Pomalidomide (HY-10984).
|
-
- HY-100277
-
|
Mifobate
SR-202
|
PPAR
|
Metabolic Disease
|
|
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects.
|
-
- HY-W040270
-
|
Amino-PEG10-amine
|
PROTAC Linker
|
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-13682B
-
|
Mifamurtide sodium
MTP-PE sodium; L-MTP-PE sodium; CGP 19835 sodium
|
Others
|
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-B2087S
-
-
- HY-133234
-
|
BMVC-8C3O
|
G-quadruplex
|
Others
|
|
BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
|
-
- 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-13682
-
|
Mifamurtide
MTP-PE; L-MTP-PE; CGP 19835
|
Others
|
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-B2087S1
-
-
- HY-136160
-
-
- HY-130411
-
|
Amino-PEG11-amine
|
PROTAC Linker
|
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-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 E3 ubiquitin ligase (Pomalidomide; HY-10984).
|
-
- HY-128838
-
-
- 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-110318
-
|
VUF11207 fumarate
|
CXCR
|
Cancer
|
|
VUF11207 fumarate (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
|
-
- HY-134591
-
-
- HY-141551
-
|
GNE-274
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research.
|
-
- HY-122582
-
|
TL13-12
|
PROTACs
ALK
|
Cancer
|
|
TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984).
|
-
- HY-108635
-
-
- HY-103636
-
|
PROTAC Sirt2 Degrader-1
|
Sirtuin
PROTACs
|
Cancer
|
|
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
|
-
- 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-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-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.
|
-
- 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-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-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-103241
-
|
Ro 90-7501
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Cancer
Neurological Disease
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
|
-
- HY-P1846
-
|
Jagged-1 (188-204)
|
Notch
|
Cancer
|
|
Jagged-1 (188-204) is a fragment of the Jagged-1 (JAG-1) protein. 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-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-43869
-
|
Vipivotide tetraxetan Linker
PSMA-617 Linker
|
ADC Linker
|
Cancer
|
|
Vipivotide tetraxetan Linker (PSMA-617 Linker) is a nonclaevable peptide linker for synthesis of Vipivotide tetraxetan (PSMA-617). Vipivotide tetraxetan (PSMA-617) is a ligand used to synthesize 177Lu-PSMA-617, which is a radioactive molecule for the treatment of prostate cancer.
|
-
- HY-13682C
-
|
Mifamurtide TFA
MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA
|
Others
|
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-130683
-
-
- HY-130638
-
-
- 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. 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-P1846A
-
|
Jagged-1 (188-204) (TFA)
|
Notch
|
Cancer
|
|
Jagged-1 (188-204) TFA is a fragment of the Jagged-1 (JAG-1) protein. 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-13956S
-
|
Pioglitazone D4
U 72107 D4
|
PPAR
Ferroptosis
|
Cancer
Metabolic Disease
|
|
Pioglitazone D4 (U 72107 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.
|
-
- 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-123921
-
|
Gefitinib-based PROTAC 3
|
PROTACs
EGFR
|
Cancer
|
|
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL 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-B0131S
-
|
Prostaglandin E1-d4
|
Prostaglandin Receptor
Endogenous Metabolite
|
Endocrinology
Cardiovascular Disease
|
|
Prostaglandin E1-d4 (Alprostadil-d4) is the deuterium labeled Prostaglandin E1. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.
|
-
- HY-111848A
-
|
PROTAC AR Degrader-4 TFA
|
SNIPER
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-4 comprises a cIAP1 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-130842
-
-
- HY-P1039
-
|
R18
PHCVPRDLSWLDLEANMCLP
|
Others
|
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-112210
-
|
Shield-1
|
FKBP
|
Others
|
|
Shield-1 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 the entire fusion protein.
|
-
- HY-111848
-
|
PROTAC AR Degrader-4
|
SNIPER
PROTACs
Androgen Receptor
|
Cancer
|
|
PROTAC AR Degrader-4 comprises a cIAP1 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-120944
-
|
BAY-7598
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-130654
-
|
(S,R,S)-AHPC-C2-PEG4-N3
VH032-C2-PEG4-N3
|
E3 Ligase Ligand-Linker Conjugate
|
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-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-130682
-
-
- HY-10232
-
|
THIP
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.
|
-
- HY-P1525
-
-
- 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-133139
-
-
- HY-130422
-
|
Tos-PEG4-t-butyl ester
Tos-PEG4-Boc
|
PROTAC Linker
|
Cancer
|
|
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 (HY-111546). BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC50 of 18 nM.
|
-
- HY-B1033
-
|
Metergoline
|
5-HT Receptor
Dopamine Receptor
Sodium Channel
|
Neurological Disease
|
|
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
|
-
- 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-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-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-133138
-
-
- 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-131385
-
|
KB02-COOH
|
Ligand 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-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.
|
-
- 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-P1525A
-
-
- 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-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-130256
-
|
β-NF-JQ1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
β-NF-JQ1 is a PROTAC that recruits AhR E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
|
-
- 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-131188
-
|
PROTAC Bcl-xL degrader-1
|
PROTACs
Bcl-2 Family
|
Cancer
|
|
PROTAC Bcl-xL degrader-1 is a PROTAC that comprises a Bcl-xL ligand binding group, a linker and an IAP E3 ligases binding group. PROTAC Bcl-xL degrader-1 is a potent Bcl-xL degrader, and shows toxicity for human platelets and MyLa 1929 cells with IC50 values of 62 nM and 8.5 μM, respectively.
|
-
- HY-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-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-136008A
-
-
- HY-16781
-
|
Grapiprant
CJ-023423; RQ-00000007; AAT-007
|
Prostaglandin Receptor
|
Metabolic Disease
Endocrinology
|
|
Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [ 3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment[3] .
|
-
- HY-128838A
-
|
(rel)-PROTAC ERRα Degrader-1
|
Others
|
Others
|
|
(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1. PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
|
-
- HY-129602
-
|
SD-36
|
PROTACs
STAT
Apoptosis
|
Cancer
|
|
SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.
|
-
- HY-131386
-
-
- HY-P1022A
-
|
Kisspeptin-54(human) TFA
Metastin(human) TFA
|
GnRH Receptor
|
Cancer
Endocrinology
|
|
Kisspeptin-54(human) TFA (Metastin(human) TFA) is an endogenous ligand for kisspeptin receptor (KISS1, GPR54). Kisspeptin-54(human) TFA binds to rat and human GPR54 receptors with Ki values of 1.81 nM and 1.45 nM, respectively. Kisspeptin-54(human) TFA hinders tumor metastasis and stimulates gonadotropin secretion.
|
-
- HY-N2453
-
|
Convallatoxin
|
PPAR
NF-κB
P-glycoprotein
|
Cancer
Inflammation/Immunology
|
|
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
|
-
- HY-P1204
-
|
[Ala17]-MCH
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
|
-
- HY-138139A
-
|
AXC-715 hydrochloride
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
AXC-715 hydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.
|
-
- HY-P1204A
-
|
[Ala17]-MCH TFA
|
MCHR1 (GPR24)
|
Metabolic Disease
|
|
[Ala17]-MCH TFA, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
|
-
- HY-10019
-
|
Varenicline
CP 526555
|
nAChR
|
Neurological Disease
|
|
Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
|
-
- HY-112495
-
|
VH032-PEG5-C6-Cl
HaloPROTAC 2
|
PROTACs
|
Cancer
|
|
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that 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-131187
-
|
BMS-1166-N-piperidine-COOH
|
Ligand for Target Protein for PROTAC
|
Cancer
|
|
BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-12397
-
|
ZK159222
|
VD/VDR
|
Endocrinology
|
|
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character.
|
-
- HY-111846
-
|
PROTAC ERα Degrader-2
|
SNIPER
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
|
-
- HY-131230
-
-
- HY-126252
-
|
A-9758
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
|
-
- HY-117727
-
|
Leriglitazone
Hydroxypioglitazone
|
PPAR
|
Metabolic Disease
|
|
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.
Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.
Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM，induces transcriptional efficacy of the PPARγ (LBD) with EC50
of 680 nM.
|
-
- HY-130815
-
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-N2025
-
|
Oroxin A
|
PPAR
Glucosidase
|
Metabolic Disease
|
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
|
-
- HY-108006
-
|
Mirogabalin besylate
DS 5565 besylate
|
Calcium Channel
|
Neurological Disease
|
|
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
|
-
- HY-129610
-
|
KB02-SLF
|
PROTACs
FKBP
|
Cancer
|
|
KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
|
-
- HY-128359
-
|
ACBI1
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.
|
-
- HY-P0172A
-
|
ATI-2341 TFA
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-119109
-
|
Laminaran
|
Others
|
Cancer
|
|
Laminaran is an β-1-3-glucan and a typical ligand for Dectin-1 from Eisenia Bicyclis, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
|
-
- HY-136242
-
|
UT-34
|
Androgen Receptor
|
Cancer
Endocrinology
|
|
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.
|
-
- HY-110220
-
|
CIM0216
|
TRP Channel
|
Neurological Disease
|
|
CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research.
|
-
- HY-15701
-
|
Leukadherin-1
|
Integrin
Complement System
|
Inflammation/Immunology
|
|
Leukadherin-1, a specific agonist of the leukocyte surface integrin CD11b/CD18, increases CD11b/CD18-dependent cell adhesion to fibrinogen with an EC50 of 4 μM. Leukadherin-1 enhances leukocyte adhesion to ligands (such as ICAM-1) and vascular endothelium and thus reduces leukocyte transendothelial migration and influx to the injury sites. Leukadherin-1 suppresses innate inflammatory signaling.
|
-
- HY-P0172
-
|
ATI-2341
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-117163
-
|
FzM1.8
|
Wnt
β-catenin
|
Cancer
|
|
FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
|
-
- HY-129917
-
|
KB02-JQ1
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
|
-
- HY-B1890
-
-
- HY-P1320A
-
|
[Nphe1]Nociceptin(1-13)NH2 TFA
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
|
-
- HY-P1320
-
|
[Nphe1]Nociceptin(1-13)NH2
|
Opioid Receptor
|
Inflammation/Immunology
|
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
|
-
- HY-120874
-
|
PF-06372865
|
GABA Receptor
|
Neurological Disease
|
|
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
|
-
- HY-137471
-
|
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-131344
-
|
mTOR inhibitor-8
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- HY-136123
-
|
Tubulin inhibitor 8
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
|
-
- HY-136122
-
|
Tubulin inhibitor 7
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
|
-
- HY-136121
-
|
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-112851
-
-
- HY-112812
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-141525
-
-
- HY-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-137497
-
|
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-112722
-
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-112373
-
|
Aurora kinase inhibitor-3
|
Aurora Kinase
|
Others
|
|
Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket.
|
-
- HY-101275
-
-
- HY-111370
-
|
mTOR inhibitor-2
|
mTOR
|
Cancer
|
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
|
-
- HY-13278A
-
-
- HY-21141
-
|
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-119369
-
-
- HY-111412
-
-
- HY-139376
-
|
FGFR1 inhibitor-2
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer.
|
-
- HY-10442
-
-
- HY-112914
-
-
- HY-70005
-
-
- HY-130260
-
-
- HY-128703
-
-
- HY-132809
-
-
- HY-17541A
-
-
- HY-17541
-
-
- HY-138295
-
|
KRAS inhibitor-10
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
|
-
- HY-139077
-
-
- HY-12186
-
|
3-Deazaneplanocin A hydrochloride
DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
|
-
- HY-112807
-
|
SGLT inhibitor-1
|
SGLT
|
Metabolic Disease
|
|
SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
|
-
- HY-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-136706
-
-
- HY-B0385
-
-
- HY-32015
-
|
Cot inhibitor-1
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-115514A
-
|
BRK inhibitor P21d hydrochloride
|
Others
|
Cancer
|
|
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
|
-
- HY-128859
-
|
EMT inhibitor-2
|
Cytochrome P450
|
Metabolic Disease
|
|
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
|
-
- HY-135826
-
-
- HY-P0017
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- HY-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-141476
-
|
PI3K/mTOR Inhibitor-3
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-3 (compound 12), an imidazoline, is a potent PI3K and mTOR dual inhibitor. PI3K/mTOR Inhibitor-3 has anti-cancer activity.
|
-
- HY-119372
-
-
- HY-128917
-
-
- HY-15182
-
-
- HY-112474
-
-
- HY-N2219
-
-
- HY-12400
-
-
- HY-N8120
-
-
- HY-13662
-
-
- HY-13662A
-
-
- HY-132291
-
|
HIV-1 inhibitor-8
|
HIV
|
Infection
|
|
HIV-1 inhibitor-8 is an orally active, low-toxicity and potent HIV‑1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-8 yields exceptionally potent antiviral activities (EC50=4.44~54.5 nM) against various HIV‑1 strains. The IC50 of HIV-1 inhibitor-8 against WT HIV-1 reverse transcriptase is 0.081 μM.
|
-
- HY-128617
-
|
Legumain inhibitor 1
|
Others
|
Cancer
|
|
Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
|
-
- HY-119937
-
-
- HY-15253
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-122723
-
|
GOT1 inhibitor-1
|
Others
|
Cancer
|
|
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-D0886
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135864
-
|
KRAS inhibitor-6
|
Ras
|
Cancer
|
|
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
|
-
- HY-135866
-
|
KRAS inhibitor-8
|
Ras
|
Cancer
|
|
KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
|
-
- HY-111408
-
-
- HY-N2033
-
-
- HY-100463
-
-
- HY-135865
-
|
KRAS inhibitor-7
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
|
-
- HY-112607
-
|
Tubulin inhibitor 1
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-124798
-
-
- HY-32018
-
|
Cot inhibitor-2
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-136813
-
|
Multitarget AD inhibitor-1
|
Beta-secretase
Amyloid-β
|
Neurological Disease
|
Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research.
|
-
- HY-110243
-
|
CAIX Inhibitor S4
|
Carbonic Anhydrase
|
Cancer
|
|
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.
|
-
- HY-17542
-
|
PLpro inhibitor
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-126328
-
|
PKC-theta inhibitor 1
|
PKC
|
Inflammation/Immunology
|
|
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.
|
-
- HY-15760
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-132196
-
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-136717
-
-
- HY-118810
-
-
- HY-B0884
-
-
- HY-112569
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-112906
-
-
- HY-50856A
-
-
- HY-104022
-
-
- HY-117262
-
-
- HY-U00410
-
-
- HY-13276
-
-
- HY-106067A
-
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-131705
-
-
- HY-112355
-
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-104032
-
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-15183
-
-
- HY-U00387
-
-
- HY-107986
-
-
- HY-119692
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-N0565A
-
-
- HY-108322
-
-
- HY-139205
-
-
- HY-112270
-
-
- HY-50880
-
-
- HY-N2221
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-N6031
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-15604A
-
-
- HY-112269
-
-
- HY-128723
-
-
- HY-50879
-
-
- HY-123955
-
|
Casein Kinase inhibitor A86
|
Casein Kinase
CDK
Apoptosis
|
Cancer
|
|
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities.
|
-
- HY-107662
-
|
TCS PrP Inhibitor 13
|
Apoptosis
|
Cancer
Infection
|
|
TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrP C) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis.
|
-
- HY-141659
-
|
USP30 inhibitor 18
|
Deubiquitinase
|
Cancer
|
|
USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-123905A
-
|
LIN28 inhibitor LI71 enantiomer
|
Others
|
Cancer
|
|
LIN28 inhibitor LI71 enantiomer is the enantiomer of LIN28 inhibitor LI71 with less active. LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM.
|
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-16657
-
-
- HY-139536
-
|
MAT2A inhibitor 4
|
Others
|
Cancer
|
|
MAT2A inhibitor 4 is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A). MAT2A inhibitor 4 can be used for the research of cancer.
|
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-119808
-
-
- HY-50900
-
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-W008923
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-101791
-
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-15358
-
|
ALK inhibitor 2
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
|
-
- HY-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-15357
-
|
ALK inhibitor 1
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-113951
-
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-12072
-
|
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-17367A
-
|
Atazanavir sulfate
BMS-232632 sulfate
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
|
Cancer
Infection
|
|
Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CL pro inhibitor with an IC50 of
3.49 μM.
|
-
- HY-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM.
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-139148
-
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-10846
-
-
- HY-B0083
-
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-10451S
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-112913
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-50680
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-114309
-
-
- HY-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859A
-
|
Zidebactam sodium salt
WCK-5107 sodium salt
|
Bacterial
|
Infection
|
|
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-118355
-
|
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-126331
-
-
- HY-12824
-
|
RNPA1000
|
Antibiotic
Bacterial
|
Infection
|
|
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-128888
-
|
WT IDH1 Inhibitor 2
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
WT IDH1 Inhibitor 2 (Compound 3) is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. WT IDH1 Inhibitor 2 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity.
|
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-50706A
-
|
Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-112476
-
|
PRL-3 Inhibitor I
|
Phosphatase
|
Cancer
|
|
PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay.
|
-
- HY-125997
-
|
BTK inhibitor 10
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
|
-
- HY-13228
-
-
- HY-126288
-
|
ERK1/2 inhibitor 2
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
|
-
- HY-16062
-
|
ARQ 621
|
Kinesin
|
Cancer
|
|
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
|
-
- HY-119935
-
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Infection
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-N1447
-
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-15842
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-N8399
-
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-134883
-
-
- HY-P1398A
-
-
- HY-B2007
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
