Search Result
Results for "
Alpha 1 proteinase Inhibitors
" in MCE Product Catalog:
2503
Inhibitors & Agonists
17
Biochemical Assay Reagents
343
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-100740C
-
|
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
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Neurological Disease
|
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(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM.
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- HY-U00333
-
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- HY-147100
-
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α1A-AR Degrader 9c
|
PROTACs
Adrenergic Receptor
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Cancer
|
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α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research.
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- HY-118335
-
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Prazobind
SZL 49
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Adrenergic Receptor
|
Neurological Disease
|
|
Prazobind (SZL 49), a prazosin analog, is a potent alpha 1-adrenoceptor blocker. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC50=1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha 1B (liver) subtypes.
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- HY-106416
-
-
- HY-100554
-
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BMY 7378
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
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BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
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- HY-P1545
-
-
- HY-B2193
-
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α-Amylase
|
Others
|
Others
|
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α-Amylase is a hydrolase enzyme that catalyses the hydrolysis of internal α-1, 4-glycosidic linkages in starch to yield products like glucose and maltose.
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- HY-145419
-
|
IRE1α kinase-IN-4
|
IRE1
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Others
|
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IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α.
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- HY-145420
-
|
IRE1α kinase-IN-5
|
IRE1
|
Others
|
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IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α.
|
-
- HY-145418
-
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IRE1α kinase-IN-3
|
IRE1
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Others
|
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IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α.
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- HY-P1545A
-
-
- HY-108717
-
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Proteinase K
Protease K
|
Ser/Thr Protease
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Others
|
|
Proteinase K (Protease K) is a nonspecific serine protease that is useful for general digestion of proteins. Proteinase K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures. Proteinase K can be use for promoting methods of viral nucleic acid extraction, and detection.
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- HY-106954
-
|
Upidosin
Rec 15/2739; Recordati 15/2739; SB 216469
|
Adrenergic Receptor
|
Inflammation/Immunology
|
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Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction.
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- HY-13671
-
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LW6
HIF-1α inhibitor; LW8
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
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LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
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- HY-N2464
-
-
- HY-17538
-
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- HY-U00399
-
-
- HY-B0471
-
-
- HY-100980
-
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HEAT hydrochloride
BE2254 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
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HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively.
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- HY-151344
-
-
- HY-B0391A
-
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Naftopidil dihydrochloride
KT-611 dihydrochloride; BM-15275 dihydrochloride
|
Adrenergic Receptor
|
Cancer
|
|
Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.
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- HY-B0391B
-
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Naftopidil hydrochloride
KT-611 hydrochloride; BM-15275 hydrochloride
|
Adrenergic Receptor
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Cancer
|
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Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia.
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- HY-B0391
-
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Naftopidil
KT-611; BM-15275
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
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Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
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- HY-B0661
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- HY-A0142
-
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Dapiprazole
|
Adrenergic Receptor
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Endocrinology
|
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Dapiprazole is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole suppresses the opioid withdrawal symptoms. Dapiprazole is also used as eye drops for reversing mydriasis.
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- HY-A0142A
-
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Dapiprazole hydrochloride
|
Adrenergic Receptor
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Endocrinology
|
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Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis.
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- HY-B0471S3
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- HY-B0391S1
-
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Naftopidil-d5
KT-611-d5; BM-15275-d5
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
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Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
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- HY-P3455
-
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Ac-SVVVRT-NH2
|
PGC-1α
|
Cancer
Metabolic Disease
|
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Ac-SVVVRT-NH2 is a PGC-1α modulator that modulates the activity of the human PGC-1α promoter (114%). Ac-SVVVRT-NH2 increases PGC-1α mRNA (125%) and accumulation of intracellular lipids (128%) in subcutaneous human adipocytes. Ac-SVVVRT-NH2 can be used in the research of diseases which is modulated by PGC-1α.
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- HY-115903
-
|
HIF-1α-IN-2
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation.
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- HY-B0471S2
-
-
- HY-B0371B
-
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(R)-Terazosin
|
Adrenergic Receptor
|
Endocrinology
|
|
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
|
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- HY-101491
-
|
SR-18292
|
PGC-1α
Autophagy
|
Metabolic Disease
|
|
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
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- HY-B0391S
-
|
Naftopidil-d3
KT-611-d3; BM-15275-d3
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Naftopidil-d3 (KT-611-d3) is the deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
|
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- HY-B0471S
-
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- HY-17538S
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-
- HY-19371
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- HY-101300
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- HY-103204
-
|
RS100329 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
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RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia.
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- HY-111387
-
-
- HY-15157
-
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Calcitetrol
1α, 24, 25-Trihydroxy VD3
|
VD/VDR
|
Metabolic Disease
|
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Calcitetrol(1α, 24, 25-Trihydroxy VD3) is the hormonally active form of vitamin D with three hydroxyl groups.
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- HY-12519
-
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Oltipraz
RP 35972; NSC 347901
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
Parasite
|
Cancer
|
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Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
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- HY-N6630
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- HY-103239
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- HY-103456
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- HY-B0471S1
-
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Phenylephrine-2,4,6-d3 hydrochloride
(R)-(-)-Phenylephrine-2,4,6-d3 hydrochloride; L-Phenylephrine-2,4,6-d3 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Phenylephrine-2,4,6-d3 ((R)-(-)-Phenylephrine-2,4,6-d3) hydrochloride is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
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- HY-14940
-
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Volinanserin
MDL100907; M 100907
|
5-HT Receptor
|
Neurological Disease
|
|
Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
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-
- HY-110266
-
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GN44028
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.
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- HY-12753A
-
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Debutyldronedarone hydrochloride
SR35021 hydrochloride
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic.
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- HY-10122
-
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Silodosin
KAD 3213; KMD 3213
|
Adrenergic Receptor
Bacterial
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Cancer
Endocrinology
|
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Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
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- HY-113212
-
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Ursocholic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
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Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
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- HY-D1606
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BODIPY FL prazosin
|
Adrenergic Receptor
|
Metabolic Disease
|
|
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with Ki values of 14.5, 43.3 nM for α1a-AR and α1b-AR, respectively. BODIPY FL prazosin also is a fluorescent ligand with the excitation and emission wavelengths are 485 and 535 nm, respectively. BODIPY FL prazosin can be used for study the differences in the subcellular localization of α1-adrenoceptor subtypes.
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- HY-139697
-
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- HY-147813
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- HY-P3150
-
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Recombinant Proteinase K
|
Ser/Thr Protease
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Others
|
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Recombinant Proteinase K is a serine protease that cleaves the carboxy-terminated peptide bonds of aliphatic and aromatic amino acids. Recombinant Proteinase K can be used to digest proteins and remove contamination from nucleic acid preparations.
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- HY-12519S
-
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Oltipraz-d3
RP 35972-d3; NSC 347901-d3
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
|
Cancer
|
|
Oltipraz-d3 (RP 35972-d3) is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
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- HY-101385
-
-
- HY-U00110
-
-
- HY-10122S
-
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Silodosin-d4
|
Adrenergic Receptor
|
Cancer
Endocrinology
|
|
Silodosin-d4 (KAD 3213-d4) is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
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- HY-15672
-
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FM19G11
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Neurological Disease
|
|
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
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- HY-113960
-
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ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
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- HY-112910
-
-
- HY-111188
-
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A55453
|
Adrenergic Receptor
|
Others
|
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A55453 is a prazosin analogue and a potent α1-adrenergic antagonist. 125I-A55453 is a high-affinity alpha 1-adrenergic receptor probe.
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- HY-P1266
-
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α-Conotoxin EI
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin EI is a selective nicotinic acetylcholine α1β1γδ receptor (nAChR) antagonist (IC50=187 nM) and an α3β4 receptor inhibitor. α-Conotoxin EI can block muscle and ganglionic receptors.
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- HY-117071
-
-
- HY-15746
-
-
- HY-15746A
-
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Dobutamine
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Adrenergic Receptor
|
Endocrinology
Cardiovascular Disease
|
|
Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion.
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- HY-14940S
-
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Volinanserin-d4 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Volinanserin-d4 (MDL100907-d4) hydrochloride is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
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- HY-103446
-
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- HY-P3653
-
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α-Conotoxin M I
|
mAChR
nAChR
|
Neurological Disease
|
|
α-Conotoxin M I is a potent and selective inhibitor of mAChR and α1β1γδ nAChR, but has no effect on nicotine-stimulated dopamine release. α-Conotoxins are small, disulfide-rich peptides that competitively inhibit muscle and neuronal nicotinic AChRs.
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- HY-B0371D
-
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(S)-Terazosin
|
Adrenergic Receptor
|
Endocrinology
|
|
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively.
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- HY-147708
-
|
T-Type calcium channel inhibitor 2
|
Calcium Channel
|
Cancer
|
|
T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively.
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- HY-15746B
-
-
- HY-15746S1
-
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(rac)-Dobutamine-d6 hydrochloride
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
(Rac)-Dobutamine-d6 hydrochloride is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion.
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- HY-15746S
-
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(rac)-Dobutamine-d4 hydrochloride
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Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
(Rac)-Dobutamine-d4 hydrochloride is a labelled racemic Dobutamine hydrochloride. Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion.
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- HY-146144
-
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HIF-IN-1
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity.
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- HY-107526
-
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(Rac)-ALX 5407
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
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- HY-151465
-
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HIF-1α-IN-4
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HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer.
|
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- HY-134863
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-
- HY-16579
-
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Etifoxine hydrochloride
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
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- HY-16579A
-
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Etifoxine
HOE 36-801
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GABA Receptor
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Neurological Disease
|
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
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- HY-12749
-
-
- HY-N0242
-
-
- HY-P3612
-
|
CTCE-0214
|
CXCR
|
Inflammation/Immunology
|
|
CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research.
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- HY-B0354A
-
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- HY-135552
-
-
- HY-12749A
-
-
- HY-B0769
-
-
- HY-151466
-
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HIF-1α-IN-5
|
HIF/HIF Prolyl-Hydroxylase
Monoamine Oxidase
|
Cancer
|
|
HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer.
|
-
- HY-B1435
-
-
- HY-B0716
-
-
- HY-12767
-
-
- HY-112769
-
|
EX229
|
AMPK
|
Metabolic Disease
|
|
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
|
-
- HY-16579AS2
-
|
Etifoxine-d5
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine-d5 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-16579AS
-
|
Etifoxine-d3
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine-d3 is the deuterium labeled Etifoxine. Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-107824
-
-
- HY-U00206
-
-
- HY-B0098
-
-
- HY-B0098A
-
-
- HY-115746
-
-
- HY-146540
-
|
GEM-5
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
MDM-2/p53
|
Cancer
|
|
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth.
|
-
- HY-16560
-
-
- HY-12760
-
-
- HY-123563
-
-
- HY-U00237
-
-
- HY-151341
-
|
HIF-1/2α-IN-1
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) [1].
|
-
- HY-14571
-
|
E7820
ER68203-00
|
Integrin
|
Cancer
|
|
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
|
-
- HY-B0459
-
-
- HY-G0008
-
-
- HY-G0008A
-
-
- HY-16708A
-
|
ZLN024 hydrochloride
|
AMPK
|
Metabolic Disease
|
|
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-16708
-
|
ZLN024
|
AMPK
|
Metabolic Disease
|
|
ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-15282
-
-
- HY-W001692
-
-
- HY-103683
-
-
- HY-N2024
-
-
- HY-126477
-
|
NNK
|
Endogenous Metabolite
|
Cancer
|
|
NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα. NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure.
|
-
- HY-10626
-
|
T0901317
|
LXR
FXR
ROR
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
|
-
- HY-16560S
-
|
Camptothecin-d5
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Cancer
Infection
|
|
Camptothecin-d5 (Campathecin-d5) is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
|
-
- HY-107326
-
-
- HY-112426
-
-
- HY-101815
-
-
- HY-P99246
-
-
- HY-120823
-
-
- HY-B0192AS
-
-
- HY-131591
-
-
- HY-101690
-
-
- HY-N7439
-
|
Mogroside VI B
|
PGC-1α
|
Metabolic Disease
|
|
Mogroside VI B, a cucurbitane glucoside, separated from the crude extract of Siraitia grosvenorii. Mogroside VI B shows effect on activating PGC-1α transcription.
|
-
- HY-10231
-
-
- HY-12717
-
|
Phentolamine
|
Adrenergic Receptor
|
Endocrinology
|
|
Phentolamine is a potent, selective and orally active α1 adrenergic and α2 adrenergic receptor antagonist. Phentolamine can be used for the treatment of erectile dysfunction.
|
-
- HY-101562
-
|
Inavolisib
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
|
-
- HY-B0459A
-
-
- HY-B0716S1
-
-
- HY-135270
-
-
- HY-W013150
-
-
- HY-16031
-
-
- HY-13715
-
-
- HY-13715A
-
-
- HY-11087
-
-
- HY-A0077
-
-
- HY-A0077A
-
-
- HY-B0639
-
|
Amifostine
WR2721
|
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action.
|
-
- HY-13715B
-
-
- HY-101336
-
-
- HY-U00365
-
-
- HY-131449
-
-
- HY-Y0313
-
-
- HY-103505
-
|
CL 218872
|
GABA Receptor
|
Neurological Disease
|
|
CL 218872 is a selective and orally active benzodiazepine of α1 subunit-containing GABA Areceptor with a Ki of 130 nM. CL 218872 exerts anxiolytic and anticonvulsant in vivo.
|
-
- HY-W009009
-
|
L-838417
|
GABA Receptor
|
Neurological Disease
|
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
|
-
- HY-147038
-
|
AMPK activator 8
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC50s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.
|
-
- HY-13715C
-
-
- HY-107532
-
-
- HY-P3149B
-
|
LEESGGGLVQPGGSMK acetate
|
TNF Receptor
|
Inflammation/Immunology
|
|
LEESGGGLVQPGGSMK acetate, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK acetate can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
|
-
- HY-P3149
-
|
LEESGGGLVQPGGSMK
|
TNF Receptor
|
Inflammation/Immunology
|
|
LEESGGGLVQPGGSMK, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
|
-
- HY-B0639A
-
|
Amifostine trihydrate
WR2721 trihydrate
|
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action.
|
-
- HY-N1098
-
-
- HY-106554
-
-
- HY-B0006B
-
-
- HY-12720
-
-
- HY-N6782
-
|
Oligomycin
|
ATP Synthase
Fungal
Antibiotic
|
Cancer
Infection
|
|
Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
|
-
- HY-P3149A
-
|
LEESGGGLVQPGGSMK TFA
|
TNF Receptor
|
Inflammation/Immunology
|
|
LEESGGGLVQPGGSMK TFA, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK TFA can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
|
-
- HY-B0716S
-
-
- HY-B0098S
-
-
- HY-107406
-
|
Antimycin A1
|
Mitochondrial Metabolism
|
Cancer
|
|
Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
|
-
- HY-B1803A
-
|
Tracazolate hydrochloride
ICI 136753 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
|
-
- HY-100991
-
|
FG 7142
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
|
-
- HY-N4334
-
-
- HY-12774
-
-
- HY-U00367
-
-
- HY-B0354AS
-
-
- HY-128671
-
-
- HY-107371
-
-
- HY-B0006C
-
-
- HY-B0192AS1
-
-
- HY-N4332
-
-
- HY-142693
-
-
- HY-12720A
-
|
Apraclonidine hydrochloride
ALO 2145
|
Adrenergic Receptor
|
Neurological Disease
|
|
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid.
|
-
- HY-N0877
-
|
Bufalin
|
Na+/K+ ATPase
|
Cancer
|
|
Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
|
-
- HY-19727A
-
-
- 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-103040
-
|
Zuranolone
|
GABA Receptor
|
Neurological Disease
|
|
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
|
-
- HY-B0661A
-
-
- HY-N7142
-
-
- HY-N6969
-
|
Dicentrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Dicentrine is a natural product isolated from the plant Stephania epigaea Lo with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates.
|
-
- HY-U00165
-
-
- HY-N2160
-
|
6'''-Feruloylspinosin
|
GABA Receptor
|
Neurological Disease
|
|
6'''-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6'''-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
|
-
- HY-P99235
-
|
Nadunolimab
|
Interleukin Related
|
Cancer
|
|
Nadunolimab is a human monoclonal IgG1 antibody targeting IL1RAP. Nadunolimab blocks IL-1α and IL-1β signaling and triggering antibody-dependent cellular cytotoxicity. Nadunolimab can be used in research of cancer.
|
-
- HY-13715S
-
-
- HY-19727
-
-
- HY-101366
-
-
- HY-136010
-
-
- HY-123840
-
|
MRK-623
|
GABA Receptor
|
Neurological Disease
|
|
MRK-623 (Compound 14k) is an orally active, high-affinity GABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect.
|
-
- HY-148252
-
|
ADRA1D receptor antagonist 1 free base
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
|
-
- HY-111255
-
|
SPD304
|
TNF Receptor
|
Cancer
|
|
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
|
-
- HY-111255A
-
|
SPD304 dihydrochloride
|
TNF Receptor
|
Inflammation/Immunology
|
|
SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
|
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
Antibiotic
|
Cancer
Infection
|
|
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
|
-
- HY-121186
-
-
- HY-114794
-
-
- HY-100369A
-
|
DMCM hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
|
-
- HY-126236
-
-
- HY-134103
-
|
ddGTP
2′,3′-Dideoxyguanosine 5′-triphosphate
|
DNA/RNA Synthesis
|
Others
|
|
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing. ddGTP acts as an inhibitor or a substrate for DNA polymerase α.
|
-
- HY-16196
-
|
ENMD-1198
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-101514
-
-
- HY-N4331
-
-
- HY-N4333
-
-
- HY-121383
-
-
- HY-B0379A
-
|
Adiphenine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects.
|
-
- HY-17034A
-
|
Dexmedetomidine hydrochloride
(+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects.
|
-
- HY-B0362A
-
|
Phentolamine mesylate
Phentolamine methanesulfonate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
|
-
- HY-12719
-
|
Dexmedetomidine
(+)-Medetomidine; (S)-Medetomidine
|
Adrenergic Receptor
|
Neurological Disease
|
|
Dexmedetomidine ((+)-Medetomidine) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine exhibits anxiolysis, sedation, and modest analgesia effects.
|
-
- HY-D1532
-
-
- HY-114174
-
|
Fmoc-Ala-Glu-Asn-Lys-NH2
|
Amyloid-β
|
Neurological Disease
|
|
Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing.
|
-
- HY-107201
-
|
β-Cyclodextrin
|
Influenza Virus
|
Infection
|
|
β-Cyclodextrin is a cyclic polysaccharide composed of seven units of glucose (α-D-glucopyranose) linked by α-(1,4) type bonds. β-Cyclodextrin has often been used to enhance the solubility of drugs. β-Cyclodextrin has anti-influenza virus H1N1 activities.
|
-
- HY-B0006BS
-
|
(S)-Carvedilol-d4
(S)-BM 14190-d4
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
(S)-Carvedilol-d4 is deuterium labeled (S)-Carvedilol. (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).
|
-
- HY-101815S
-
-
- HY-Y0313S
-
-
- HY-117623
-
|
PF-06685249
PF-249
|
AMPK
|
Metabolic Disease
|
|
PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 can be used for diabetic nephropathy research.
|
-
- HY-B0702
-
-
- HY-B0061
-
|
Tandospirone citrate
SM-3997 citrate
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
|
-
- HY-134103A
-
|
ddGTP trisodium
2′,3′-Dideoxyguanosine 5′-triphosphate trisodium
|
DNA/RNA Synthesis
|
Others
|
|
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) trisodium is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing. ddGTP trisodium acts as an inhibitor or a substrate for DNA polymerase α.
|
-
- HY-13740S
-
-
- HY-10791
-
-
- HY-108137
-
|
Z-LVG-CHN2
|
Cathepsin
HSV
SARS-CoV
|
Infection
Inflammation/Immunology
|
|
Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease.
|
-
- HY-18371
-
|
TC-S 7009
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
|
-
- HY-19505
-
|
TPA-023B
|
GABA Receptor
|
Neurological Disease
|
|
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.
|
-
- HY-B0219A
-
-
- HY-B0219
-
-
- HY-B0192A
-
|
Alfuzosin hydrochloride
SL 77499-10
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (SL 77499-10) hydrochloride is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin hydrochloride relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin hydrochloride can be used in study of benign prostatic hyperplasia (BPH).
|
-
- HY-B0192
-
|
Alfuzosin
SL 77499
|
Adrenergic Receptor
|
Endocrinology
|
|
Alfuzosin (SL 77499-10) is an orally active, selective and competitive α1-adrenoceptor antagonist. Alfuzosin relaxes the muscles of the prostate and bladder neck, aiding in urination. Alfuzosin can be used in study of benign prostatic hyperplasia (BPH).
|
-
- HY-100290
-
-
- HY-111969
-
|
BT18
|
Others
|
Neurological Disease
|
|
BT18 is a molecule mimic with function similar to glial cell line-derived neurotrophic factor (GDNF). BT18 shows an effect on GDNF family receptor GFRα1 and RET receptor tyrosine kinase RetA function.
|
-
- HY-B1494
-
|
Picrotoxinin
|
Chloride Channel
GABA Receptor
|
Neurological Disease
|
|
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM.
|
-
- HY-11048
-
|
NS11394
|
GABA Receptor
|
Neurological Disease
|
|
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
|
-
- HY-N5136
-
|
25(R,S)-Ruscogenin
|
Apoptosis
PI3K
Akt
mTOR
|
Cancer
|
|
Ruscogenin suppresses HCC metastasis by reducing the expression of MMP-2, MMP-9, uPA, VEGF and HIF-1α via regulating the PI3K/Akt/mTOR signaling pathway. And Ruscogenin alleviates LPS-induced pulmonary endothelial cell apoptosis by su
|
-
- HY-B0661AS1
-
-
- HY-B0371
-
|
Terazosin
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
|
-
- HY-B0661AS
-
-
- HY-B0371F
-
|
Terazosin hydrochloride
|
Adrenergic Receptor
|
Endocrinology
Metabolic Disease
|
|
Terazosin hydrochloride is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
|
-
- HY-N0596
-
|
Panaxadiol
20(R)-Panaxadiol
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities.
|
-
- HY-122762
-
|
Cetraxate hydrochloride
DV-1006
|
Ser/Thr Protease
|
Inflammation/Immunology
|
|
Cetraxate hydrochloride (DV-1006), an orally active anti-ulcer agent with mucosal protective effects, can be used for gastric ulcers research. Cetraxate hydrochloride is a potent acrosomal proteinase acrosin inhibitor with a Ki and an IC50 of 0.94 μM and 3.3 μM, respectively.
|
-
- HY-14903
-
|
Ulimorelin
TZP-101
|
GHSR
Adrenergic Receptor
|
Metabolic Disease
|
|
Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
|
-
- HY-12987
-
-
- HY-B0006CS
-
|
(R)-Carvedilol-d4
(R)-BM 14190-d4
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
(R)-Carvedilol-d4 is deuterium labeled (R)-Carvedilol. (R)-Carvedilol ((R)-BM 14190), the R-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).
|
-
- HY-Y0313S1
-
-
- HY-107489
-
|
RO 4938581
|
GABA Receptor
|
Neurological Disease
|
|
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
|
-
- HY-100536
-
|
IWP-3
|
Wnt
|
Cancer
|
|
IWP-3 is an potent inhibitor of Wnt production with an IC50 of 40 nM. IWP-3 inhibits Porcupine (Porcn) function thereby blocking palmitoylation of Wnt proteins. IWP-3 inhibits CK1γ3 and CK1ε only moderately and does not inhibit CK1α.
|
-
- HY-N5112B
-
|
β,β-Dimethylacrylshikonin
Isoarnebin I
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Lithospermum erythrorhizon Sieb. et Zucc. , promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
|
-
- HY-19731
-
|
SID 3712249
MiR-544 Inhibitor 1
|
MicroRNA
Apoptosis
|
Cancer
|
|
SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer.
|
-
- HY-15205
-
|
Ganetespib
STA-9090
|
HSP
Apoptosis
|
Cancer
|
|
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3.
|
-
- HY-122058A
-
|
KRH-3955 hydrochloride
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
|
-
- HY-P1091
-
|
Hemopressin (human, mouse)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models.
|
-
- HY-N7142S
-
|
DL-Norepinephrine-d6 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
DL-Norepinephrine-d6 hydrochloride is the deuterium labeled DL-Norepinephrine hydrochloride. DL-Norepinephrine hydrochloride is a synthetic phenylethylamine that mimics the sympathomimetic actions of the endogenous norepinephrine．DL-Norepinephrine hydrochloride is a neurotransmitter targets α1 and β1 adrenoceptors, has an increasing effect on subendocardial oxygen tension.
|
-
- HY-B0781
-
-
- HY-120270
-
|
PF-06679142
|
AMPK
|
Metabolic Disease
|
|
PF-06679142 (Compound 10) is a potent, orally active AMPK activator with an EC50 of 22 nM against α1β1γ1-AMPK. PF-06679142 can be used for diabetic nephropathy research.
|
-
- HY-103512
-
|
TP003
|
GABA Receptor
|
Neurological Disease
|
|
TP003 is a non-selective benzodiazepine site agonist with EC50s of 20.3, 10.6, 3.24, 5.64 nM for α1β2γ2, α2β3γ2, α3β3γ2, α5β2γ2, respectively. TP003 induces anxiolysis via α2GABAA receptors.
|
-
- HY-15800
-
|
CZC-25146 hydrochloride
|
LRRK2
|
Inflammation/Immunology
Neurological Disease
|
|
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.
|
-
- HY-B0379AS
-
|
Adiphenine-d4 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Adiphenine-d4 hydrochloride is the deuterium labeled Adiphenine hydrochloride. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects.
|
-
- HY-N1919
-
-
- HY-N1919A
-
-
- HY-B0371A
-
|
Terazosin hydrochloride dihydrate
|
Adrenergic Receptor
|
Endocrinology
Metabolic Disease
|
|
Terazosin hydrochloride dihydrate is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin hydrochloride dihydrate works by relaxing blood vessels and the opening of the bladder. Terazosin hydrochloride dihydrate has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
|
-
- HY-101641
-
-
- HY-B0413S
-
|
Fenbendazole-d3
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Antibiotic
|
Infection
|
|
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole is a benzimidazole anthelmintic. Fenbendazole is active against Giardia in vitro (IC50 = 0.3 μM). Fenbendazole (20 mg/kg) prevents infiltration of parasites into the brain in a rabbit model of E. cuniculi infection. Fenbendazole also activates HIF-1α and prevents oxidative stress-induced death in primary neurons in vitro.
|
-
- HY-125838
-
|
J30-8
|
JNK
|
Neurological Disease
|
|
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases.
|
-
- HY-120087
-
|
KG-548
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
KG-548 is an ARNT/TACC3 disruptor and a HIF-1α inhibitor. KG-548 directly interferes with ARNT/TACC3 complex formation by competing with TACC3 for binding to the ARNT PAS-B domain. ARNT is the aryl hydrocarbon receptor nuclear translocator, also known as HIF-β.
|
-
- HY-103413
-
|
Eticlopride hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent.
|
-
- HY-A0019
-
|
Paliperidone
9-Hydroxyrisperidone
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-N6775
-
|
Sonolisib
PX-866
|
PI3K
|
Cancer
|
|
Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
|
-
- HY-19037
-
|
SM-2470
|
Adrenergic Receptor
|
Metabolic Disease
Neurological Disease
|
|
SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats. SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization.
|
-
- HY-15893
-
|
DMOG
Dimethyloxallyl Glycine
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Cancer
|
|
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
|
-
- HY-115463
-
|
EB-3D
|
AMPK
Apoptosis
|
Cancer
|
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
|
-
- HY-N1987
-
|
Cucurbitacin IIb
|
Apoptosis
|
Inflammation/Immunology
|
|
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
|
-
- HY-12717AS
-
|
Phentolamine-d4 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Phentolamine-d4 (Phentolamine-d4) hydrochloride is the deuterium labeled Phentolamine hydrochloride. Phentolamine hydrochloride is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine hydrochloride can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
|
-
- HY-P1090
-
|
Hemopressin(rat)
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models.
|
-
- HY-12962
-
|
NMDA-IN-1
|
iGluR
|
Neurological Disease
|
|
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
|
-
- HY-P1091A
-
|
Hemopressin(human, mouse) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-108509
-
-
- HY-103520
-
|
DS2
|
GABA Receptor
|
Neurological Disease
|
|
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research.
|
-
- HY-151361
-
|
AMPK-IN-3
|
AMPK
|
Cancer
|
|
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer.
|
-
- HY-15800A
-
|
CZC-25146
|
LRRK2
|
Inflammation/Immunology
Neurological Disease
|
|
CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases.
|
-
- HY-B0006A
-
-
- HY-B0371S
-
|
Terazosin-d8
|
Adrenergic Receptor
|
Metabolic Disease
Endocrinology
|
|
Terazosin-d8 is deuterium labeled Terazosin. Terazosin is a quinazoline derivative and a competitive and orally active α1-adrenoceptor antagonist. Terazosin works by relaxing blood vessels and the opening of the bladder. Terazosin has the potential for benign prostatic hyperplasia (BPH) and high blood pressure treatment.
|
-
- HY-101755
-
-
- HY-P1090A
-
|
Hemopressin(rat) TFA
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-129453
-
|
BOP sodium
|
Integrin
|
Inflammation/Immunology
|
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
|
-
- HY-105670
-
|
PHA-543613
|
nAChR
|
Neurological Disease
|
|
PHA-543613 is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki of 8.8 nM. PHA-543613 displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
|
-
- HY-105670B
-
|
PHA-543613 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
|
-
- HY-A0019S
-
|
Paliperidone-d4
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-17034AS
-
|
Dexmedetomidine-13C,d3 hydrochloride
(+)-Medetomidine-13C,d3 hydrochloride; (S)-Medetomidine-13C,d3 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine-13C,d3 (hydrochloride) is the 13C- and deuterium labeled Dexmedetomidine (hydrochloride). Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects.
|
-
- HY-B0223
-
-
- HY-100370
-
|
MRK-016
|
GABA Receptor
|
Cancer
|
|
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
|
-
- HY-B0006
-
-
- HY-B0781S
-
-
- HY-120619
-
|
BMS-193885
|
Neuropeptide Y Receptor
|
Neurological Disease
Endocrinology
|
|
BMS-193885 is a potent, selective, competitive, and brain penetrant neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM, and has an IC50 of 5.9 nM for hY1, which displays > 100, > 160, > 160 and > 160-fold selectivity over α1, hY2, hY4 and hY5 receptors, respectively [1] .
|
-
- HY-103521
-
|
Anxiolytic/nonsedative agent-1
|
GABA Receptor
|
Neurological Disease
|
|
Anxiolytic/nonsedative agent-1 (compound 2b) is a potent and selective GABAA agonist. Anxiolytic/nonsedative agent-1 shows appreciable affinity for the BzR in bovine brain membranes with Kis of 14, 121, 239 nM for α1β2γ2, α2β2γ2, α5β3γ2, respectively. Anxiolytic/nonsedative agent-1 shows α2 selective efficacy in vitro and anxioselective effects in vivo.
|
-
- HY-103511
-
|
TCS1105
|
Others
|
Neurological Disease
|
|
TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion.
|
-
- HY-14649S2
-
|
11-cis-Retinoic Acid-d5
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-B0239
-
|
Chloramphenicol
|
Antibiotic
Bacterial
HIF/HIF Prolyl-Hydroxylase
VEGFR
Autophagy
Apoptosis
Beclin1
JNK
Akt
MMP
|
Cancer
Infection
|
|
Chloramphenicol is an orally active, potent and broad-spectrum antibiotic. Chloramphenicol shows antibacterial activity. Chloramphenicol represses the oxygen-labile transcription factor and hypoxia inducible factor-1 alpha (HIF-1α) in hypoxic A549 and H1299 cells. Chloramphenicol suppresses the mRNA levels of vascular endothelial growth factor (VEGF) and glucose transporter 1, eventually decreasing VEGF release. Chloramphenicol can be used for anaerobic infections and lung cancer research.
|
-
- HY-N6607
-
-
- HY-B0702S
-
|
Nicergoline-13C,d3
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
Nicergoline-13C,d3 is the 13C- and deuterium labeled Nicergoline. Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.
|
-
- HY-19357
-
-
- HY-110282
-
|
S3QEL-2
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation.
|
-
- HY-B0135A
-
|
Furosemide sodium
|
NKCC
GABA Receptor
|
Cancer
Metabolic Disease
|
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-B0135
-
|
Furosemide
|
NKCC
GABA Receptor
|
Metabolic Disease
Cancer
|
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-120337
-
|
V-11-0711
|
Others
|
Cancer
|
|
V-11-0711 is a potent and selective choline kinase alpha (ChoKα) inhibitor with an IC50 of 20 nM. V-11-0711 causes a reversible growth arrest in HeLa cells.
|
-
- HY-B0006S
-
|
Carvedilol-d3
|
Adrenergic Receptor
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
AA is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
|
-
- HY-12987S1
-
-
- HY-N0761
-
|
Isoferulic acid
3-Hydroxy-4-methoxycinnamic acid
|
Adrenergic Receptor
Influenza Virus
|
Infection
Endocrinology
Metabolic Disease
|
|
Isoferulic acid (3-Hydroxy-4-methoxycinnamic acid) is a cinnamic acid derivative that has antidiabetic activity. Isoferulic acid binds to and activates α1-adrenergic receptors (IC50=1.4 µM) to enhance secretion of β-endorphin (EC50=52.2 nM) and increase glucose use. Isoferulic acid also has anti-influenza virus activities.
|
-
- HY-10233
-
|
Gaboxadol hydrochloride
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid agent.
|
-
- HY-12987S
-
-
- HY-103093
-
|
Zotepine
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.
|
-
- HY-B0988
-
-
- HY-17412A
-
-
- HY-B1625
-
-
- HY-17412
-
-
- HY-B0006S2
-
|
Carvedilol-d5
BM 14190-d5
|
Adrenergic Receptor
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Carvedilol-d5 is deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
|
-
- HY-19686
-
|
Ipsapirone
TVX Q 7821 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function.
|
-
- HY-111052
-
|
AZD7325
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
Neurological Disease
|
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
|
-
- HY-B0135S
-
|
Furosemide-d5
|
NKCC
GABA Receptor
|
Metabolic Disease
Cancer
|
|
Furosemide-d5 is the deuterium labeled Furosemide. Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-N2187
-
|
Deoxyshikonin
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Infection
Cardiovascular Disease
|
|
Deoxyshikonin is isolated from Arnebia euchroma with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
|
-
- HY-135482
-
|
GABAA receptor agent 2 TFA
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3).
|
-
- HY-100943
-
|
Cinanserin hydrochloride
SQ 10643
|
5-HT Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
|
-
- HY-B0006S1
-
|
Carvedilol-d4
BM 14190-d4
|
Adrenergic Receptor
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Carvedilol-d4 (BM 14190-d4) is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
|
-
- HY-B0193A
-
|
Prazosin hydrochloride
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
|
-
- HY-12286
-
|
PI-1840
|
Proteasome
Apoptosis
Autophagy
Caspase
Bcl-2 Family
NF-κB
PARP
|
Cancer
|
|
PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.
|
-
- HY-147423
-
-
- HY-15780A
-
|
Brexpiprazole hydrochloride
OPC-34712 hydrochloride
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
|
-
- HY-P2657
-
|
Verucopeptin
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-15780
-
|
Brexpiprazole
OPC-34712
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic drug, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
|
-
- HY-N1163
-
-
- HY-B0892S
-
|
Benzyl alcohol-α-13C-α,α-d2
Benzenemethanol-α-13C-α,α-d2
|
Endogenous Metabolite
|
Others
|
|
Benzyl alcohol-α-13C-α,α-d2 (Benzenemethanol-α-13C-α,α-d2) is the 13C-labeled Benzyl alcohol. Benzyl alcohol is an aromatic alcohol; a colorless liquid with a mild pleasant aromatic odor.
|
-
- HY-150536
-
|
EP39
|
HIV
HIV Protease
|
Infection
|
|
EP39 is a potent HIV-1 maturation inhibitor. EP39 interacts with the SP1 domain of Gag. EP39 decreases the dynamics of CA-SP1 junction, by binding to the QVT motif of the SP1 domain, and perturbs the natural coil-helix equilibrium on both sides of the SP1 domain by stabilizing the transient alpha helical structure. EP39 acts by arresting maturation of HIV-1 thereby blocking its infectivity.
|
-
- HY-107625A
-
|
SNAP 94847 hydrochloride
|
MCHR1 (GPR24)
|
Neurological Disease
|
|
SNAP 94847 hydrochloride is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-107625
-
|
SNAP 94847
|
MCHR1 (GPR24)
|
Neurological Disease
Endocrinology
|
|
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters.
|
-
- HY-10349A
-
|
WAY-100635 Maleate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.
|
-
- HY-15536A
-
-
- HY-146225
-
|
α-Amylase/α-Glucosidase-IN-2
|
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-2 (compound 5) is a potent α-amylase and α-glucosidase dual inhibitor with IC50 values of 13.02, 13.09 µM for α-amylase and α-glucosidase, respectively. α-Amylase/α-Glucosidase-IN-2 has the potential for the research of diabetic complications.
|
-
- HY-147711
-
|
α-Amylase/α-Glucosidase-IN-1
|
Glucosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia.
|
-
- HY-12799
-
-
- HY-N2853
-
|
D-α-Tocopherylquinone
α-Tocopherylquinone
|
Others
|
Cancer
|
|
D-α-Tocopherylquinone (α-Tocopherylquinone) is a quinone, can be isolated from Phaeodactylum tricornutum. D-α-Tocopherylquinone is a oxidation product of α-Tocopherol (vitamin E). D-α-Tocopherylquinone can act as an anticoagulant and as an antioxidant.
|
-
- HY-B1204S
-
|
Histamine-α,α,β,β-d4 dihydrochloride
Ergamine-α,α,β,β-d4 dihydrochloride
|
Histamine Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
Cancer
|
|
Histamine-α,α,β,β-d4 (Ergamine-α,α,β,β-d4) dihydrochloride is the deuterium labeled Histamine. Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
|
-
- HY-N9487
-
-
- HY-N10564
-
|
8α,9α-Epoxycoleon-U-quinone
|
P-glycoprotein
|
Cancer
|
|
8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX.
|
-
- HY-N2514
-
|
α-Lactose
α-D-Lactose
|
Others
|
Others
|
|
α-Lactose (α-D-Lactose) is the major sugar present in milk. Lactose exists in the form of two anomers, α and β. The α form normally crystallizes as a monohydrate.
|
-
- HY-131997
-
|
2'MeO6MF
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and psychomotor stabilizing properties. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
|
-
- HY-N9960
-
-
- HY-14541
-
|
Olanzapine
LY170053
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
|
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
|
-
- HY-12697A
-
|
NGB 2904 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis. NGB 2904 hydrochloride can inhibit Cocaine's rewarding effects and Cocaine-induced reinstatement of drug-seeking behavior.
|
-
- HY-P2802
-
|
α-Glucosidase
α-D-Glucosidase
|
Glucosidase
Others
|
Metabolic Disease
|
|
α-Glucosidase (α-D-Glucosidase), a carbohydrate hydrolyzing enzyme, catalyzes the liberation of α-glucose from the non-reducing end of the substrate. α-Glucosidase can facilitate the absorption of glucose by the small intestine. Inhibition of α-Glucosidase is an effective management of non-insulin-dependent diabetes mellitus (NIDDM).
|
-
- HY-N1467
-
|
(-)-α-Terpineol
(S)-α-Terpineol
|
Others
|
Others
|
|
(-)-α-Terpineol ((S)-α-Terpineol), a monoterpene compound, is one of compounds in Melaleuca alternifolia.
|
-
- HY-N0683
-
-
- HY-123076
-
|
Pifithrin-α, p-Nitro, Cyclic
PFN-α
|
MDM-2/p53
|
Neurological Disease
|
|
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
|
-
- HY-N1720
-
-
- HY-P1365
-
|
α-Conotoxin MII
α-CTxMII
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors [1].
|
-
- HY-123489
-
-
- HY-113962S
-
-
- HY-N0611
-
|
alpha-Boswellic acid
α-Boswellic acid
|
Others
|
Inflammation/Immunology
|
|
alpha-Boswellic acid (α-Boswellic acid) is a pentacyclic triterpene compound from extracts of Frankincense, has anticonvulsant and anti-cancer properties. alpha-Boswellic acid prevents and decreases the progression of Alzheimer’s hallmarks in vivo and can be used for Alzheimer’s disease research.
|
-
- HY-W020044
-
|
DL-alpha-Tocopherol
DL-α-Tocopherol
|
Ferroptosis
|
Others
|
|
DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB.
|
-
- HY-B1371A
-
-
- HY-P1264
-
|
α-Bungarotoxin
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
|
-
- HY-N0683A
-
-
- HY-N0700
-
-
- HY-102022
-
|
α-Galactosylceramide
α-GalCer; KRN7000
|
Others
|
Cancer
Inflammation/Immunology
|
|
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).
|
-
- HY-118135
-
|
4-Methylumbelliferyl-α-D-galactopyranoside
4MU-α-Gal
|
Others
|
Others
|
|
4-Methylumbelliferyl-α-D-galactopyranoside (4MU-α-Gal), a substrate for α-galactosidase A (GLA), is a blue pro-fluorogenic substrate. 4-Methylumbelliferyl-α-D-galactopyranoside forms two products, galactose and fluorescent 4MU, upon cleavage by GLA.
|
-
- HY-N0255
-
|
alpha-Hederin
α-Hederin
|
Apoptosis
|
Others
|
|
alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway.
|
-
- 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-N0492
-
|
α-Lipoic Acid
Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
|
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
|
-
- HY-N0492A
-
|
α-Lipoic Acid sodium
Thioctic acid sodium; (±)-α-Lipoic acid sodium; DL-α-Lipoic acid sodium
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
|
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1.
|
-
- HY-120877
-
|
MRT199665
|
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
|
-
- HY-10564
-
|
Sarpogrelate hydrochloride
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
|
-
- HY-P1365A
-
|
α-Conotoxin MII TFA
α-CTxMII TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors [1].
|
-
- HY-P9908A
-
-
- HY-123489S
-
|
3α,21-Dihydroxy-5α-pregnan-20-one-d3
THDOC-d3
|
GABA Receptor
|
Neurological Disease
|
|
3α,21-Dihydroxy-5α-pregnan-20-one-d3 (THDOC-d3) is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
|
-
- HY-P0252
-
-
- HY-N0710
-
|
alpha-Cyperone
α-Cyperone; (+)-α-Cyperone
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
alpha-Cyperone (α-Cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1, resulting in reduction of inflammation, which would be highly beneficial for treatment of inflammatory diseases such as AD.
|
-
- HY-N8423
-
|
α-Amyrin
|
Others
|
Inflammation/Immunology
|
|
α-Amyrin is a pentacyclic triterpenoid. α-Amyrin has long-lasting antinociceptive and anti-inflammatory properties. α-Amyrin can be used for the research of inflammatory.
|
-
- HY-134471
-
|
TNF-α-IN-2
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.
|
-
- HY-19949
-
-
- HY-N7148S
-
-
- HY-N0683S
-
-
- HY-N0683S1
-
-
- HY-N0683S2
-
-
- HY-136748
-
|
HIF-2α-IN-4
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.
|
-
- HY-148264
-
-
- HY-P1270
-
|
α-Conotoxin Im-I
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin Im-I is a selective α7/α9 nAChR antagonist, blocking α7 nicotinic receptors with the highest apparent affinity, while having an 8-fold lower affinity for homomeric α9 nicotinic receptors. α-Conotoxin Im-I is toxic and induces seizures in rodents. α-Conotoxin Im-I is a tool for studying neuronal nAChR.
|
-
- HY-18370
-
-
- HY-P1268
-
|
α-Conotoxin PIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-W014118
-
|
α-Hexylcinnamaldehyde
|
Others
|
Cancer
|
|
α-Hexylcinnamaldehyde, a compound derived from Cinnamaldehyde. α-Hexylcinnamaldehyde has the potential antimutagenic and chemosensitizing properties. α-Hexylcinnamaldehyde is widely used as an ingredient in many personal care, and as an additive in food and the pharmaceutical industry.
|
-
- HY-114771
-
-
- HY-N3002
-
|
α-Arbutin
4-Hydroxyphenyl α-D-glucopyranoside
|
Tyrosinase
|
Metabolic Disease
|
|
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
|
-
- HY-W014049
-
|
N'-Nitro-D-arginine
|
NO Synthase
|
Others
|
|
N'-Nitro-D-arginine, a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8).
|
-
- HY-121618
-
|
α-Thujone
|
GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
|
Cancer
Infection
Neurological Disease
|
|
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
|
-
- HY-144178
-
-
- HY-137178
-
-
- HY-N6968
-
|
α-Humulene
Humulene; α-Caryophyllene
|
NO Synthase
COX
|
Inflammation/Immunology
|
|
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
|
-
- HY-142618
-
-
- HY-P3654
-
|
α-Conotoxin S IA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with high affinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface.
|
-
- HY-B1278S1
-
-
- HY-122485
-
|
α-Copaene
|
Others
|
Others
|
|
α-Copaene, a sesquiterpene hydrocarbon, is a fruit volatile. α-Copaene can be used as an oviposition promoter of Bactrocera oleae.
|
-
- HY-16686
-
|
α-Tocopherol phosphate
Alpha-Tocopherol phosphate; TocP; vitamin E phosphate
|
Others
|
Others
|
|
α-Tocopherol phosphate is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
|
-
- HY-144176
-
-
- HY-Y0191
-
-
- HY-P0252A
-
-
- HY-N0328
-
-
- HY-P1071
-
-
- HY-146981
-
-
- HY-N2854
-
-
- HY-18874
-
-
- HY-150560
-
|
α-Glucosidase-IN-11
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels.
|
-
- HY-P1860
-
-
- HY-P3140
-
|
α-Synuclein (61-75)
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein (61-75) is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD).
|
-
- HY-U00376
-
-
- HY-N0347
-
-
- HY-P1268A
-
|
α-Conotoxin PIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-129434A
-
|
4aα,7α,7aα-Nepetalactone
|
Bacterial
|
Infection
|
|
4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
|
-
- HY-14541S
-
|
Olanzapine-d3
LY170053-d3
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Cancer
Neurological Disease
|
|
Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
|
-
- HY-12697AS
-
|
NGB 2904-d8 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
NGB 2904-d8 hydrochloride is the deuterium labeled NGB 2904 hydrochloride. NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis. NGB 2904 hydrochloride can inhibit Cocaine's rewarding effects and Cocaine-induced reinstatement of drug-seeking behavior.
|
-
- HY-Y0124S
-
|
NSC 16590-d6
α,α-Dimethylglycine-d6; α-Aminoisobutanoic acid-d6
|
Endogenous Metabolite
|
Others
|
|
NSC 16590-d6 (α,α-Dimethylglycine-d6) is the deuterium labeled NSC 16590. NSC 16590 inhibits the production of endogenous ethylene in the cotyledonary segments of cocklebur.
|
-
- HY-118517
-
|
α-Hydroxytamoxifen
(E)-α-Hydroxy tamoxifen; α-OHTAM
|
Others
|
Cancer
|
|
α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
|
-
- HY-147518
-
|
p38-α MAPK-IN-5
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research.
|
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamic acid
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
|
-
- HY-146032
-
-
- HY-14620
-
|
α-Farnesene
|
Others
|
Others
|
|
α-Farnesene is classified as a sesquiterpene, and is a herbivore-induced plant volatile (HIPV). α-Farnesene has an important effect on insect resistance in many plant species.
|
-
- HY-P0252B
-
|
α-MSH free acid
α-Melanocyte-Stimulating Hormone free acid
|
Melanocortin Receptor
|
Neurological Disease
|
|
α-MSH free acid (α-Melanocyte-Stimulating Hormone free acid) is an MC3R and MC4R agonist with EC50s of 0.16 nM and 5.6 nM, respectively. α-MSH free acid activates cAMP generation at MC3R and MC4R.
|
-
- HY-P1269
-
|
α-Conotoxin AuIB
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
|
-
- HY-N10525
-
-
- HY-138097
-
|
α-NETA
|
Aldehyde Dehydrogenase (ALDH)
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
|
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity.
|
-
- HY-B1278S
-
-
- HY-N0728
-
|
α-Linolenic acid
|
PI3K
Akt
|
Cancer
Cardiovascular Disease
|
|
α-Linolenic acid, isolated from Perilla frutescens, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
|
-
- HY-N0492S
-
-
- HY-107935
-
|
6α-Fluoroprednisolone
Fluprednisolone
|
Others
|
Inflammation/Immunology
|
|
6α-Fluoroprednisolone (Fluprednisolone) is an internal standard for methylprednisolone, prednisolone and prednisone. 6α-Fluoroprednisolone is an anti-inflammatory agent. 6α-Fluoroprednisolone can be used for congenital adrenal virilism and Addison's disease research.
|
-
- HY-N7264
-
|
7α-Hydroxycholesterol
|
Others
|
Metabolic Disease
|
|
7α-Hydroxycholesterol is a cholesterol oxide and is formed by both enzymatic and non-enzymatic oxidation. 7α-Hydroxycholesterol can be used as a biomarker for lipid peroxidation.
|
-
- HY-N8531
-
|
4α-Methylcholesterol
|
Others
|
Others
|
|
4α-Methylcholesterol is a Cholesterol derivative. 4α-Methylcholesterol can oxidize 3-hydroxy steroid, with the apparent Km of 12.6 μM.
|
-
- HY-128417S
-
-
- HY-P0297
-
-
- HY-112275
-
-
- HY-107826
-
-
- HY-106029
-
|
4α-TPA
α-TPA
|
Others
|
Cancer
|
|
4α-TPA is an inactive form of TPA, and is used as a negative control for TPA-activated events.
|
-
- HY-P3659
-
-
- HY-115978
-
-
- HY-W089785
-
|
Methyl α-D-galactopyranoside monohydrate
|
Others
|
Others
|
|
Methyl α-D-galactopyranoside monohydrate is an alpha-D-galactoside having a methyl substituent at the anomeric position. Methyl α-D-galactopyranoside inhibits debaryomyces hansenii UFV-1 extracellular and intracellular α-galactosidases with Ki values of 0.82 and 1.12 mM, respectively.
|
-
- HY-142708
-
-
- HY-N6710
-
-
- HY-B0225B
-
-
- HY-B0225A
-
-
- HY-B0225
-
-
- HY-129113
-
|
α-Chaconine
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
|
-
- HY-136735
-
|
IRE1α kinase-IN-1
|
IRE1
|
Cancer
Neurological Disease
|
|
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).
|
-
- HY-147823
-
-
- HY-146984
-
-
- HY-N2843
-
-
- HY-B0757A
-
-
- HY-B1203A
-
-
- HY-130437
-
|
p-nitro-Pifithrin-α
|
MDM-2/p53
TGF-β Receptor
Caspase
|
Infection
Metabolic Disease
|
|
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease.
|
-
- HY-113462
-
|
α-Carotene
|
Others
|
Cancer
|
|
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs. α-Carotene is isolated from yellow-orange and dark-green vegetables.
|
-
- HY-147718
-
-
- HY-151142
-
-
- HY-P1875A
-
-
- HY-113031S
-
-
- HY-P1071A
-
-
- HY-147964
-
-
- HY-151135
-
-
- HY-147965
-
-
- HY-151141
-
-
- HY-P3140A
-
|
α-Synuclein (61-75) (TFA)
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein (61-75) TFA is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD).
|
-
- HY-109564
-
-
- HY-19610
-
-
- HY-P1860A
-
-
- HY-128417S1
-
-
- HY-115433S
-
-
- HY-115433S1
-
-
- HY-P3645
-
|
(Nle4)-α-MSH
|
Melanocortin Receptor
|
Others
|
|
(Nle4)-α-MSH is a synthetic analogue of α-MSH (HY-P0252), a melanocyte-stimulating hormone. (Nle4)-α-MSH reversibly darkens frog skins and also exhibits prolonged activity after heat-alkali treatment.
|
-
- HY-W020182
-
|
α-Terpinene
Terpilene
|
Fungal
Parasite
|
Infection
|
|
α-Terpinene (Terpilene) is a monoterpene found in the essential oils of a large variety of foods and aromatic plants such as Mentha piperita. α-Terpinene is active against Trypanosoma evansi and has the potential for trypanosomosis treatment. α-Terpinene has antioxidant and antifungal properties.
|
-
- HY-151143
-
-
- HY-151145
-
-
- HY-151144
-
-
- HY-N3037
-
-
- HY-146752
-
-
- HY-P99148
-
-
- HY-147644
-
-
- HY-134036
-
-
- HY-N2848
-
-
- HY-W020044S
-
|
DL-alpha-Tocopherol-13C3
|
Ferroptosis
|
Others
|
|
DL-alpha-Tocopherol-13C3 is the 13C-labeled DL-alpha-Tocopherol. DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB.
|
-
- HY-131723
-
|
Pregnenolone 16α-carbonitrile
|
Cytochrome P450
|
Metabolic Disease
|
|
Pregnenolone 16α-carbonitrile is an orally active prototypical and effective rodent-PXR activator. Pregnenolone 16α-carbonitrile, a synthetic steroid, induces cytochrome P450 3A expression. Pregnenolone 16α-carbonitrile exhibits increased resistance to subsequent stressful insults.
|
-
- HY-18509
-
|
IRE1α kinase-IN-2
|
IRE1
|
Cancer
|
|
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines.
|
-
- HY-146156
-
-
- HY-150960
-
-
- HY-N0375
-
-
- HY-P1269A
-
-
- HY-130264
-
|
HIF-2α-IN-2
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
|
-
- HY-101343
-
|
RS 39604
|
5-HT Receptor
|
Neurological Disease
|
|
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites.
|
-
- HY-10349
-
|
WAY-100635
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.
|
-
- HY-N6962
-
|
α-Spinasterol
|
TRP Channel
COX
Bacterial
|
Infection
Neurological Disease
|
|
α-Spinasterol, isolated from Melandrium firmum, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
|
-
- HY-43470
-
-
- HY-150959
-
-
- HY-150961
-
-
- HY-P1267
-
|
α-Conotoxin PnIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-113344S
-
-
- HY-N0728S
-
|
α-Linolenic acid-d5
|
PI3K
Akt
|
Cancer
Cardiovascular Disease
|
|
α-Linolenic acid-d5 is the deuterium labeled α-Linolenic acid. α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
|
-
- HY-N0728S2
-
|
α-Linolenic acid-d14
|
PI3K
Akt
|
Cancer
Cardiovascular Disease
|
|
α-Linolenic acid-d14 is the deuterium labeled α-Linolenic acid. α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
|
-
- HY-147879
-
-
- HY-151138
-
-
- HY-147831
-
|
EIF2α activator 1
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively.
|
-
- HY-128417
-
-
- HY-N0642
-
|
α-L-Rhamnose monohydrate
|
Others
|
Infection
Metabolic Disease
Cancer
|
|
α-L-Rhamnose monohydrate is a component of the plant cell wall pectic polysaccharides rhamnogalacturonan I and rhamnogalacturonan II. α-L-Rhamnose monohydrate is also a component of bacterial polysaccharides where it plays an important role in pathogenicity.
|
-
- HY-Y0739
-
|
(1R)-α-Pinene
|
Bacterial
|
Infection
|
|
(1R)-α-Pinene is a volatile monoterpene with antimicrobial activities. (1R)-α-Pinene reduces Bacillus cereus population growth, and exhibits repellent effects.
|
-
- HY-101332
-
|
EGLU
(2S)-α-Ethylglutamic acid; (2S)-α-EGLU
|
mGluR
|
Neurological Disease
|
|
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent.
|
-
- HY-N10320
-
-
- HY-N1917
-
-
- HY-142659
-
-
- HY-113455S
-
-
- HY-W014941
-
-
- HY-129389
-
|
Benzyl-α-GalNAc
|
Others
|
Cancer
|
|
Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-FU (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation.
|
-
- HY-121222
-
|
alpha-Bisabolol
|
Apoptosis
|
Cancer
|
|
alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
|
-
- HY-126304A
-
-
- HY-N8653
-
-
- HY-12836
-
-
- HY-N6825
-
-
- HY-13249
-
|
1alpha-Hydroxy VD4
1α-Hydroxy vitamin D4
|
VD/VDR
|
Cancer
|
|
1alpha-Hydroxy VD4 , a 1alpha(OH)D derivative, can effectively induce the differentiation of monoblastic leukaemia U937, P39/TSU and P31/FUJ cells.
|
-
- HY-B0141A
-
-
- HY-147954
-
|
α-Glycosidase-IN-1
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Metabolic Disease
Neurological Disease
|
|
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
|
-
- HY-115433
-
-
- HY-B1513
-
-
- HY-N5142
-
|
α-Terpineol
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria.
α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption.
|
-
- HY-113344
-
-
- HY-B1278
-
-
- HY-P9908
-
-
- HY-149008
-
|
α-Amylase-IN-3
|
Amylases
|
Cancer
Metabolic Disease
|
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease.
|
-
- HY-P0203
-
|
α-CGRP, rat
|
CGRP Receptor
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
α-CGRP, rat, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
|
-
- HY-N8164
-
-
- HY-10564S
-
|
Sarpogrelate-d3 hydrochloride
MCI-9042-d3
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Sarpogrelate-d3 hydrochloride (MCI-9042-d3) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
|
-
- HY-110203
-
|
R-7050
TNF-α Antagonist III
|
TNF Receptor
|
Cancer
|
|
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
-
- HY-13331
-
|
Clascoterone
Cortexolone 17 Alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-N7136
-
|
α-Terpinyl acetate
|
Cytochrome P450
|
Metabolic Disease
|
|
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
|
-
- HY-125777A
-
|
α-Conotoxin Vc1.1 TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.
|
-
- HY-15793
-
-
- HY-100542
-
-
- HY-113209
-
|
8-Isoprostaglandin F2α
|
Endogenous Metabolite
|
Others
|
|
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
|
-
- HY-B0742
-
|
Hydroxyprogesterone caproate
17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate
|
Others
|
Others
|
|
Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17α-hydroxyprogesterone formed from caproic acid.
|
-
- HY-18733
-
-
- HY-144696
-
|
Dyrk1A/α-synuclein-IN-2
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect.
|
-
- HY-N0728S3
-
|
α-Linolenic acid-13C18
|
PI3K
Akt
|
Cancer
Cardiovascular Disease
|
|
α-Linolenic acid-13C18 is the 13C labeled α-Linolenic acid. α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
|
-
- HY-147832
-
|
EIF2α activator 2
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively.
|
-
- HY-N5123
-
|
α-L-Rhamnose
|
Others
|
Others
|
|
α-L-Rhamnose is a terminal residue of steviol glycosides Dulcoside A and Dulcoside B. α-L-Rhamnose recognizing lectin site of human dermal fibroblasts functions as a signal transducer: modulation of Ca 2+ fluxes and gene expression.
|
-
- HY-145678
-
-
- HY-N2666
-
|
5α-Hydroxycostic acid
|
VEGFR
|
Cancer
|
|
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways.
|
-
- HY-12836A
-
|
IFN alpha-IFNAR-IN-1 hydrochloride
|
IFNAR
|
Inflammation/Immunology
|
|
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. IFN alpha-IFNAR-IN-1 hydrochloride inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) (IC50=2-8 μM).
|
-
- HY-123349
-
|
5α-Hydroxy-6-keto cholesterol
|
Drug Metabolite
|
Cardiovascular Disease
|
|
5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM.
|
-
- HY-P1267A
-
|
α-Conotoxin PnIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-148318
-
|
CK2α-IN-1
|
Casein Kinase
|
Cancer
|
|
CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies.
|
-
- HY-N0548
-
|
α-Angelica lactone
|
Gutathione S-transferase
|
Cancer
|
|
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes.
|
-
- HY-150692
-
|
Estrogen receptor α antagonist 1
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer.
|
-
- HY-147668
-
-
- HY-147666
-
-
- HY-147669
-
-
- HY-147667
-
-
- HY-146305
-
-
- HY-114423
-
-
- HY-N1605
-
|
17α-Neriifolin
|
Others
|
Others
|
|
17α-Neriifolin is a compound isolated from a methylene chloride extract of the seeds of Cerbera odollam.
|
-
- HY-N1026
-
-
- HY-N1027
-
-
- HY-145542
-
-
- HY-147777
-
-
- HY-W127530
-
|
α-Tocopherol phosphate disodium
Alpha-Tocopherol phosphate disodium; TocP disodium; Vitamin E phosphate disodium
|
Apoptosis
Reactive Oxygen Species
|
Cardiovascular Disease
|
|
α-Tocopherol phosphate (alpha-Tocopherol phosphate) disodium, a promising antioxidant, can protect against long-wave UVA1 induced cell death and scavenge UVA1 induced ROS in a skin cell model. α-Tocopherol phosphate disodium possesses therapeutic potential in the inhibition of apoptosis and increases the migratory capacity of endothelial progenitor cells under high-glucose/hypoxic conditions and promotes angiogenesis.
|
-
- HY-147778
-
-
- HY-B0979
-
|
Lobeline hydrochloride
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
|
-
- HY-N9048
-
-
- HY-N2992
-
-
- HY-100999
-
-
- HY-141336
-
-
- HY-P3766
-
|
Protein kinase C (alpha) peptide TFA
|
PKC
|
Others
|
|
Protein kinase C α peptide (TFA) is a peptide of PKC-α. PKC-α acts as a lipid-dependent ser/thr protein kinase, can modulate various cellular processes, including cell survival, proliferation, differentiation, migration, adhesion and so on.
|
-
- HY-N6854A
-
-
- HY-125348
-
|
6α-Hydroxy paclitaxel
|
Others
|
Cancer
|
|
6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer.
|
-
- HY-128463
-
-
- HY-113038B
-
|
α-Hydroxyglutaric acid
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
|
-
- HY-N1606
-
-
- HY-N2842
-
-
- HY-131553
-
|
D-α-Tocopherol Succinate
Vitamin E succinate
|
Apoptosis
|
Cancer
|
|
D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer.
|
-
- HY-126683
-
-
- HY-151203
-
|
PKG1α activator 3
|
Others
|
Cardiovascular Disease
|
|
PKG1α activator 3 is a PKG1α activator (EC50 basal/partial=13/0.52 μM). PKG1α activator 3 shows anti-proliferative effects to smooth muscle cell, and can be used in cardiovascular disease research.
|
-
- HY-10003A
-
-
- HY-32350
-
-
- HY-125617
-
-
- HY-113209S1
-
|
8-iso Prostaglandin F2α-d9
|
Endogenous Metabolite
|
Others
|
|
8-iso Prostaglandin F2α-d9 is the deuterium labeled 8-Isoprostaglandin F2α. 8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
|
-
- HY-113246
-
-
- HY-P0203A
-
|
α-CGRP, rat TFA
|
CGRP Receptor
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
α-CGRP, rat TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
|
-
- HY-118608
-
-
- HY-D1710
-
-
- HY-33549
-
|
α-Methyl-p-tyrosine
|
Others
|
Cancer
|
|
α-Methyl-p-tyrosine is a competitive inhibitor of the enzyme tyrosine hydroxylase, which converts tyrosine to Levodopa (DOPA). α-Methyl-p-tyrosine is an orally active inhibitor of catecholamine synthesis which inhibits the hydroxylation of tyrosine to DOPA.
|
-
- HY-112535
-
-
- HY-B0648S
-
|
Medroxyprogesterone-d3
17α-Hydroxy-6α-methylprogesterone-d3; U8840-d3
|
Progesterone Receptor
|
Endocrinology
|
|
Medroxyprogesterone-d3 (17α-Hydroxy-6α-methylprogesterone-d3) is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
|
-
- HY-N1030
-
-
- HY-125833
-
|
Alpha-Naphthoflavone
|
Aromatase
|
Cancer
|
|
Alpha-Naphthoflavone is a flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
|
-
- HY-151490
-
-
- HY-151491
-
-
- HY-N7785
-
-
- HY-N6913
-
|
3α-Hydroxymogrol
|
AMPK
|
Metabolic Disease
|
|
3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation.
|
-
- HY-N10128
-
-
- HY-N3802
-
|
Eleutheroside C
Ethyl α-D-galactoside; Ethyl α-D-galactopyranoside
|
Others
|
Others
|
|
Eleutheroside C (Ethyl α-D-galactoside) is a glycoside isolated from the bulbs of Polianthes tuberosa.
|
-
- HY-144695
-
|
Dyrk1A/α-synuclein-IN-1
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect.
|
-
- HY-123519
-
-
- HY-151492
-
|
PI3KC2α-IN-3
|
PI3K
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
PI3KC2α-IN-3 is a potent and highly selective PI3KC2α inhibitor (IC50: 126 nM). PI3KC2α-IN-3 interacts with the ATP-binding site of PI3KC2α. PI3KC2α-IN-3 impairs endocytic membrane dynamics and membrane remodeling. PI3KC2α-IN-3 can be used in the research of thrombosis, diabetes and cancers.
|
-
- HY-15484
-
-
- HY-107819S
-
|
5α-Cholestan-3β-ol-d5
Dihydrocholesterol-d5; 5α-Cholestanol-d5; NSC 18188-d5
|
Endogenous Metabolite
|
|
|
5α-Cholestan-3β-ol-d5 is the deuterium labeled 5α-Cholestan-3β-ol. 5α-Cholestan-3β-ol is a derivitized steroid compound.
|
-
- HY-107819
-
-
- HY-N8971
-
|
Bauer-7-ene-3β,16α-diol
16α-Hydroxybauerenol
|
Bacterial
|
Infection
|
|
Bauer-7-ene-3β,16α-diol, a triterpenoid, is a natural product that can be isolated from dried flower buds of Tussilago farfara L. or Petasites tricholobus (Compositae). Bauer-7-ene-3β,16α-diol shows medium antibacterial activity against E. coli.
|
-
- HY-B1278A
-
-
- HY-N7389B
-
|
GDP-α-D-mannose disodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM).
|
-
- HY-136347
-
-
- HY-135190
-
-
- HY-N7087
-
|
Tulipalin A
α-Methylene butyrolactone
|
Drug Metabolite
|
|
|
Tulipalin A (α-Methylene butyrolactone) is a glycoside. Tulipalin A is a causative allergen that induces Allergic contact dermatitides. Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells.
|
-
- HY-144509S
-
-
- HY-113038
-
|
D-α-Hydroxyglutaric acid
(R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
|
-
- HY-P1758
-
-
- HY-N6602
-
|
α-Solanine
|
Apoptosis
|
Cancer
|
|
α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in Solanum nigrum, has been observed to inhibit growth and induce apoptosis in cancer cells.
|
-
- HY-19776
-
-
- HY-128428
-
|
Carboprost
15(S)-15-Methyl Prostaglandin F2α; 15-Methyl-PGF2α
|
Prostaglandin Receptor
|
Endocrinology
|
|
Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a metabolically stable synthetic analog of prostaglandin F2α. Carboprost stimulates uterine contractions and induces abortion. Carboprost is used for postpartum hemorrhage due to uterine atony and for the termination of pregnancy in the second trimester.
|
-
- HY-12710A
-
-
- HY-104004
-
-
- HY-P1294
-
-
- HY-B1658A
-
|
Frovatriptan succinate hydrate
(R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.
|
-
- HY-B1658B
-
|
Frovatriptan succinate
(R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinate
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
|
-
- HY-W086896
-
-
- HY-N0549
-
-
- HY-W039897
-
-
- HY-100838
-
|
cis-α-(Carboxycyclopropyl)glycine
L-CCG III
|
EAAT2
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes.
|
-
- HY-N2990
-
-
- HY-P1314
-
-
- HY-P2519
-
-
- HY-128747A
-
-
- HY-128747
-
-
- HY-121481
-
|
Cucurbitadienol
10α-Cucurbitadienol
|
Others
|
Inflammation/Immunology
|
|
Cucurbitadienol (10α-Cucurbitadienol) is a natural product that can be found in the seeds of Trichosanthes kirilowii. Cucurbitadienol exhibits anti-inflammatory effect.
|
-
- HY-B0522A
-
|
Ampicillin sodium
D-(-)-α-Aminobenzylpenicillin sodium salt
|
Bacterial
Antibiotic
|
Infection
|
|
Ampicillin sodium (D-(-)-α-Aminobenzylpenicillin sodium salt) is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
|
-
- HY-N10091
-
|
2,3-Dihydro-3α-methoxynimbolide
|
Apoptosis
|
Others
|
|
2,3-Dihydro-3α-methoxynimbolide is a limonoid compound isolated from the extracts of bark, leaves, roots, and seeds of Azadirachta indica A. Juss. var. siamensis Valeton. 2,3-Dihydro-3α-methoxynimbolide exhibits potent cyto-toxicities against one or more cell lines. 2,3-Dihydro-3α-methoxynimbolide activates caspases-3, -8, and -9, while increases the ratio of Bax/Bcl-2. 2,3-Dihydro-3α-methoxynimbolide induces apoptosis via both mitochondrial and death receptor pathways in AZ521.
|
-
- HY-N10601
-
|
11-Oxo-α-amyrin
Neoilexonol
|
Others
|
Others
|
|
11-Oxo-α-amyrin (Neoilexonol) is a triterpenoid that can be isolated from Leonurus japonicus (Lamiaceae).
|
-
- HY-N4215
-
|
11(α)-Methoxysaikosaponin F
|
Others
|
Inflammation/Immunology
|
|
11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitory activity.
|
-
- HY-N0181A
-
-
- HY-148325
-
|
α7 Nicotinic receptor agonist-1
|
nAChR
|
Neurological Disease
|
|
α7 Nicotinic receptor agonist-1 (Preparation 5) is an α7 nAChR agonist. α7 Nicotinic receptor agonist-1 can be used in studies of psychiatric disorders (such as schizophrenia, manic or hypomanic depression and anxiety disorders) and intellectual disorders (such as alzheimer's disease, learning deficits, cognitive deficits, attention deficits, memory loss, lewy body dementia and attention deficit hyperactivity disorder).
|
-
- HY-131335
-
|
p38α inhibitor 2
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
|
-
- HY-139671
-
-
- HY-117580S
-
-
- HY-P9911A
-
-
- HY-B0225AS
-
|
Methyldopa-d3 hydrochloride
L-(-)-α-Methyldopa-d3 hydrochloride; MK-351-d3 hydrochloride
|
Adrenergic Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa-d3 (hydrochloride) is deuterium labeled Methyldopa (hydrochloride). Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-10002A
-
|
(1S)-Calcitriol
1α,25-Dihydroxy-3-epi-vitamin-D3
|
VD/VDR
|
Others
|
|
(1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3) is a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3). (1S)-Calcitriol exhibits potent vitamin D receptor (VDR)-mediated actions such as inhibition of keratinocyte growth or suppression of parathyroid hormone secretion.
|
-
- HY-P2519A
-
-
- HY-P1314A
-
-
- HY-14648S3
-
|
Dexamethasone-4,6α,21,21-d4
|
Glucocorticoid Receptor
SARS-CoV
Autophagy
Complement System
Mitophagy
Bacterial
Antibiotic
|
|
|
Dexamethasone-4,6α,21,21-d4 is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
|
-
- HY-B0141AS1
-
-
- HY-138688
-
-
- HY-N1014
-
-
- 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-B1203S
-
-
- HY-116291
-
-
- HY-B0141AS
-
-
- HY-12956
-
-
- HY-151664
-
-
- HY-146082
-
|
(Z)-α-Cyanostilbene
|
Others
|
Cancer
|
|
(Z)-α-Cyanostilbene (compound 8), a dicyano substituted acrylonitrile, shows selective antiproliferative activity against HeLa and HepG2 cells, with IC50s of 0.33 and 0.52 μM, respectively.
|
-
- HY-129459
-
-
- HY-15156
-
-
- HY-15327S
-
-
- HY-P1294A
-
-
- HY-N1640
-
|
1-O-Deacetyl-2α-hydroxykhayanolide E
|
Others
|
Others
|
|
1-O-Deacetyl-2α-hydroxykhayanolide E is a natural product that can be isolated from Swietenia mahagoni. 1-O-Deacetyl-2α-hydroxykhayanolide E is widely distributed in the leaves and branches of Swietenia mahagoni.
|
-
- HY-113381
-
-
- HY-W010248
-
-
- HY-113259
-
|
7α-Hydroxy-4-cholesten-3-one
|
Endogenous Metabolite
|
Metabolic Disease
|
|
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1.
|
-
- HY-19974
-
|
TAK-220
|
CCR
HIV
|
Infection
Endocrinology
|
|
TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
|
-
- HY-146083
-
|
(Z)-p-cyano-α-Cyanostilbene
|
Others
|
Cancer
|
|
(Z)-p-cyano-α-Cyanostilbene (compound 11), a phenantrene derivative, has antiproliferative activity. (Z)-p-cyano-α-Cyanostilbene shows significant selectivity against HeLa (IC50=0.21 µM) and HepG2 (IC50=0.230 µM) cells without cytotoxic against normal skin fibroblasts (IC50>100 µM).
|
-
- HY-151816
-
-
- HY-N2042
-
-
- HY-19269
-
|
FK706
|
Elastase
|
Inflammation/Immunology
|
|
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.
|
-
- HY-125648
-
|
Euphorbadienol
Alpha-Euphorbol
|
Parasite
|
Infection
|
|
Euphorbadienol (alpha-Euphorbol), a triterpenic compound, isolated from the latex of Euphorbia resinifera. The derivatives of Euphorbadienol can be used as elicitors of disease resistance, and has antileishmanial and antitrypanosomal activity.
|
-
- HY-147063
-
|
N-Acetyl-α-D-glucosamine 1-phosphate disodium
|
Endogenous Metabolite
|
Others
|
|
N-acetyl-α-d-glucosamine 1-phosphate disodium (GlcNAc-1-P), an anomeric sugar phosphate, is a key intermediate in the biosynthesis of N-linked glycoproteins. N-acetyl-α-d-glucosamine 1-phosphate disodium is a metabolic precursor of the bacterial cell-wall components teichoic acid and mureine.
|
-
- HY-113259S
-
|
7α-Hydroxy-4-cholesten-3-one-d7
|
Endogenous Metabolite
|
Metabolic Disease
|
|
7α-Hydroxy-4-cholesten-3-one-d7 is the deuterium labeled 7α-Hydroxy-4-cholesten-3-one. 7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1.
|
-
- 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-139702
-
|
α5β1 integrin agonist-1
|
Integrin
|
Cancer
|
|
α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
|
-
- HY-N0629
-
-
- HY-N5068
-
-
- HY-N2048
-
|
2,2':5',2''-Terthiophene
α-Terthiophene; α-Terthienyl; Trithiophene
|
Bacterial
Antibiotic
|
Infection
|
|
2,2':5',2''-Terthiophene (α-Terthiophene) is an oligomer of the heterocycle thiophene. 2,2':5',2''-Terthiophene has been employed as building block for the organic semi-conductor polythiophene.
|
-
- HY-N9345
-
-
- HY-128942
-
-
- HY-141126
-
-
- HY-B1658BS
-
|
Frovatriptan-d3 succinate
(R)-Frovatriptan-d3 succinate; SB 209509-d3 succinate; VML 251-d3 succinate
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
|
-
- HY-W012722
-
-
- HY-108652
-
-
- HY-134440
-
-
- HY-117580
-
-
- HY-B0522B
-
|
Ampicillin trihydrate
D-(-)-α-Aminobenzylpenicillin trihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Ampicillin trihydrate (D-(-)-α-Aminobenzylpenicillin trihydrate) is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
|
-
- HY-12956A
-
|
Dinoprost tromethamine salt
Prostaglandin F2α tromethamine salt; PGF2α THAM; Prostaglandin F2α THAM
|
Prostaglandin Receptor
Endogenous Metabolite
Autophagy
Apoptosis
|
Endocrinology
|
|
Dinoprost tromethamine salt (Prostaglandin F2α tromethamine salt) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost tromethamine salt is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost tromethamine salt plays a key role in the onset and progression of labour.
|
-
- HY-N0181AS
-
|
Lumisterol-d3
9β,10α-Ergosterol-d3
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol-d3 (9β,10α-Ergosterol-d3) is the deuterium labeled Lumisterol. Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-N0181AS1
-
|
Lumisterol-d5
9β,10α-Ergosterol-d5
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol-d5 (9β,10α-Ergosterol-d5) is the deuterium labeled Lumisterol. Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-B0216
-
-
- HY-113019S
-
-
- HY-134452
-
|
MeAIB
α-(Methylamino)isobutyric acid
|
Others
|
Others
|
|
MeAIB (α-(Methylamino)isobutyric acid) is a specific substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na +-dependent manner.
|
-
- HY-14618
-
|
Zingiberene
α-Zingiberene; (-)-Zingiberene
|
Autophagy
|
Cancer
|
|
Zingiberene (α-Zingiberene) is a monocyclic sesquiterpene which is the predominant constituent of ginger with oil content (Zingiber officinale). Neuroprotective potential. Zingiberene triggers autophagy. Anticancer activity.
|
-
- HY-U00141
-
|
ABTL-0812
α-Hydroxylinoleic acid
|
Autophagy
|
Metabolic Disease
|
|
ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity.
|
-
- HY-128420
-
|
Lobeline sulfate
α-Lobeline sulfate; L-Lobeline sulfate
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
|
-
- HY-W010248S
-
-
- HY-N5143
-
-
- HY-112716
-
-
- HY-145717
-
-
- HY-N2994
-
-
- HY-B0891S
-
|
17α-Hydroxyprogesterone-d8
17-Hydroxyprogesterone-d8; 17-OHP-d8
|
Progesterone Receptor
Endogenous Metabolite
|
Others
|
|
17α-Hydroxyprogesterone-d8 (17-Hydroxyprogesterone-d8) is the deuterium labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
|
-
- HY-N1203
-
-
- HY-15327
-
-
- HY-B0891
-
-
- HY-133887
-
-
- HY-N2989
-
-
- HY-N6821
-
-
- HY-P1536
-
-
- HY-112174
-
-
- HY-133538
-
-
- HY-100206
-
|
5α-Androstane-3β,5,6β-triol
|
AMPK
|
Neurological Disease
|
|
5α-Androstane-3β,5,6β-triol is a neuroprotectant. 5α-Androstane-3β,5,6β-triol can remarkably reverse intracellular acidification and alleviate neuronal injury through the inhibition of AMPK signaling. 5α-Androstane-3β,5,6β-triol remarkably reduced the infarct volume and attenuated neurologic impairment in acute ischemic stroke models of middle cerebral artery occlusion in vivo.
|
-
- HY-N1718
-
-
- HY-N6084
-
|
Humulone
α-Lupulic acid
|
COX
GABA Receptor
Apoptosis
|
Cardiovascular Disease
|
|
Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
|
-
- HY-139654
-
|
α/β-Hydrolase-IN-1
|
Others
|
Infection
|
|
α/β-Hydrolase-IN-1 exhibits the best-in-class MICs of 50 μM (25 μg/mL) and 16 μM (8.4 μg/mL) against M. smegmatis and M. tuberculosis H37Ra, respectively.
|
-
- HY-B1065
-
-
- HY-140960
-
-
- HY-114362
-
-
- HY-N0179
-
|
Ecdysone
α-Ecdysone
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
|
|
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
|
-
- HY-100371
-
|
(RS)-MCPG
Alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
|
-
- HY-146066
-
|
α7 nAchR-JAK2-STAT3 agonist 1
|
nAChR
JAK
STAT
NO Synthase
|
Inflammation/Immunology
|
|
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis.
|
-
- HY-P2558
-
-
- HY-W013636
-
|
2-Ketoglutaric acid
Alpha-Ketoglutaric acid
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
|
-
- HY-N4310
-
-
- HY-17571A
-
|
Oxytocin acetate
α-Hypophamine acetate; Oxytocic hormone acetate
|
Oxytocin Receptor
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
Oxytocin (α-Hypophamine) acetate is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin acetate can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
|
-
- HY-N6911
-
-
- HY-W013636A
-
|
2-Ketoglutaric acid Sodium
Alpha-Ketoglutaric acid Sodium
|
Tyrosinase
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM).
|
-
- HY-B0216S1
-
-
- HY-B0216S
-
-
- HY-B0172A
-
-
- HY-N8800
-
-
- HY-12316
-
|
20(S)-Hydroxycholesterol
20α-Hydroxycholesterol
|
Smo
Endogenous Metabolite
|
Cancer
|
|
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
|
-
- HY-N5113
-
|
6α-Chloro-5β-hydroxywithaferin A
|
Others
|
Others
|
|
6α-Chloro-5β-hydroxywithaferin A is a withanolide that can be isolated from W. somnifera. W. somnifera has antioxidant, anti-inflammatory, immunomodulatory, anticarcinogenic, antibacterial antiparkinsonism and antistress properties.
|
-
- HY-B0891S1
-
|
17α-Hydroxyprogesterone-13C3
17-Hydroxyprogesterone-13C3; 17-OHP-13C3
|
Progesterone Receptor
Endogenous Metabolite
|
Others
|
|
17α-Hydroxyprogesterone-13C3 (17-Hydroxyprogesterone-13C3) is the 13C-labeled 17α-Hydroxyprogesterone. 17α-Hydroxyprogesterone (17-Hydroxyprogesterone) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
|
-
- HY-N6967
-
|
Levomenol
(-)-α-Bisabolol
|
Apoptosis
|
Inflammation/Immunology
Neurological Disease
|
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active.
|
-
- HY-N0173
-
|
Cinchonidine
α-Quinidine
|
Serotonin Transporter
Parasite
|
Infection
|
|
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
|
-
- HY-N3808
-
-
- HY-N5128
-
-
- HY-32350S
-
-
- HY-N9453
-
-
- HY-N9368
-
-
- HY-13102
-
|
UK-383367
|
Procollagen C Proteinase
|
Others
|
|
UK-383367 (UK 383367) is a potent and selective inhibitor of BMP-1 (procollagen C-proteinase) with IC50 of 44 nM; Selective for BMP-1 over MMPs 1, 2, 3, 9 and 14 (IC50 values are >10,000 nM for listed MMPs).
|
-
- HY-103641
-
-
- HY-103641A
-
-
- HY-N1601
-
-
- HY-141137
-
-
- HY-N1608
-
-
- HY-115738
-
-
- HY-151863
-
|
alpha-GalNAc-TEG-N3
|
Others
|
Others
|
|
alpha-GalNAc-TEG-N3 is a click chemistry reagent. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity.
|
-
- HY-N2466
-
|
Melanotan I
MT-I; [Nle4,D-Phe7]-α-MSH
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for sunlight-induced skin cancers research.
|
-
- HY-N2466A
-
|
Melanotan I acetate
MT-I acetate; [Nle4,D-Phe7]-α-MSH acetate
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research.
|
-
- HY-P9911
-
|
Vedolizumab
Anti-Human lymphocyte α4β7 integrin, Humanized Antibody
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
Vedolizumab is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
|
-
- HY-P3662
-
|
Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2
|
Tyrosinase
|
Cancer
|
|
Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 is a melanotropin, a melanocyte-stimulating hormone. Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 stimulates tyrosinase and exhibits thermoregulatory effect in rats model.
|
-
- HY-B1142
-
|
Lipoamide
(±)-α-Lipoamide; DL-Lipoamide; DL-6,8-Thioctamide
|
Others
|
Others
|
|
Lipoamide ((±)-α-Lipoamide) is a monocarboxylic acid amide resulting from the formal condensation of the carboxy group of lipoic acid with ammonia. Lipoamide as a coenzyme to transfer acetyl group and hydrogen in the process of pyruvate deacylation.
|
-
- HY-N9398
-
|
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol
|
Sirtuin
|
Cancer
|
|
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol, a SIRT1 activator, exhibits significant stimulation of SIRT1 activity. Anti-tumor activity.
|
-
- HY-N9529
-
-
- HY-W018512
-
-
- HY-N2174
-
-
- HY-135312
-
|
AZ'6421
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
|
-
- HY-N7433
-
-
- HY-N4241
-
-
- HY-N1035
-
|
Urs-12-ene-3β,16β,22α-triol
|
Others
|
Others
|
|
Urs-12-ene-3β,16β,22α-triol is a terpenoid compound isolated from the ethanol extract of fresh aerial parts of the Patagonian shrub Nardophyllum bryoides.
|
-
- HY-N10410
-
-
- HY-P1309
-
-
- HY-114457
-
|
Phosphatidylinositol 4,5-bisphosphate
L-Alpha-Phosphatidylinositol-4,5-bisphosphate
|
PI3K
|
Others
|
|
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate), a phospholipid component of cell membranes, is a substrate for phospholipase C (PLC) and phosphoinositide 3-kinase (PI3K) and as a primary messenger.
|
-
- HY-N9304
-
|
Fern-7-en-19α-ol
19a-Hydroxyferna-7,9(11)-diene
|
Others
|
Others
|
|
Fern-7-en-19α-ol (9a-Hydroxyferna-7,9(11)-diene) is a triterpenoid compound isolated from Adiantum caudatum.
|
-
- HY-B0172S
-
-
- HY-N5051
-
-
- HY-W018512S
-
|
7-Ketolithocholic acid-d5
3α-Hydroxy-7-oxo-5β-cholanic acid-d5
|
Endogenous Metabolite
|
Metabolic Disease
|
|
7-Ketolithocholic acid-d5 (3α-Hydroxy-7-oxo-5β-cholanic acid-d5) is the deuterium labeled 7-Ketolithocholic acid. 7-Ketolithocholic acid (3α-Hydroxy-7-oxo-5β-cholanic acid), a bile acid, can be absorbed and suppresses endogenous bile acid production and biliary cholesterol secretion.
|
-
- HY-B0216S2
-
-
- HY-148194
-
|
SC239
|
ADC Linker
|
Cancer
|
|
SC239 is a cleavable 2-aminophenyl hemiasterlin drug-linker. SC239 can be as the drug-linker for ADC.
|
-
- HY-139201A
-
|
Poly-D-lysine hydrobromide (MW 70000-150000)
|
Others
|
Cancer
|
|
Poly-D-lysine hydrobromide (MW 70000-150000) is a synthetic polymeric substrate and is one of the most widely used substrate in neural cell culture. Poly-D-lysine hydrobromide (MW 70000-150000) removes proteinase K-resistant PrP from prion-infected SN56 neuroblastoma cells without affecting PrP C.
|
-
- HY-139201
-
|
Poly-D-lysine hydrobromide (MW 30000-70000)
|
Others
|
Cancer
|
|
Poly-D-lysine hydrobromide (MW 30000-70000) is a synthetic polymeric substrate and is one of the most widely used substrate in neural cell culture. Poly-D-lysine hydrobromide (MW 30000-70000) removes proteinase K-resistant PrP from prion-infected SN56 neuroblastoma cells without affecting PrP C.
|
-
- HY-P2518
-
-
- HY-B0172AS
-
-
- HY-P2518A
-
-
- HY-P1309A
-
-
- HY-15652
-
|
Freselestat
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
|
-
- HY-16772
-
|
EPI-743
α-Tocotrienol quinone; PTC-743; Vatiquinone; NCT04378075
|
Mitochondrial Metabolism
Ferroptosis
|
Neurological Disease
|
|
EPI-743 (Vatiquinone; α-Tocotrienol quinone; PTC-743; NCT04378075) is a potent cellular oxidative stress protectant, inhibits ferroptosis in cells, which could be used for the study for mitochondrial diseases. EPI-743 is a synthetic analog of vitamin E with oral activity, targets repletion of reduced intracellular glutathione.
|
-
- HY-N5129
-
-
- HY-N8163
-
-
- HY-135794
-
|
11-Ketodihydrotestosterone
11-KDHT; 5α-Dihydro-11-keto testosterone
|
Androgen Receptor
|
Endocrinology
|
|
11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
|
-
- HY-P3728
-
-
- HY-15652A
-
|
Freselestat quarterhydrate
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
|
-
- HY-N4162
-
-
- HY-N8100
-
-
- HY-B0717
-
|
Tocofersolan
TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS
|
Others
|
Metabolic Disease
Neurological Disease
|
|
Tocofersolan is synthetic polyethylene glycol derivative of α-tocopherol. Tocofersolan is an orally active and water-soluble analog of vitamin E. Tocofersolan can reduce neurobehavioral deficits in zebrafish embryos exposed to moderate and high concentrations of BaP during early development. Tocofersolan shows antioxidant activity. Tocofersolan can be used to provide an orally bioavailable source of vitamin E.
|
-
- HY-12956S
-
|
Dinoprost-d4
Prostaglandin F2a-d4; PGF2α-d4
|
Prostaglandin Receptor
Endogenous Metabolite
Autophagy
Apoptosis
|
Endocrinology
|
|
Dinoprost-d4 (Prostaglandin F2a-d4) is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.
|
-
- HY-12956S1
-
|
Dinoprost-d9
Prostaglandin F2a-d9; PGF2α-d9
|
Prostaglandin Receptor
Endogenous Metabolite
Autophagy
Apoptosis
|
Endocrinology
|
|
Dinoprost-d9 (Prostaglandin F2a-d9) is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.
|
-
- HY-N8093
-
-
- HY-Y0124
-
|
NSC 16590
α,α-Dimethylglycine; α-Aminoisobutanoic acid
|
Endogenous Metabolite
|
Others
|
|
NSC 16590 inhibits the production of endogenous ethylene in the cotyledonary segments of cocklebur.
|
-
- HY-N9522
-
-
- HY-112023
-
|
Lumisterol 3 (>90%)
9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity C
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.
|
-
- HY-B1203
-
-
- HY-N1132
-
-
- HY-N0417
-
|
Cucurbitacin E
α-Elaterin; α-Elaterine
|
CDK
Autophagy
|
Cancer
|
|
Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
|
-
- HY-B0648
-
-
- HY-135794S
-
|
11-Ketodihydrotestosterone-d3
11-KDHT-d3; 5α-Dihydro-11-keto testosterone-d3
|
Androgen Receptor
|
Endocrinology
|
|
11-Ketodihydrotestosterone-d3 (11-KDHT-d3) is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
|
-
- HY-103066
-
|
Br-PBTC
|
nAChR
|
Neurological Disease
|
|
Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit.
|
-
- HY-111547
-
|
M1001
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
M1001 is a weak hypoxia-inducible factor-2α (HIF-2α) agonist. M1001 can bind to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 can be used in chronic kidney disease research.
|
-
- HY-147174
-
-
- HY-B1696
-
|
Methyldopate
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate is an ethyl ester prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate has the potential for severe hypertension research [1].
|
-
- HY-N1132A
-
-
- HY-U00425
-
-
- HY-B1696A
-
|
Methyldopate hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research.
|
-
- HY-128838A
-
|
(rel)-PROTAC ERRα Degrader-1
|
Estrogen Receptor/ERR
|
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-138542
-
-
- HY-146268
-
|
CaMKIIα-IN-1
|
CaMK
|
Neurological Disease
|
|
CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability.
|
-
- HY-101640
-
-
- HY-N10626
-
-
- HY-100300
-
-
- HY-111478
-
-
- HY-N0127
-
-
- HY-14929A
-
|
Migalastat hydrochloride
GR181413A
|
Others
|
Others
|
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-N1650
-
|
Pygenic acid B
2α,3α,24-Trihydroxyurs-12-en-28-oic acid
|
Fungal
|
Infection
|
|
Pygenic acid B is a triterpenoid that can be isolated from the leaves of Glochidion obliquum. Pygenic acid B shows antifungal activity against C. musae. Pygenic acid B shows ONOO- scavenging activity.
|
-
- HY-17552
-
|
sn-Glycero-3-phosphocholine
Choline Alfoscerate; Alpha-GPC; L-α-GPC
|
Cholinesterase (ChE)
Endogenous Metabolite
|
Neurological Disease
|
|
sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia.
|
-
- HY-U00244
-
-
- HY-101610
-
-
- HY-N1974
-
-
- HY-N1049
-
|
Zeorin
α-Zeorin
|
Others
|
Others
|
|
Zeorin is a compound isolated from the lichen Parmotrema sancti-angelii.
|
-
- HY-B0522
-
-
- HY-B1761
-
|
Santonin
Alpha-Santonin
|
Parasite
|
Infection
|
|
Santonin is an active principle of the plant Artemisia cina, which is formely used to treat worms.
|
-
- HY-112098
-
|
PROTAC ERα Degrader-1
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
|
-
- HY-15438
-
|
SB 415286
|
GSK-3
Apoptosis
|
Metabolic Disease
|
|
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
|
-
- HY-111846
-
|
PROTAC ERα Degrader-2
|
SNIPERs
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-2 comprises a IAP 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-U00117
-
-
- HY-108697
-
|
PT2399
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
|
-
- HY-128839
-
-
- HY-139185
-
|
PROTAC ERRα Degrader-3
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα Degrader-3 is a potent and selective ERRα degrader based on von Hippel-Lindau ligand. PROTAC ERRα Degrader-3 is capable of specifically degrading ERRα protein by >80% at a concentration of 30 nM. PROTAC ERRα Degrader-3 is inactive against ERRβ and ERRγ proteins.
|
-
- HY-N10306
-
-
- HY-146733
-
-
- HY-138937
-
|
NDB
|
FXR
|
Metabolic Disease
|
|
NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.
|
-
- HY-128838
-
-
- HY-110121
-
|
NS3861 fumarate
|
nAChR
|
Neurological Disease
|
|
NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
|
-
- HY-12152
-
|
PNU-120596
NSC 216666
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.
|
-
- HY-144699
-
|
ERRα antagonist-2
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.
|
-
- HY-110121A
-
|
NS3861
|
nAChR
|
Neurological Disease
|
|
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
|
-
- HY-P99153
-
|
Farletuzumab
MORAb-003
|
Antibiotic
|
Cancer
|
|
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a therapeutic humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer.
|
-
- HY-143239
-
|
PPARα/γ agonist 1
|
PPAR
|
Metabolic Disease
|
|
PPARα/γ agonist 1 is a potent and dual PPARα/γ partial agonist with EC50 values of 28 nM and 69 nM for PPARα and PPARγ, respectively. PPARα/γ agonist 1 is a promising prototype for dyslipidemia and diabetes research.
|
-
- HY-100689
-
|
Propyl pyrazole triol
PPT
|
Estrogen Receptor/ERR
|
Cancer
|
|
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
|
-
- HY-B1203S1
-
|
Fludrocortisone-d2
9α-Fludrocortisone-d2; 9α-Fluorcortisol-d2
|
Mineralocorticoid Receptor
|
|
|
Fludrocortisone-d2 is the deuterium labeled Fludrocortisone. Fludrocortisone, a synthetic mineralocorticoid with anti-inflammatory activity.
|
-
- HY-111507
-
|
PDGFRα kinase inhibitor 1
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-143227
-
-
- HY-B1058A
-
-
- HY-B1058
-
-
- HY-14929
-
|
Migalastat
GR181413A free base
|
Others
|
Others
|
|
Migalastat (GR181413A free base) is an orally active and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-144733
-
-
- HY-107666
-
-
- HY-125840
-
|
Belzutifan
PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC).
|
-
- HY-U00244S
-
-
- HY-130499
-
|
ERRα Ligand-Linker Conjugates 1
|
Target Protein Ligand-Linker Conjugates
|
Cancer
|
|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
|
-
- HY-15770
-
|
TR-14035
|
Integrin
|
Inflammation/Immunology
|
|
TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.
|
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- HY-129674
-
-
- HY-N6964
-
-
- HY-107673
-
-
- HY-W019838
-
-
- HY-107395
-
-
- HY-N1132S2
-
|
D-(+)-Trehalose-d4
D-Trehalose-d4; α,α-Trehalose-d4
|
Endogenous Metabolite
|
Others
|
|
D-(+)-Trehalose-d4 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi.
|
-
- HY-N1132S1
-
|
D-(+)-Trehalose-d2
D-Trehalose-d2; α,α-Trehalose-d2
|
Endogenous Metabolite
|
Others
|
|
D-(+)-Trehalose-d2 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi.
|
-
- HY-N1132S
-
|
D-(+)-Trehalose-d14
D-Trehalose-d14; α,α-Trehalose-d14
|
Endogenous Metabolite
|
Others
|
|
D-(+)-Trehalose-d14 is the deuterium labeled D-(+)-Trehalose. D-(+)-Trehalose, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipi.
|
-
- 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-U00326
-
|
PI3Kα/mTOR-IN-1
|
PI3K
mTOR
|
Cancer
|
|
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
|
-
- HY-108469
-
|
BI-6015
|
Others
|
Cancer
Metabolic Disease
|
|
BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.
|
-
- HY-N0328S
-
|
Mangostin-d3
|
Reactive Oxygen Species
Apoptosis
Bacterial
Fungal
Virus Protease
|
Cancer
|
|
alpha-Mangostin-d3 (α-Mangostin-d3) is the deuterium labeled alpha-Mangostin. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
|
-
- HY-144111
-
|
PPARα/δ agonist 1
|
PPAR
|
Inflammation/Immunology
|
|
PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis.
|
-
- HY-145071
-
|
PROTAC ERα Y537S degrader-1
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Y537S degrader-1 comprises a ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Y537S degrader-1 extracts from patent WO2021143822, example 12. PROTAC ERα Y537S degrader-1 is an estrogen receptor-alpha (ERα) Y537S degrader.
|
-
- HY-N2071
-
|
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities.
|
-
- HY-30216
-
-
- HY-B0566
-
-
- HY-107381
-
-
- HY-N2332A
-
-
- HY-U00459
-
|
GSK2850163
|
IRE1
|
Cancer
|
|
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-P1397
-
|
RVD-Hpα
|
Cannabinoid Receptor
|
Neurological Disease
|
|
RVD-Hpα, an α-hemoglobin-derived peptide containing three additional amino acids, is a CB1 cannabinoid receptor agonist. RVD-Hpα is a positive allosteric modulator of cannabinoid receptor 2.
|
-
- HY-U00459B
-
|
GSK2850163 hydrochloride
|
IRE1
|
Cancer
|
|
GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- 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-146267
-
|
ERα degrader 5
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo.
|
-
- HY-N2059
-
|
Santalol
|
Others
|
Cancer
|
|
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
|
-
- HY-147699
-
|
FRα-IN-1
|
Antifolate
|
Cancer
|
|
FRα-IN-1 (Compound 4) is a tumor-targeting agent. FRα-IN-1 shows selective anticancer activity towards folate receptors (FRα and FRβ) expression cells.
|
-
- HY-134334
-
-
- HY-146424
-
-
- HY-144306
-
|
ERα degrader 4
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the treatment of breast cancer.
|
-
- 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-117147A
-
|
GSK2945 hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-111845
-
-
- HY-117147
-
|
GSK2945
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-124290
-
|
Carotegrast methyl
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of Carotegrast methyl, is a specific and dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
|
-
- HY-B0648S1
-
-
- HY-145940
-
|
BAY-204
BRD3727
|
Others
|
Cancer
|
|
BAY-204 is an inhibitor of Casein kinase 1 alpha and delta (CSNK1α and δ) useful for the treatment of proliferative disorders.
|
-
- HY-14652
-
-
- HY-U00014
-
|
AVE-8134
|
PPAR
|
Metabolic Disease
|
|
AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.
|
-
- HY-12867
-
-
- HY-14413
-
|
SR3335
ML 176
|
ROR
|
Metabolic Disease
|
|
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
|
-
- HY-P99219
-
|
Sifalimumab
MEDI-545; MDX 1103
|
IFNAR
|
Inflammation/Immunology
|
|
Sifalimumab (MEDI-545) is an anti-IFNα monoclonal antibody. Sifalimumab suppresses the abnormal immune activity by binding to multiple interferon-alpha (IFNα) subtypes. Sifalimumab can be used in systemic lupus erythematosus (SLE) research.
|
-
- HY-103212
-
|
Azepexole dihydrochloride
B-HT 933 dihydrochloride; Oxazoloazepin dihydrochloride
|
Adrenergic Receptor
|
Endocrinology
Cardiovascular Disease
|
|
Azepexole (B-HT 933) dihydrochloride is a potent and selective alpha 2-adrenoceptor agonist with pKis of 8.3, 7.6, and 7.5 for α2A-, α2B- and α2C-adrenoceptor subtypes, resepctively. Azepexole dihydrochloride causes concentration-dependent inhibition of peristaltic contractions (IC50= 78.72 nM).
|
-
- HY-146020
-
|
Topoisomerase IIα-IN-1
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines.
|
-
- HY-131404
-
|
TPBM
|
Estrogen Receptor/ERR
|
Cancer
|
|
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth.
|
-
- HY-136207
-
|
TC-2559 difumarate
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-129619
-
|
SNIPER(ER)-87
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
|
-
- HY-B0659
-
-
- HY-N10628
-
-
- HY-B0942
-
-
- HY-131345
-
|
PI3Kα-IN-4
|
PI3K
|
Cancer
|
|
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.
|
-
- HY-147767
-
|
PI3Kα-IN-6
|
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis.
|
-
- HY-149000
-
|
PI3Kα-IN-7
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis.
|
-
- HY-132179
-
-
- HY-111376
-
-
- HY-100735
-
-
- HY-50855B
-
-
- 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-B1203AS
-
-
- HY-146021
-
|
Topoisomerase IIα-IN-2
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase.
|
-
- HY-N7076
-
|
Aleuritic acid
(±)-erythro-Aleuritic acid; α-Aleuritic acid
|
Others
|
Others
|
|
Aleuritic acid ((±)-erythro-Aleuritic acid) is a major ingredient in Croton crassifolius Geisel. and used in the perfumery industry.
|
-
- HY-107915
-
|
Levonordefrin
(-)-Cobefrin; (-)-α-Methylnoradrenaline; (-)-Nordefrin
|
Adrenergic Receptor
|
Others
|
|
Levonordefrin, a common alternative to levoepinephrine as a vasoconstrictor in dental local anesthetic preparations, is usually used in fivefold higher concentrations. Levonordefrin is generally considered equivalent to epinephrine.
|
-
- HY-N0334
-
|
(+)-Magnoflorine
Magnoflorine; α-Magnoflorine; Thalictrine
|
Fungal
|
Infection
Metabolic Disease
|
|
(+)-Magnoflorine (Magnoflorine), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. (+)-Magnoflorine has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-N0535
-
|
(+)-Magnoflorine chloride
Magnoflorine chloride; α-Magnoflorine chloride; Thalictrine chloride
|
Fungal
|
Infection
Metabolic Disease
|
|
Magnoflorine chloride (Magnoflorine chloride), an aporphine alkaloid found in Magnolia or Aristolochia, reduces the formation of C. albicans biofilm. Magnoflorine chloride has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-32348
-
-
- HY-N4328
-
-
- HY-N2166
-
|
Tomatine
α-Tomatine; Lycopersicin; Tomatin
|
Proteasome
Apoptosis
|
Neurological Disease
|
|
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity.
|
-
- HY-N2143
-
-
- 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-P9970
-
-
- HY-147801
-
-
- HY-15831
-
-
- HY-14126
-
-
- HY-16995
-
-
- HY-P0082A
-
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Glucagon (1-29), bovine, human, porcine hydrochloride
Porcine glucagon hydrochloride
|
GCGR
|
Metabolic Disease
|
|
Glucagon (1-29), bovine, human, porcine hydrochloride is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis. Glucagon (1-29), bovine, human, porcine hydrochloride activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-75385
-
-
- HY-P0082
-
|
Glucagon (1-29), bovine, human, porcine
Porcine glucagon
|
GCGR
|
Metabolic Disease
|
|
Glucagon (1-29), bovine, human, porcine is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon (1-29), bovine, human, porcine activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-16988A
-
-
- HY-B0659A
-
