Search Result
Results for "
effective orally
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
22
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-135825
-
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Autophagy
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Neurological Disease
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TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment .
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- HY-112094S
-
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Ser/Thr Protease
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Cardiovascular Disease
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WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
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-
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- HY-109127A
-
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BCX7353 dihydrochloride
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Kallikrein
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Others
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Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
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- HY-145685
-
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DNA/RNA Synthesis
Others
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Cancer
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RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer .
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- HY-160019
-
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Deubiquitinase
Mitophagy
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Neurological Disease
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MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
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- HY-109127R
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Ser/Thr Protease
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Others
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Berotralstat (Standard) is the analytical standard of Berotralstat. This product is intended for research and analytical applications. Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE .
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- HY-118911
-
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ATM/ATR
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Cancer
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ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC50: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors .
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- HY-157585S
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-
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- HY-137849
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PARP
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Cancer
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RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model .
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- HY-B1045
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-
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- HY-109127
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BCX7353
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Kallikrein
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Cancer
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Berotralstat (BCX7353) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema .
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- HY-116713
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-
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- HY-119057
-
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Parasite
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Infection
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DSM74 (compound 21) is an orally active and potent antimalarial inhibitor of PfDHODH (IC50=0.28 μM) and PbDHODH (IC50=0.38 μM). DSM74 inhibits the growth of Plasmodium in animals .
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- HY-U00207
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-
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- HY-U00363
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-
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- HY-10116
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PI3K
mTOR
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Cancer
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PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM) .
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- HY-70073
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-
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- HY-15009
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-
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- HY-19467
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-
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- HY-107456
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-
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- HY-144875
-
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CDK
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Cancer
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CTX-712 is an orally effective CLK 2 inhibitor, with an IC50 of 1.4 nM, showing anti-tumor activity .
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- HY-105583
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Others
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Others
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Cloforex (Frenapyl) is an orally effective amphetamine-type anorexic and a precursor to Clophentermine. Cloforex can be used to induce foam cell accumulation in rats .
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- HY-B0291
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Parasite
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Infection
Cancer
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Oxfendazole is a sulfoxide form of fenbendazole that is effective when taken orally. Oxfendazole fights parasites and has tumor-promoting activity .
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- HY-B1436
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STAT
Bacterial
Antibiotic
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Infection
Cancer
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Nifuroxazide is an effective inhibitor of STAT3, also exerts potent anti-tumor and anti-metastasis activity. Nifuroxazide is an orally active nitrofuran antibiotic.
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- HY-B1895
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-
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- HY-100419
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VEGFR
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Cancer
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BFH772 is a potent oral VEGFR2 inhibitor, which is highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM .
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- HY-U00168
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- HY-N11630
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Influenza Virus
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Others
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Pinellic acid is a natural product that could be isolated from a medicinal plant Pinelliae tuber. Pinellic acid is an effective oral adjuvant for nasal influenza vaccine .
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- HY-112712
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Cyclophilin
HCV
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Infection
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Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a .
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- HY-W353258
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BAY 12-8039 monohydrate
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Bacterial
Antibiotic
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Infection
Cancer
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Moxifloxacin (BAY 12-8039) hydrochloride monohydrate is an orally active bacterial inhibitor that is effective against Streptococcus pneumoniae. Moxifloxacin hydrochloride monohydrate can be used in tuberculosis research .
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- HY-14155
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MMP
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Inflammation/Immunology
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MMP145 (compound 27) is a potent, selective and orally active MMP-12 inhibitor. MMP145 is effective in inflammation and asthma reasearch .
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- HY-157250
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Apoptosis
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Endocrinology
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BHD is an effective, orally active and reversible contraceptive agent. BHD induces the apoptosis of spermatogenic cells rapidly and disruptes the blood-testis barrier effectively .
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- HY-117281
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- HY-148026
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BGB 11417
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Bcl-2 Family
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Cancer
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Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines .
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- HY-120864
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Wnt
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Cancer
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SEN461 is a potent and orally active Wnt pathway inhibitor. SEN461 shows effective anti-tumor activity and can be used for GBM research .
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- HY-12870
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Estrogen Receptor/ERR
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Cancer
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AZD9496 is an effective, selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM. AZD9496 is an orally active, selective estrogen receptor degrader (SERD).
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- HY-139626
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Histone Methyltransferase
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Cancer
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EPZ-719 is a selective, orally effective SETD2 inhibitor with an IC50 value of 0.005 μM. EPZ-719 has anticancer activity .
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- HY-121565
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Others
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Metabolic Disease
Endocrinology
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SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice .
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- HY-130750
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Reactive Oxygen Species
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Neurological Disease
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Phycocyanobilin, an orally active antioxidative agent, is an effective scavenger for various reactive oxygen species. Phycocyanobilin can be used for the research of Alzheimer’s disease .
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- HY-129826
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mAChR
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Others
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J-104129 is a selective and orally active muscarinic M3 receptor antagonist (Ki = 4.2 nM). J-104129 is effective in promoting bronchodilation .
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- HY-19429A
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- HY-N2486
-
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects .
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- HY-14316A
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Ebanicline dihydrochloride; ABT-594 dihydrochloride
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nAChR
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Neurological Disease
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Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
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- HY-119198
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Apoptosis
Histone Methyltransferase
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Cancer
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NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers .
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- HY-B0378A
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RS-10085
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Angiotensin-converting Enzyme (ACE)
Apoptosis
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Cardiovascular Disease
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Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects - .
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- HY-B1691
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Hexamine hippurate
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Bacterial
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Cancer
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Methenamine hippurate (Hexamine hippurate) is an orally active urinary antiseptic agent with a wide antibacterial spectrum. Methenamine hippurate is effective against most common urinary tract pathogens .
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- HY-142618
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- HY-14316B
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Ebanicline hydrochloride; ABT-594 hydrochloride
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nAChR
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Neurological Disease
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Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
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- HY-19909A
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EGFR
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Cancer
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NRC-2694-A is an orally effective EGFR tyrosine kinase inhibitor. NRC-2694-A can be used in the study of malignant squamous cell carcinoma (HNSCC) .
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- HY-105126
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TR4698
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Others
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Others
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Rioprostil (TR4698) is an orally effective analogue of prostaglandin E1, possessing potent antisecretory and anti-gastric lesion properties. Rioprostil can be utilized in mucosal protection research .
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- HY-156117
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STING
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Cancer
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LB244 is a homologue of BB-Cl-amidine, which is an orally effective STING inhibitor (EC50=0.8 μM) and can be used to inhibit STING-dependent inflammatory diseases. The pharmacokinetic properties of LB244 indicate limited oral activity in mice .
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- HY-124185
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Others
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Others
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LC 6 is an anti-allergic compound that has the activity of inhibiting passive cutaneous allergic reactions in rats. Its half effective dose (ED50) is 35 mg/kg body weight. Oral administration is effective and long-lasting, and the effect is obviously dose-dependent. Its long-term binding to mast cells makes it a valuable tool for studying allergic reaction receptors.
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- HY-119480
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Bacterial
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Infection
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Megazol is an orally active antibacterial agent. Megazol has effective inhibitory against T. b. brueei with an EC50 of 0.01 μg/mL. Megazol can be used for the research of protozoan infections .
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- HY-17412S
-
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Isotope-Labeled Compounds
Antibiotic
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Others
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Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
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- HY-137922
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Others
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Metabolic Disease
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SHS4121705 is an orally effective mitochondrial uncoupling agent with an IC50 of 4.3 μM in L6 myoblasts. SHS4121705 can be used in the study of non-alcoholic steatohepatitis (NASH) .
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- HY-139798
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Bacterial
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Infection
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Iboxamycin is a potent antibiotic candidate bearing a fused bicyclic amino acid residue. Iboxamycin is orally bioavailable, safe and effective in researching both Gram-positive and Gram-negative bacterial infections in mice .
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- HY-A0151
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RP 7843; SKF 5883; Thioperazine
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Dopamine Receptor
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Neurological Disease
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Thioproperazine (RP 7843) is an orally active antipsychotic agent with calming, antiemetic activity. Thioproperazine is effective in promoting the release of dopamine in rat striatum. Thioproperazine can be used in studies of schizophrenia and bipolar disorder .
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- HY-A0093
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KOE-1173 hydrochloride
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Sodium Channel
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Cardiovascular Disease
Neurological Disease
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Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
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- HY-119521
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KOE-1173
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Sodium Channel
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Cardiovascular Disease
Neurological Disease
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Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
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- HY-14305A
-
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p38 MAPK
Autophagy
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Inflammation/Immunology
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BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease .
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- HY-120160
-
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CP-86325
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PPAR
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Neurological Disease
Metabolic Disease
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Darglitazone (CP-86325), a thiazolidinedione, is a potent, selective, and orally active PPAR-γ agonist. Darglitazone is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
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- HY-128571
-
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FLT3
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Cancer
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FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia .
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- HY-116228
-
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Caderofloxacin; CS-940
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Bacterial
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Infection
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Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases .
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- HY-A0124
-
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(6R)-BH4; (6R)-Tetrahydro-L-biopterin
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Endogenous Metabolite
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Metabolic Disease
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Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin can be used in study of phenylketonuria (PKU) .
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- HY-W011309
-
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1-O-HDG; HXDG
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PPAR
PGE synthase
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Inflammation/Immunology
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1-O-Hexadecylglycerol can up-regulate PPAR-γ expression, inhibit pGE2, and exhibit anti-inflammatory properties . 1-O-Hexadecylglycerol is effective in oral administration .
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- HY-118770
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- HY-B1916
-
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Spiramycin B; Spiramycin II; Foromacidin B
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Antibiotic
Bacterial
Parasite
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Infection
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Acetylspiramycin (Spiramycin B) is an effective oral macrolide antibiotic produced by Streptomyces, It can inhibit the splenic lymphocyte transformation induced by phytohemagglutinin (PHA), LPS (HY-D1056) and antigen, reduce the procoagulant activity of macrophages, have good antibacterial effect on gram-positive bacteria, and is also an effective antigenic insect agent, which can be used to fight parasitic infection .
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- HY-105110
-
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SM-8668
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Fungal
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Infection
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SM-8668 is an effective orally active antifungal agent, with median effective doses (ED50) of 0.18, 3.7, and 5.9 mg/kg for systemic candidiasis, aspergillosis, and cryptococcosis in mice, respectively. Pharmacokinetic studies in mice and rats indicate that SM-8668 has a long half-life and a high total exposure. SM-8668 can be used in anti-infective research .
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- HY-120160A
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CP 86325 Sodium
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PPAR
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Neurological Disease
Metabolic Disease
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Darglitazone Sodium, a thiazolidinedione, is an orally active, potent, and selective PPAR-γ (peroxisome proliferator-activated receptor) agonist. Darglitazone Sodium is effective in controlling blood glucose and lipid metabolism, and can be used for type II diabetes research .
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- HY-B1895R
-
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Histamine Receptor
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Neurological Disease
Inflammation/Immunology
Endocrinology
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Levodropropizine (Standard) is the analytical standard of Levodropropizine. This product is intended for research and analytical applications. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent .
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- HY-142221
-
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PD-1/PD-L1
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Cancer
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ARB-272572 is an oral effective small molecule PD-L1 inhibitor, with an IC50 value of 400 pM. ARB-272572 has research significance in tumors and chronic viral infections .
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- HY-119816
-
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Others
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Cardiovascular Disease
|
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Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension [1] [2].
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- HY-101234
-
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Histamine Receptor
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Inflammation/Immunology
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ICI 162846 is an orally active antagonist of H2 receptor. ICI 162846 inhibits acid production accompanied by an increase in the secretion of histamine in chronic duodenal ulcer (CDU) models. ICI 162846 is effective in preventing CDU .
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- HY-119018
-
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Others
|
Inflammation/Immunology
|
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AHR-6293 is an orally effective and potent anti-inflammatory agent. AHR-6293 has a better anti-inflammatory effect than AHR-5850, but does not have the activity of inhibiting platelet aggregation .
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- HY-162920
-
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Aminopeptidase
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Cardiovascular Disease
|
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QGC583 is an effective selective Aminopeptidase A (APA) inhibitor with oral activity and blood-brain barrier permeability, boasting an IC50 value of 4 nM. QGC583 can inhibit APA activity in the brain, kidneys, and heart of rats .
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- HY-150306
-
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HSV
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Infection
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IM-250 is an orally active helicase-primase inhibitor. IM-250 is effective against HSV infection. IM-250 inhibits HSV-1 infection in Vero cells (IC50: ~20 nM) .
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- HY-158363
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- HY-10053
-
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Neurokinin Receptor
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Neurological Disease
Endocrinology
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Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting .
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- HY-B0657
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Clodronate
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Others
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Others
Cancer
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Clodronic acid is an orally active bisphosphonate, which is used for researching osteoporosis and diseases associated with excessive bone resorption. Clodronic acid inhibits bone resorption through induction of osteoclast apoptosis. Clodronic acid is effective in the maintenance or improvement of bone mineral density .
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- HY-162937
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Microtubule/Tubulin
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Cancer
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KIF18A-IN-13 (Compound 16) is an effective and orally active inhibitor of KIF18A with anticancer activity in vivo. KIF18A-IN-13 can be utilized for research in ovarian cancer .
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- HY-N2486R
-
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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Desoxyrhaponticin (Standard) is the analytical standard of Desoxyrhaponticin. This product is intended for research and analytical applications. Desoxyrhaponticin is a kind of oral drug that inhibits effective fatty acid synthesis (FASN), and has a fatal effect on cancer cells. Desoxyrhaponticin has the ability to inhibit glucose uptake, improve oral glucose tolerance as a diabetic agent, and possess anti-diabetic effects .
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- HY-101946
-
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Leukotriene Receptor
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Inflammation/Immunology
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AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
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- HY-19910
-
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SCYX-7158; AN5568
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Parasite
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Infection
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Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL .
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- HY-B1651
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Ferrous fumarate
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Others
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Metabolic Disease
Cancer
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Iron (II) fumarate is an orally effective active dietary supplement. Iron (II) fumarate can alleviate metabolic damage and damage to silkworms caused by cypermethrin (HY-123178). Iron (II) fumarate can be used for research on iron deficiency anemia .
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- HY-119486
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PF-06649751; CVL-751
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Dopamine Receptor
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Neurological Disease
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Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease .
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- HY-B0954A
-
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mAChR
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Endocrinology
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Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
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- HY-163374
-
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CDK
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Cancer
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Cdc7-IN-20 (EP-05) is an orally effective and selective Cdc7 inhibitor with IC50 and Ki values of 0.93 and 0.11 nM, respectively. Cdc7-IN-20 has antitumor activity .
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-
- HY-117281S1
-
-
- HY-163994
-
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KWD 2058 hydrochloride
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Others
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Others
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|
Ibuterol (KWD 2058) hydrochloride, a diester of Terbutaline (HY-B0802A), is an orally active, selective and effective β-stimulating agent with lipophilic activities. Ibuterol hydrochloride is also an orally active ocular hypotensive agent. Ibuterol hydrochloride relieves bronchial obstruction in asthma without causing circulatory effects. Ibuterol hydrochloride is proming for rasearch of intraocular hypertension, asthma and bronchitis .
|
-
- HY-A0124A
-
|
(6R)-BH4 dihydrochloride; (6R)-Tetrahydro-L-biopterin dihydrochloride
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin also drives autoimmunity. Sapropterin can be used in study of phenylketonuria (PKU) .
|
-
- HY-16723
-
-
- HY-B0615A
-
|
EN 313; Ethmozin; Moracizine
|
Others
|
Cardiovascular Disease
|
|
Moricizine Hydrochloride (EN 313) is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period .
|
-
- HY-155250
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis .
|
-
- HY-W370556
-
|
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 is a racemate of LM11A-31. LM11A-31 is a non-peptide modulator of p75NTR (neurotrophin receptor p75) and is an orally effective proNGF antagonist .
|
-
- HY-129716
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
L-693989 is an orally active water-soluble lipopeptide with anticandidal and antipneumocystis activity. L-693989 is effective in preventing the development of both P. carinii cysts and trophozoites. L-693989 is promising for research of P. carinii pneumonia .
|
-
- HY-A0093R
-
|
KOE-1173 hydrochloride (Standard)
|
Sodium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Mexiletine (hydrochloride) (Standard) is the analytical standard of Mexiletine (hydrochloride). This product is intended for research and analytical applications. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
|
-
- HY-16110
-
|
UFT; BMS-200604
|
Others
|
Cancer
|
|
Tegafur-Uracil (UFT; BMS-200604) is an effective oral chemotherapy drug based on fluoropyrimidine. Tegafur-Uracil inhibits thymidylate synthase. Tegafur-Uracil can be used in combination with leucovorin (LV) and polysaccharide K (PSK) for research on solid tumors .
|
-
- HY-119832
-
|
EGIS-2062 free acid; EGYT-2062 free acid
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Setastine (EGIS-2062 (free acid); EGYT-2062 (free acid) is an orally effective, non-sedative and long acting anti-allergic agent. Setastine possesses potent histamine Hi-receptor blocking properties and can be used for allergies and rhinitis research [1]<.
|
-
- HY-17595
-
|
|
Parasite
Apoptosis
Microtubule/Tubulin
|
Infection
Cancer
|
|
Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
|
-
- HY-14789
-
-
- HY-14369
-
-
- HY-19447A
-
|
LB80380 maleate
|
HBV
|
Infection
|
|
Besifovir Dipivoxil maleate (LB80380 maleate) is an oral proagent of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies [2]
|
-
- HY-B0976
-
|
Th-1165; Phenoterol
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol (Th-1165), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-13571AS1
-
|
|
Isotope-Labeled Compounds
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
|
-
- HY-13571AS
-
|
|
Isotope-Labeled Compounds
Glucocorticoid Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
|
-
- HY-116387A
-
|
BRL 6231
|
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
WR99210 hydrochloride is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 hydrochloride shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains as well as T. gondii .
|
-
- HY-B0378AR
-
|
|
Angiotensin-converting Enzyme (ACE)
Apoptosis
|
Cardiovascular Disease
|
|
Moexipril (hydrochloride) (Standard) is the analytical standard of Moexipril (hydrochloride). This product is intended for research and analytical applications. Moexipril hydrochloride (RS-10085) is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila (hydrochloride). Moexipril hydrochloride exhibits antihypertensive and neuroprotective effects - .
|
-
- HY-161952
-
|
|
SHP2
|
Cancer
|
|
JAB-3312 is an orally effective anticancer phosphatase SHP2 inhibitor (IC50: 1.9 nM) with anti-cancer activity. JAB-3312 has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model .
|
-
- HY-14716
-
|
|
DNA/RNA Synthesis
Raf
|
Cancer
|
|
CCT239065 is an orally available, effective inhibitor of the mutant protein kinase V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation .
|
-
- HY-16784
-
|
IDX719; IDX18719
|
HCV
HCV Protease
|
Infection
|
|
Samatasvir (IDX71) is a potent, orally active NS5A inhibitor of HCV replication. Samatasvir is effective and selective against infectious HCV and replicons, with EC50s falling within a tight range of 2 to 24 pM in genotype 1 through 5 replicons .
|
-
- HY-148788
-
|
GBT-601; GBT-021601
|
Others
|
Others
|
|
Osivelotor is an orally effective small molecule. Osivelotor is an allosteric regulator of deoxyhemoglobin S (HbS). Osivelotor increases the affinity of HbS to oxygen, inhibits HbS polymerization, and thus prevents erythrocyte sickling in the blood. Osivelotor can be used for research of sickle cell disease (SCD) .
|
-
- HY-100886
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .
|
-
- HY-16723A
-
|
(R)-TV 45070; (R)-XEN402
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
(R)-Funapide ((R)-TV 45070) is the less active R-enantiomer of Funapide. Funapide is a potent inhibitor of the sodium channel Nav1.7, Nav1.8 and other Nav channels expressed in the peripheral nervous system. Fornabil is an orally effective analgesic agent .
|
-
- HY-107064
-
|
CGP 9000; Oraspor
|
Bacterial
Antibiotic
|
Infection
|
|
Cefroxadine (CGP 9000) is an orally active cephalosporin antibiotic. Cefroxadine is more effective than cephalexin against Escherichia coli and Klebsiella pneumoniae with MIC values of 3.13 and 1.56 μg/mL respectively with a concentration of 10 6 μg/mL. Cefroxadine can be used for the research of infection .
|
-
- HY-B1691R
-
|
|
Bacterial
|
Cancer
|
|
Methenamine (hippurate) (Standard) is the analytical standard of Methenamine (hippurate). This product is intended for research and analytical applications. Methenamine hippurate (Hexamine hippurate) is an orally active urinary antiseptic agent with a wide antibacterial spectrum. Methenamine hippurate is effective against most common urinary tract pathogens .
|
-
- HY-111338
-
Tacrine
5 Publications Verification
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .
|
-
- HY-13676
-
|
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
|
-
- HY-112299
-
|
TAS6417; CLN-081
|
EGFR
Apoptosis
|
Cancer
|
|
Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
|
-
- HY-B0976A
-
|
Th-1165a; Phenoterol hydrobromide
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-147268
-
|
RAF/KIN_2787
|
Raf
p38 MAPK
|
Cancer
|
|
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
|
-
- HY-147017
-
|
GSK286
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and agent-sensitive (DS) M. tuberculosis.
|
-
- HY-161522
-
|
|
Glucosidase
Carbonic Anhydrase
|
Endocrinology
|
|
α-Glucosidase-IN-63 (Compound 4d) is an inhibitor of α-Glucosidase (IC50=0.44 μM). α-Glucosidase-IN-63 inhibits hCA II with an activity of Ki= 7.0 nM. α-Glucosidase-IN-63 is orally effective. .
|
-
- HY-B1327
-
|
7-Chlorotetracycline hydrochloride
|
Bacterial
Antibiotic
Parasite
|
Infection
Inflammation/Immunology
|
|
Chlortetracycline hydrochloride (7-Chlorotetracycline hydrochloride) is an orally active, effective and selectively methanogenic bacteria inhibitor with bactericidal effects. Chlortetracycline hydrochloride is also a antibiotic that acts by inhibiting bacterial protein synthesis. Additionally, Chlortetracycline hydrochloride is a specific and potent calcium ionophore antibiotic, inhibiting binding of aminoacyl-tRNA to ribosomes .
|
-
- HY-B1327A
-
|
7-Chlorotetracycline
|
Bacterial
Antibiotic
Parasite
|
Infection
Inflammation/Immunology
|
|
Chlortetracycline (7-Chlorotetracycline) is an orally active, effective and selectively methanogenic bacteria inhibitor with bactericidal effects. Chlortetracycline is also a antibiotic that acts by inhibiting bacterial protein synthesis. Additionally, Chlortetracycline is a specific and potent calcium ionophore antibiotic, inhibiting binding of aminoacyl-tRNA to ribosomes .
|
-
- HY-159648
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
PF-07328948 is an orally effective BDK (branch chain ketoacid dehydrogenase kinase) inhibitor. PF-07328948 acts as a BCKDH (branch chain ketoacid dehydrogenase) enzyme complex degrader to enhance BCAA (branch chain amino acid) catabolism and has potential inhibitory effects on heart failure .
|
-
- HY-100500
-
|
KBT 1585 hydrochloride
|
Penicillin-binding protein (PBP)
Bacterial
|
Infection
Cancer
|
|
Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active proagent of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection .
|
-
- HY-137958A
-
|
AT-511
|
HCV
SARS-CoV
|
Infection
|
|
Bemnifosbuvir (AT-511) is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir has pangenotypic antiviral activity .
|
-
- HY-145581
-
|
AZD4831
|
Glutathione Peroxidase
|
Cardiovascular Disease
|
|
Mitiperstat (AZD4831) is an effective oral inhibitor of myeloperoxidase (MPO). Mitiperstat can reduce inflammation and improve microvascular function, and it can be used in studies related to heart failure, preserved or mildly reduced ejection fraction, non-alcoholic fatty liver disease, and chronic obstructive pulmonary disease .
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-19490A
-
|
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia .
|
-
- HY-119816R
-
|
|
Others
|
Cardiovascular Disease
|
|
Piretanide (Standard) is the analytical standard of Piretanide. This product is intended for research and analytical applications. Piretanide is an oral active, relatively safe and effective diuretic. Piretanide has the potential for the research of congestive heart failure with a potential advantage of having potassium-sparing properties. Piretanide can also be used for the research of hypertension .
|
-
- HY-107129
-
|
|
GCGR
|
Metabolic Disease
|
|
MK-3577 is an orally effective glucagon receptor (GCGR) antagonist that reduces hepatic glucose production and lowers blood glucose levels by blocking glucagon receptors on target organs, primarily the liver. Pharmacokinetic analysis in domestic cats indicates that MK-3577 reaches peak levels 3 to 4 hours after oral administration, with a half-life of approximately 15 hours. MK-3577 can be used in diabetes research .
|
-
- HY-10780
-
|
|
Others
|
Cardiovascular Disease
|
|
JTV-803 mesylate is a human factor Xa inhibitor with oral anticoagulant activity. JTV-803 exhibits competitive inhibition of human factor Xa, with a Ki value of 0.019μM and IC50Value is 0.081μM. JTV-803 is 100 times more selective at inhibiting human factor Xa than its comparator. JTV-803 is an effective oral anticoagulant for the prevention of thrombosis .
|
-
- HY-133017
-
|
SAR439859
|
Estrogen Receptor/ERR
|
Cancer
|
|
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER + breast cancer.
|
-
- HY-131723
-
|
|
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-159688
-
|
|
Bacterial
|
Infection
|
|
Cefditoren is an orally active antibiotic with broad-spectrum antibacterial activity, capable of inhibiting both Gram-negative and Gram-positive bacteria. It has a MIC50 of 0.25-0.5 mg/L against Streptococcus pneumoniae strains. Cefditoren is effective against respiratory tract infections and skin infections .
|
-
- HY-A0124AR
-
|
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Sapropterin (dihydrochloride) (Standard) is the analytical standard of Sapropterin (dihydrochloride). This product is intended for research and analytical applications. Sapropterin ((6R)-BH4) is an orally active phenylalanine hydroxylase (PAH) cofactor, which is effective in reducing blood phenylalanine concentrations. Sapropterin also drives autoimmunity. Sapropterin can be used in study of phenylketonuria (PKU) .
|
-
- HY-14756
-
|
|
Thrombopoietin Receptor
|
Others
|
|
Totrombopag is an orally effective thrombopoietin receptor (TpoR) agonist. By activating TpoR, Totrombopag initiates an intracellular signaling cascade mediated by JAK2 kinase and the transcription factor Stat5, a signaling process that is the primary mechanism regulating megakaryocyte growth and differentiation into platelets. Totrombopag can be used to study platelet production and megakaryocyte biology .
|
-
- HY-105634A
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
|
-
- HY-W094474
-
|
hydrate/monohydrateortrihydrate
|
GSK-3
Apoptosis
|
Infection
Neurological Disease
|
|
Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease .
|
-
- HY-17412S1
-
|
|
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
|
-
- HY-117842
-
|
|
Others
|
Inflammation/Immunology
|
|
KY 234 is an orally effective inhibitor that targets thromboxane A2 production, with an IC50 of 5 μM. KY 234 significantly inhibits leukotriene D4 (LTD4), histamine, and antigen-induced bronchoconstriction in guinea pigs, with IC50 values of 6.0 mg/kg, 2.5 mg/kg, and 6.3 mg/kg, respectively .
|
-
- HY-10826
-
|
|
Aminopeptidase
|
Cardiovascular Disease
Neurological Disease
|
|
DG051 (free acid) is an effective inhibitor of leukotriene A4 hydrolase (LTA4H), with a Kd of 26 nM. It has high water solubility (greater than 30 mg/mL) and high oral bioavailability (over 80% across different species). DG051 (free acid) can be used in research related to myocardial infarction and stroke .
|
-
- HY-17595R
-
|
|
Parasite
Apoptosis
Microtubule/Tubulin
|
Infection
Cancer
|
|
Mebendazole (Standard) is the analytical standard of Mebendazole. This product is intended for research and analytical applications. Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
|
-
- HY-17409
-
|
|
Fungal
Antibiotic
Apoptosis
Bacterial
|
Infection
Cancer
|
|
Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
|
-
- HY-B0615AS
-
|
EN 313-d8; Ethmozin-d8; Moracizine-d8
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
|
-
- HY-116387
-
WR99210
2 Publications Verification
BRL 6231 free base
|
Dihydrofolate reductase (DHFR)
Parasite
|
Infection
|
|
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii .
|
-
- HY-106301
-
|
L-364,718; MK-329
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-N7225
-
|
Gnidilatidin
|
Others
|
Cancer
|
|
Yuanhuacine (Gnidilatidin), a diterpene from Daphne genkwa, is an effective and highly selective inhibitor of the basal-like 2 (BL2) subtype of TNBC. Yuanhuacine can induce G2/M cell cycle arrest and has broad anti-tumor activity. Yuanhuacine is an orally active DNA damaging agent .
|
-
- HY-10053S1
-
|
|
Isotope-Labeled Compounds
Neurokinin Receptor
|
Neurological Disease
Endocrinology
|
|
Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
|
-
- HY-162037
-
|
|
CDK
FLT3
|
Cancer
|
|
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
|
-
- HY-158050
-
|
|
c-Fms
|
Cancer
|
|
PXB17 can inhibit CSF1R (IC50 = 1.7 nM) by blocking the activation of PI3K/ AKT/mTORC1 signaling. PXB17 is orally effective. PXB17 significantly inhibits the growth of CRC, improves PD-1 mAb efficacy and reduces tumor recurrence in CRC .
|
-
- HY-162584
-
|
|
TRP Channel
|
Others
|
|
TRPC4/5-IN-2 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC4/5-IN-2 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD) .
|
-
- HY-167891
-
|
|
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
|
|
GPD-1116 is an orally active Phosphodiesterase (PDE) 4 and PDE1 inhibitor. GPD-1116 can reduce smoke-induced apoptosis of lung cells. GPD-1116 is effective in several disease models in animals, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma and pulmonary hypertension .
|
-
- HY-14532
-
|
CMX001; HDP-CDV
|
CMV
HSV
Orthopoxvirus
|
Infection
|
|
Brincidofovir (CMX001), the lipid-conjugated prodrug of Cidofovir (HY-17438), is an orally available, long-acting antiviral. Brincidofovir shows activity against a broad spectrum of DNA viruses including cytomegalovirus (CMV), adenovirus (ADV), varicella zoster virus, herpes simplex virus, polyomaviruses, papillomaviruses, poxviruses, and mixed double-stranded DNA virus infections. Brincidofovir, an oral antiviral in late stage development, has proven effective against orthopoxviruses in vitro and in vivo. .
|
-
- HY-13011
-
|
CH5424802; RO5424802; RG7853
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-17364
-
Temozolomide
Maximum Cited Publications
120 Publications Verification
NSC 362856; CCRG 81045; TMZ
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects .
|
-
- HY-B0027
-
|
|
Antibiotic
Bacterial
|
Infection
Metabolic Disease
|
|
Valnemulin hydrochloride is an orally effective truncated pleurotin antibiotic that inhibits protein synthesis in bacteria by binding to peptidyl transferase in the 50s ribosome subunit. Valnemulin hydrochloride effectively eliminates Mycobacterium bovis in the lungs in an experimental bovine model of Mycoplasma bovis infection. Valnemulin hydrochloride can reduce the mortality of epidemic rabbit enteropathy and has no adverse effect on the growth performance of rabbits .
|
-
- HY-17593
-
|
CEM-101; OP-1068
|
Bacterial
Antibiotic
|
Infection
|
|
Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
|
-
- HY-18754
-
|
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
|
-
- HY-122906
-
|
|
c-Fms
|
Inflammation/Immunology
|
|
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis .
|
-
- HY-13676S
-
|
|
Isotope-Labeled Compounds
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
|
-
- HY-107322A
-
|
Mepirodipine; YM-09730-5 Free base
|
Calcium Channel
|
Cardiovascular Disease
|
|
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
|
-
- HY-N4107
-
|
|
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-122114
-
|
|
Potassium Channel
|
Neurological Disease
|
|
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC50 of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects .
|
-
- HY-18641
-
|
|
LPL Receptor
|
Cancer
|
|
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with Ki values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo .
|
-
- HY-16770
-
|
P-005672
|
Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Sarecycline is an orally effective narrow-spectrum tetracycline derivative antibiotic. Sarecycline has anti-inflammatory activity. Sarecycline inhibits the activity of Gram-positive bacteria and several types of keratobacterium acnes. Sarecycline interferes with tRNA accommodation and tethers mRNA to the 70S ribosome. Sarecycline can be used to study moderate to severe acne .
|
-
- HY-W749867
-
|
Calcium disodium EDTA dihydrate
|
Bacterial
|
Infection
Others
|
|
CaⅡ-EDTA disodium dihydrate (Calcium disodium EDTA dihydrate) is an orally active metal chelating reagent, exhibits bactericidal activities against periodontal pathogens Aggregatibacter actinomycetemcomitans, Prevotella intermedia and Porphyromonas gingivalis . CaⅡ-EDTA disodium dihydrate is effective chelating antidotes for lead- and cadmium poisoning .
|
-
- HY-162783
-
|
|
Histone Methyltransferase
|
Cancer
|
|
AZ-PRMT5i-1 (Compound 28) is an effective and orally active MTAP-selective PRMT5 inhibitor. AZ-PRMT5i-1 also demonstrates MTA cooperativity and exhibits both in vitro and in vivo antitumor activities, and can be used to study MTAP-deficient cancers .
|
-
- HY-146466
-
|
|
Others
|
Cancer
|
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-B0688
-
Dapsone
1 Publications Verification
4,4′-Diaminodiphenyl sulfone; DDS
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-18754A
-
|
FR 167653 sulfate
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo .
|
-
- HY-117048
-
|
PF-04191834
|
Lipoxygenase
|
Inflammation/Immunology
|
|
PF-4191834 (PF-04191834) is an orally active, noniron chelating, and non-redox inhibitor of the 5-Lipoxygenase (5-LOX) (IC50=229 nM), displays ~300-fold selectivity for 5-LOX over 12-LOX and 15-LOX, shows no activity toward the cyclooxygenase enzymes, and is effective in inflammation and pain .
|
-
- HY-13676S1
-
|
|
Isotope-Labeled Compounds
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
|
-
- HY-123801
-
|
GL-II-93
|
GABA Receptor
|
Others
|
|
MIDD0301 (GL-II-93) is an orally effective, anti-asthmatic positive allosteric modulator of GABAA receptor. MIDD0301 had no significant adverse immune reactions at repeated doses and was better than Prednisone (HY-B0214). MIDD0301 relaxes histamine contractions in guinea pig and human tracheal smooth muscle for the study of bronchial systolic diseases .
|
-
- HY-13676R
-
|
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate (Standard) is the analytical standard of Megestrol acetate. This product is intended for research and analytical applications. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
|
-
- HY-135041
-
|
SB-559448 choline
|
Thrombopoietin Receptor
|
Others
|
|
Totrombopag (SB-559448) choline is an orally effective thrombopoietin receptor (TpoR) agonist. By activating TpoR, Totrombopag choline initiates an intracellular signaling cascade mediated by JAK2 kinase and the transcription factor Stat5, a signaling process that is the primary mechanism regulating megakaryocyte growth and differentiation into platelets. Totrombopag choline can be used to study platelet production and megakaryocyte biology .
|
-
- HY-13011A
-
|
CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
|
-
- HY-107429
-
|
PF-04965842
|
JAK
|
Inflammation/Immunology
|
|
Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
|
-
- HY-N0626
-
|
|
Fungal
Bacterial
Endogenous Metabolite
Antibiotic
IGF-1R
|
Infection
|
|
Sorbic acid is an effective, safe, and non-toxic food preservative. It can effectively inhibit most molds, yeasts, and certain bacteria. Sorbic acid is orally active and can enhance the growth performance of economically important animals (Duroc × Landrace × Yorkshire piglets) by activating the insulin-like growth factor system (IGF), and it can also lead to lipid accumulation by disrupting lipid clearance pathways 。
|
-
- HY-B0688S
-
|
4,4′-Diaminodiphenyl sulfone-d8; DDS-d8
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
Cancer
|
|
Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
|
-
- HY-137958
-
|
AT-527
|
HCV
SARS-CoV
|
Infection
|
|
Bemnifosbuvir hemisulfate (AT-527), a hemisulfate salt of AT-511, a guanosine nucleotide proagent, is a potent and orally active HCV viral replication inhibitor. Bemnifosbuvir hemisulfate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity .
|
-
- HY-144305
-
|
|
URAT1
GLUT
|
Infection
|
|
KPH2f is a safe, orally active, and effective dual URAT1/GLUT9 inhibitor with IC50s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. KPH2f shows little effects on OAT1 and ABCG2 (IC50=32.14 and 26.74 μM) .
|
-
- HY-148792
-
|
PRAX-562
|
Sodium Channel
|
Neurological Disease
|
|
Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .
|
-
- HY-153386
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .
|
-
- HY-155782
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis .
|
-
- HY-107725A
-
|
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
BIBO3304 (diTFA) is an orally effective and selective neuropeptide Y (NPY) Y1 receptor antagonist. BIBO3304 (diTFA) has a high affinity for both human and rat Y1 receptors, with IC50 values of 0.38 and 0.72 nM, respectively. BIBO3304 (diTFA) promotes bone-tendon healing through the Wnt/β-catenin signaling pathway .
|
-
- HY-B0976AR
-
|
Th-1165a (Standard); Phenoterol hydrobromide (Standard)
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol (hydrobromide) (Standard) is the analytical standard of Fenoterol (hydrobromide). This product is intended for research and analytical applications. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research .
|
-
- HY-15790H
-
-
- HY-50878
-
|
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-B0023
-
|
CS 905
|
Calcium Channel
MEK
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Azelnidipine (CS 905) is a dihydropyridine calcium channel blocker that is effective orally. Azelnidipine inhibits the intracellular calcium ion flow and lower blood pressure by selectively blocking L-type calcium channel on the membrane of vascular smooth muscle. Azelnidipine inhibits esophageal squamous cell carcinoma proliferation by targeting MEK1/2. Azelnidipine also has anti-inflammatory, antioxidant and neuroprotective effects .
|
-
- HY-B0364A
-
|
Dyclocaine hydrochloride
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Infection
Cancer
|
|
Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 μM for ALDH2 and 76 μM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local agent that can suppress or relieve pain. that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
|
-
- HY-B0780
-
-
- HY-B1156
-
|
Cefradine; SQ-11436
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-108044
-
|
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease .
|
-
- HY-129982
-
|
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
|
SC-435 is an orally effective apical sodium codependent bile acid transporter (ASBT) inhibitor. SC-435 effectively removes neurotoxic bile acids and ammonia from the blood by inhibiting intestinal ASBT, thereby alleviating liver and brain damage caused by liver failure. SC-435 can alter hepatic cholesterol metabolism and lower plasma low-density lipoprotein-cholesterol concentrations .
|
-
- HY-144456
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model .
|
-
- HY-50878B
-
|
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-105634AR
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Nomegestrol acetate (Standard) is the analytical standard of Nomegestrol acetate. This product is intended for research and analytical applications. Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies .
|
-
- HY-B1156A
-
|
Cefradine sodium; SQ-11436 sodium
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine sodium is a broad-spectrum and orally active cephalosporin. Cephradine sodium is active against both gram-positive and gram-negative pathogens. Cephradine sodium is effective in eradicating most penicillinase-producing organisms. Cephradine sodium has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine sodium blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-106301R
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Devazepide (Standard) is the analytical standard of Devazepide. This product is intended for research and analytical applications. Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of cholecystokinin (CCK) receptor, with IC50s of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors, respectively. Devazepide (L-364,718) is effective for gastrointestinal disorders .
|
-
- HY-17409R
-
|
|
Fungal
Antibiotic
Apoptosis
Bacterial
|
Infection
|
|
Nystatin (Standard) is the analytical standard of Nystatin. This product is intended for research and analytical applications. Nystatin is an orally active polyene antifungal antibiotic effective against yeast and mycoplasma. Nystatin increases the permeability of plasma membranes to small monovalent ions, including chloridion . Nystatin is a cholesterol-sequestering agent , partially prevents Oxaliplatin-induced lipid raft aggregation, DR4 and DR5 clustering, and thereby reduces apoptosis .
|
-
- HY-107758
-
|
|
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Y-29794 oxalate is a selective, orally active and blood-brain barrier permeable non-peptide prolyl endopeptidase inhibitor. Y-29794 oxalate blocks the IRS1-AKT-mTORC1 pathway and inhibits tumor growth. Y-29794 oxalate is also effective in inhibiting the progression of Aβ-like deposition in the hippocampus of aging-accelerated mice (SAM) .
|
-
- HY-10221
-
|
SAHA; Suberoylanilide hydroxamic acid
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
HPV
|
Infection
Cancer
|
|
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
|
-
- HY-N0202
-
|
Asterolide
|
ERK
Apoptosis
p38 MAPK
Akt
Src
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
- HY-B2141
-
|
|
NO Synthase
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Others
Metabolic Disease
|
|
Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats .
|
-
- HY-17364S
-
|
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
|
-
- HY-B0976AS
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
|
-
- HY-N7085
-
|
5,7-Dimethoxycoumarin; Limettin
|
JNK
p38 MAPK
ERK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
|
-
- HY-13011S
-
|
CH5424802-d8; RO5424802-d8; AF802-d8
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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- HY-13011S1
-
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CH5424802-d6; RO5424802-d6; AF802-d6
|
Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
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Cancer
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|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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-
- HY-153714
-
|
BNM-1192; Menin-MLL inhibitor 27
|
Epigenetic Reader Domain
Potassium Channel
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Cancer
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|
BN-104 (BNM-1192) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. BN-104 is a weak hERG inhibitor, with an IC50 greater than 100 μM. BN-104 has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia .
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-
- HY-117955
-
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WAY 141839; Co 2-6749
|
GABA Receptor
|
Neurological Disease
|
|
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
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-
- HY-13011R
-
|
|
Anaplastic lymphoma kinase (ALK)
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Cancer
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|
Alectinib (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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-
- HY-17364R
-
|
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DNA Alkylator/Crosslinker
Autophagy
Apoptosis
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Cancer
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|
Temozolomide (Standard) is the analytical standard of Temozolomide. This product is intended for research and analytical applications. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects .
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- HY-17593R
-
|
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Bacterial
Antibiotic
|
Infection
|
|
Solithromycin (Standard) is the analytical standard of Solithromycin. This product is intended for research and analytical applications. Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
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- HY-B0688S1
-
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4,4′-Diaminodiphenyl sulfone-d4; DDS-d4
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
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- HY-B0027R
-
|
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Antibiotic
Bacterial
|
Metabolic Disease
Inflammation/Immunology
|
|
Valnemulin (hydrochloride) (Standard) is the analytical standard of Valnemulin (hydrochloride). This product is intended for research and analytical applications. Valnemulin (hydrochloride) is an orally effective truncated pleurotin antibiotic that inhibits protein synthesis in bacteria by binding to peptidyl transferase in the 50s ribosome subunit. Valnemulin hydrochloride effectively eliminates Mycobacterium bovis in the lungs in an experimental bovine model of Mycoplasma bovis infection. Valnemulin hydrochloride can reduce the mortality of epidemic rabbit enteropathy and has no adverse effect on the growth performance of rabbits .
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-
- HY-N4107R
-
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TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
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-
- HY-107429R
-
|
|
JAK
|
Inflammation/Immunology
|
|
Abrocitinib (Standard) is the analytical standard of Abrocitinib. This product is intended for research and analytical applications. Abrocitinib (PF-04965842) is a potent, orally active and selective JAK1 inhibitor, with IC50s of 29 and 803 nM for JAK1 and JAK2, respectively. Abrocitinib (PF-04965842) exhibits less active effect on TYK2 (IC50, 1.253 μM), and inhibits phosphorylation of STAT1, STAT3 and STAT5 after stimulation. Effective in autoimmune disease .
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-
- HY-B0688R
-
|
|
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone (Standard) is the analytical standard of Dapsone. This product is intended for research and analytical applications. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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-
- HY-15485
-
|
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Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma .
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-
- HY-15790
-
-
- HY-50878S
-
|
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-B2163
-
|
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
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-
- HY-N0108
-
|
Parietin; Rheochrysidin
|
Bacterial
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells .
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-
- HY-N6973
-
Boldine
1 Publications Verification
|
RANKL/RANK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Boldine is an apomorphine isoquinoline alkaloid extracted from the root of the pheasant pepper (Litsea cubeba). Boldine is an oral effective antioxidant, anti-inflammatory, antitumor agent, and can inhibit osteoclast formation. Boldine induces apoptosis of human bladder cancer cells by regulating ERK, AKT and GSK-3β. Boldine ameliorates bone destruction by down-regulating the OPG/RANKL/RANK signaling pathway. It can be used in rheumatoid arthritis research .
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-
- HY-128449
-
|
Cefradine monohydrate
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-B0648
-
|
17α-Hydroxy-6α-methylprogesterone; U8840
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
Medroxyprogesterone (17α-Hydroxy-6α-methylprogesterone) is a synthetic human variant of progesterone that is a progesterone receptor agonist with oral activity. Medroxyprogesterone can induce cell proliferation through the PI3K/Akt signaling pathway. Medroxyprogesterone has an inhibitory effect on atherosclerosis in mice. The progesterone agonist activity of Medroxyprogesterone is less effective than Medroxyprogesterone acetate (HY-B0469) .
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-
- HY-123639
-
|
N-(2-Phenylethyl)-indomethacin amide
|
COX
|
Inflammation/Immunology
Cancer
|
|
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active COX-2 inhibitor with an IC50 of 0.06 μM for purified human COX-2. LM-4108 shows anti-inflammatory activity and may be effective in prevention of cancer. Half-lives for the disappearance of 10 μM LM-4108 in rat, human, and mouse liver microsomes were 11 min, 21 min, and 51 min, respectively .
|
-
- HY-116538
-
|
trans-10,cis-12 CLA2
|
Endogenous Metabolite
PPAR
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
(10E,12Z)-Octadeca-10,12-dienoic acidactivates PPAR α and inhibits adipocyte differentiation . (10E,12Z)-Octadeca-10,12-dienoic acid and its downstream metabolites have various antioxidant and antitumor activities. (10E,12Z)-Octadeca-10,12-dienoic acid is effective orally .
|
-
- HY-159896
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
PAR4 antagonist 8 (Compound 20f) is an effective, orally active, and selective PAR4 antagonist with an IC50 value of 15.32 nM. PAR4 antagonist 8 exhibits favorable pharmacokinetic properties. PAR4 antagonist 8 not only effectively inhibits human platelet aggregation induced by PAR4 agonists (IC50 = 6.39 nM) but also inhibits mouse platelet aggregation. PAR4 antagonist 8 can be used in antithrombotic research .
|
-
- HY-W050154R
-
|
|
Parasite
Tyrosinase
NF-κB
CDK
|
Infection
Inflammation/Immunology
Cancer
|
|
Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .
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-
- HY-10221R
-
|
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
HPV
|
Infection
Cancer
|
|
Vorinostat (Standard) is the analytical standard of Vorinostat. This product is intended for research and analytical applications. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
|
-
- HY-50878R
-
|
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-101676
-
|
NID 525
|
Leukotriene Receptor
PPAR
Cytochrome P450
|
Metabolic Disease
|
|
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-19719
-
|
ARQ-092
|
Akt
Parasite
|
Infection
Cancer
|
|
Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib is effective against Leishmania .
|
-
- HY-115412
-
|
SAHA-d5; Suberoylanilide hydroxamic acid-d5
|
HDAC
Autophagy
Mitophagy
Filovirus
Apoptosis
HPV
|
Infection
Cancer
|
|
Vorinostat-d5 (SAHA-d5) is the deuterium labeled Vorinostat. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis . Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification .
|
-
- HY-12700
-
|
|
Trace Amine-associated Receptor (TAAR)
|
Neurological Disease
|
|
RO5256390 is an orally effective trace amine associated receptor 1 (TAAR1) agonist. RO5256390 exhibits pro-cognitive and antidepressant-like properties in rodent and primate models, showing similar brain activation patterns to Olanzapine (HY-14541). RO5256390 blocks compulsive overeating behavior in rats. RO5256390 can inhibit ATP (HY-B2176)-induced TNF secretion in mouse bone marrow-derived macrophages .
|
-
- HY-19719A
-
|
ARQ-092 hydrochloride
|
Akt
Parasite
|
Infection
Cancer
|
|
Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib hydrochloride is effective against Leishmania .
|
-
- HY-108521
-
|
|
RAR/RXR
Apoptosis
|
Metabolic Disease
Cancer
|
|
HX531 is an effective RXR antagonist with oral activity, with an IC50 of 18 nM, with activity against black melanoma. HC531 can eliminate the anti-apoptotic effects of all-trans-retinoic acid (t-RA) and exerts anti-obesity and anti-diabetic effects through leptin-dependent pathways and the p53-p21Cip1 pathway, resulting in G0/G1 cell cycle arrest .
|
-
- HY-B0688S2
-
|
4,4′-Diaminodiphenyl sulfone-13C12; DDS-13C12
|
Isotope-Labeled Compounds
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species
|
Infection
Inflammation/Immunology
|
|
Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-146434
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
TGFβ-IN-2 (Compound 9d) inhibits TGF-β-induced total collagen accumulation in NRK-49F cells with the IC50 of 4.31 μM. TGFβ-IN-2 suppresses the TGF-β-induced protein expression of COL1A1, α-SMA, and p-Smad3 in vitro. TGFβ-IN-2 can be used as a potential effective compound for anti-fibrosis in vivo by oral administration .
|
-
- HY-163514
-
|
|
Cholinesterase (ChE)
DYRK
|
Neurological Disease
|
|
hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research .
|
-
- HY-121746
-
|
|
PPAR
Calcium Channel
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
|
|
GW7845 is an orally active non-thiazolidinedione, tyrosine-derived PPARγ agonist. GW7845 is effective at inhibiting voltage-dependent calcium channels (VDCC) and relaxing pressurized arteries with IC50 of 3 μM by using Ba 2+ as the charge carrier through VDCC. GW7845-induced apoptosis is mitochondria- and apoptosome-dependent. GW7845 induces rapid mitochondrial membrane depolarization and release of cytochrome c in primary pro-B cells and BU-11 cells .
|
-
- HY-B0364AR
-
|
|
Bacterial
Fungal
Aldehyde Dehydrogenase (ALDH)
|
Infection
Cancer
|
|
Dyclonine (hydrochloride) (Standard) is the analytical standard of Dyclonine (hydrochloride). This product is intended for research and analytical applications. Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 μM for ALDH2 and 76 μM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local agent that can suppress or relieve pain. that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
|
-
- HY-B1156R
-
|
|
Bacterial
Antibiotic
TOPK
|
Infection
Inflammation/Immunology
|
|
Cephradine (Standard) is the analytical standard of Cephradine. This product is intended for research and analytical applications. Cephradine (Cefradine) is a broad-spectrum and orally active cephalosporin. Cephradine is active against both gram-positive and gram-negative pathogens. Cephradine is effective in eradicating most penicillinase-producing organisms. Cephradine has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
|
-
- HY-N7085R
-
|
|
ERK
JNK
p38 MAPK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
|
-
- HY-147531
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 106 (compound 8) is an orally active and potent antibacterial agent with antibiofilm activity. Antibacterial agent 106 shows potent antibacterial effect against multi-agent resistant (MDR)-Gram positive pathogens. Antibacterial agent 106 is highly effective in clearing 99.7% of the intracellular methicillin-resistant S. aureus (MRSA) harbored inside macrophages . Antibacterial agent 106 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15196
-
TAK-285
2 Publications Verification
|
EGFR
|
Cancer
|
|
TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
|
-
- HY-100769
-
|
YL0919
|
5-HT Receptor
|
Neurological Disease
|
|
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A?receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-158261
-
|
|
Cholinesterase (ChE)
Amyloid-β
Beta-secretase
|
Neurological Disease
|
|
AChE-IN-63 (Compound 5AD) is a selective inhibitor of hAChE (IC50=0.103 μM). AChE-IN-63 also inhibits hBChE and hBACE-1 (IC50= 10 μM (hBChE); 1.342 μM (hBACE-1)). AChE-IN-63 inhibits Aβ aggregation, preventing the formation and deposition of Aβ1-42. AChE-IN-63 can effectively penetrate the blood-brain barrier and is orally effective. It is primarily used in Alzheimer's disease research .
|
-
- HY-N0202R
-
|
|
ERK
Apoptosis
p38 MAPK
Src
Akt
STAT
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
|
-
- HY-164670
-
|
|
Others
|
Inflammation/Immunology
|
|
D228 is an orally active antiinflammatory agent. D228 reduces ConA induced T lymphocyte cell proliferation (IC50: 42.85 μM) and LPS induced B lymphocyte cell proliferation (IC50: 3.15 μM). D228 is effective against inflammatory bowel disease (IBD). D228 alleviates the DSS (HY-116282C)-induced inflammation response in the IBD model by downregulating the MyD88/TRAF6/p38 signaling .
|
-
- HY-114504
-
|
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models .
|
-
- HY-B2181
-
|
Bismuth(III) oxynitrate
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Bismuth subnitrate (Bismuth(III) oxynitrate) is a simple and efficient catalyst for the synthesis of methyl ketone by martensitic acetylene hydration reaction. When Bismuth subnitrate is intraperitoneally injected into mice, the distribution characteristics of bismuth (Bi) in the brain are similar to those of other exogenous metals such as mercury, silver and gold. Bismuth subnitrate has antibacterial activity, which can inhibit the growth of Staphylococcus aureus and Escherichia coli. Bismuth subnitrate is effective orally and can be used for the study of gastrointestinal diseases, which has protective effect on alcoholic gastric ulcer in rats .
|
-
- HY-161356
-
|
|
SARS-CoV
|
Infection
|
|
BPR3P0128 is an orally active, non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that has been shown to inhibit the activity of various SARS-CoV-2 variants. The EC50 for SARS-CoV-2 and HCoV-229E are 0.62 µM and 0.14 µM. BPR3P0128 demonstrates effective anti-pancoronavirus activity within the submicromolar range. PR3P0128 shows synergistic antiviral activity when combined with Remdesivir (HY-104077) .
|
-
- HY-118285
-
|
|
mGluR
|
Neurological Disease
|
|
Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
|
-
- HY-B2163R
-
|
|
PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Astaxanthin (Standard) is the analytical standard of Astaxanthin. This product is intended for research and analytical applications. Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
|
-
- HY-112823A
-
|
HS-10296 mesylate
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
|
-
- HY-112823B
-
|
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-W050154
-
|
|
Parasite
Tyrosinase
NF-κB
CDK
|
Infection
Inflammation/Immunology
Cancer
|
|
Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity .
|
-
- HY-N6746
-
|
NSC 186
|
Bacterial
Fungal
Endogenous Metabolite
Apoptosis
|
Infection
Neurological Disease
Cancer
|
|
Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity .
|
-
- HY-112823
-
|
HS-10296
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-145259
-
|
|
HDAC
Histone Demethylase
|
Cancer
|
|
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-50878AS
-
|
PF-02341066-d9 hydrochloride
|
c-Met/HGFR
Autophagy
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Isotope-Labeled Compounds
|
Cancer
|
|
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-161953
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC50=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects .
|
-
- HY-16278
-
|
LCQ-908
|
Acyltransferase
BCRP
OAT
|
Infection
Metabolic Disease
|
|
Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-16278A
-
|
LCQ 908 sodium
|
Acyltransferase
BCRP
OAT
|
Infection
Metabolic Disease
|
|
Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro .
|
-
- HY-149155
-
|
|
Others
|
Infection
|
|
o-Cymen-5-ol is a broad-spectrum antimicrobial agent with direct antimicrobial activity. o-Cymen-5-ol showed effective minimum inhibitory concentrations (MICs) against a variety of bacteria and fungi, such as Streptococcus mutans and Candida albicans. The combination of o-Cymen-5-ol and zinc showed synergistic effects, enhancing the inhibitory effect against oral pathogens. o-Cymen-5-ol was able to inhibit the glycolysis process and co-enhanced this effect with zinc. o-Cymen-5-ol showed a stronger antibacterial effect in toothpaste than placebo .
|
-
- HY-112823R
-
|
|
EGFR
|
Cancer
|
|
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-10122
-
|
KAD 3213; KMD 3213
|
Adrenergic Receptor
Bacterial
|
Endocrinology
Cancer
|
|
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 .
|
-
- HY-162677
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
|
-
- HY-164411
-
|
|
c-Met/HGFR
|
Cancer
|
|
KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
|
-
- HY-163982
-
|
|
FOXO
Others
|
Inflammation/Immunology
|
|
FOXJ1 agonist 1 (compound 16c) is an orally effective small molecule that can effectively enhance the expression of FOXJ1. Foxj1-IN-1 acts on the mammalian airway system composed of multiciliated cells (MCC) to prevent the development and onset of chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 can induce the production of motile cilia in the respiratory system of zebrafish and mammals, and inhibit elastase-induced COPD mouse models. Foxj1-IN-1 has good liver microsomal stability, in vivo PK curve and AUC; it has no significant inhibition of CYP and hERG, and does not have significant cytotoxicity .
|
-
- HY-10122S
-
|
|
Isotope-Labeled Compounds
Adrenergic Receptor
|
Endocrinology
Cancer
|
|
Silodosin-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[1][3].
|
-
- HY-116673
-
|
|
Histone Acetyltransferase
|
Neurological Disease
|
|
TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
|
-
- HY-159579
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
CW-3308 is an orally effective PROTAC that selectively targets BRD9 and is expected to be used to inhibit synovial sarcoma, rhabdomyoma, and other BRD9-dependent human diseases. CW-3308 is composed of PROTAC target protein ligand Naphthyridin-Me-dimethoxybenzene-COOH (HY-159596) (red part), Linker 3-Azaspiro[5.5]undecane-9-methanol (HY-159598) (black part), E3 ubiquitin ligase ligand Thalidomide-methylpyrrolidine (HY-159597) (blue part), where the conjugate of E3 ubiquitin ligase ligand + linker is Thalidomide-pyrrolidine-C-azaspiro (HY-159599) [1] .
|
-
- HY-10122R
-
|
|
Adrenergic Receptor
Bacterial
|
Endocrinology
Cancer
|
|
Silodosin (Standard) is the analytical standard of Silodosin. This product is intended for research and analytical applications. 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 .
|
-
- HY-B0596
-
|
TA-0910
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-N7110
-
|
|
Akt
ERK
JNK
GABA Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT, ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABAA) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role .
|
-
- HY-W027553
-
|
NIK-247 free base
|
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Neurological Disease
Metabolic Disease
|
|
Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
- HY-N6746S1
-
|
NSC 186-13C13
|
Isotope-Labeled Compounds
Apoptosis
Bacterial
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Citrinin- 13C13 (NSC 186- 13C13) is the 13C labeled Citrinin (HY-N6746). Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity .
|
-
- HY-117921
-
|
|
Others
|
Inflammation/Immunology
|
|
DA-E 5090 is an orally effective inhibitor of IL-1 production that can be converted into a pharmacologically active deacetylated form (DA-E5090) in vivo. In this study, the effects of DA-E5090 on IL-1 production in vitro were examined by LPS-stimulated human monocytes. The results showed that DA-E5090 could dose-dependently inhibit the production of IL-1α and IL-1β (1-10 μM) by LPS-stimulated human monocytes, as determined by LAF assay and ELISA. Northern blotting analysis showed that DA-E5090 inhibited the transcription of IL-1α and IL-1β mRNA.
|
-
- HY-164476
-
|
|
EGFR
GSK-3
PD-1/PD-L1
|
Cancer
|
|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
|
-
- HY-116538R
-
|
|
Endogenous Metabolite
PPAR
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
(10E,12Z)-Octadeca-10,12-dienoic acid (Standard) is the analytical standard of (10E,12Z)-Octadeca-10,12-dienoic acid. This product is intended for research and analytical applications. (10E,12Z)-Octadeca-10,12-dienoic acidactivates PPAR α and inhibits adipocyte differentiation . (10E,12Z)-Octadeca-10,12-dienoic acid and its downstream metabolites have various antioxidant and antitumor activities. (10E,12Z)-Octadeca-10,12-dienoic acid is effective orally .
|
-
- HY-B0596A
-
|
TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
|
-
- HY-151260
-
|
|
Beta-secretase
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .
|
-
- HY-162415
-
|
|
c-Fms
Apoptosis
|
Cancer
|
|
CSF1R-IN-22 (Compound C19) is an orally effective CSF-1R selective inhibitor (IC50<6 nM). CSF1R-IN-22 enhances the secretion of CXCL9 from M2 macrophages, increases CD8 + T cell infiltration. CSF1R-IN-22 boosts anti-tumor immune responses of anti-PD-1, and induces apoptosis in tumor cells. CSF1R-IN-22 can effectively reprogram M2-like TAMs (tumor-associated macrophages) to the M1 phenotype and reshape the TME by inducing the recruitment of CD8 + T cells into tumors and reducing the infiltration of immunosuppressive Tregs and MDSCs .
|
-
- HY-116275
-
|
|
Others
|
Cancer
|
|
KRM-II-81 is a gamma-aminobutyric acid type A (GABAA) receptor ligand with analgesic, anxiolytic and anti-epileptic activities. KRM-II-81 exhibits positive allosteric modulation of GABAA receptors selective for the α2/3 subunit. KRM-II-81 reduces formalin-induced pain response after oral administration. KRM-II-81 significantly reduces pain behavior induced by chronic spinal nerve ligation. Analysis of KRM-II-81 showed that its plasma and brain concentrations were positively correlated with analgesic effects. The enhancement effect of KRM-II-81 on GABA current shows its key role in the analgesic mechanism. KRM-II-81 was less effective in respiratory depression, demonstrating its safety and tolerability .
|
-
- HY-162816
-
|
|
PROTACs
MAP4K
|
Cancer
|
|
PROTAC PD-L1 degrader-2 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC PD-L1 degrader-2 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC PD-L1 degrader-2 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC PD-L1 degrader-2 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841) [1] .
|
-
- HY-136720
-
|
|
Others
|
Others
|
|
ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
|
-
- HY-117991
-
|
|
Others
|
Cancer
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DW10075 is a novel, highly selective VEGFR inhibitor that targets the VEGF/VEGF receptor (VEGFR) pathway, which has been shown to be an effective anti-angiogenic approach for cancer therapy. Studies have found that DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3 among 21 kinases, while having no effect on the other 18 kinases, including FGFR and PDGFR. In human umbilical vein endothelial cells (HUVECs), DW10075 significantly prevented VEGF-induced activation of VEGFR and its downstream signaling, thereby inhibiting VEGF-induced HUVEC proliferation. In addition, DW10075 dose-dependently inhibited VEGF-induced HUVEC migration and tube formation, and suppressed angiogenesis in the rat aortic ring model and the chick embryo chorionic membrane model. DW10075 also exhibited antiproliferative activity against 22 different human cancer cell lines, with IC50 values ranging from 2.2 μmol/L (for U87-MG human glioblastoma cells) to 22.2 μmol/L (for A375 melanoma cells). In the nude mouse U87-MG xenograft tumor model, oral administration of DW10075 significantly inhibited tumor growth and reduced the expression of CD31 and Ki67 in tumor tissues. In summary, DW10075 is a potential anti-tumor angiogenesis agent that deserves further development.
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HY-L061
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3,666 compounds
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Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 3,666 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
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| Cat. No. |
Product Name |
Type |
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- HY-W353258
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BAY 12-8039 monohydrate
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Biochemical Assay Reagents
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Moxifloxacin (BAY 12-8039) hydrochloride monohydrate is an orally active bacterial inhibitor that is effective against Streptococcus pneumoniae. Moxifloxacin hydrochloride monohydrate can be used in tuberculosis research .
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- HY-W749867
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Calcium disodium EDTA dihydrate
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Chelators
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CaⅡ-EDTA disodium dihydrate (Calcium disodium EDTA dihydrate) is an orally active metal chelating reagent, exhibits bactericidal activities against periodontal pathogens Aggregatibacter actinomycetemcomitans, Prevotella intermedia and Porphyromonas gingivalis . CaⅡ-EDTA disodium dihydrate is effective chelating antidotes for lead- and cadmium poisoning .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N11630
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-
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- HY-130750
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-
-
- HY-N2486
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-
-
- HY-A0124A
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-
-
- HY-B1327
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-
-
- HY-17409
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-
-
- HY-N7225
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-
-
- HY-N4107
-
-
-
- HY-N0626
-
-
-
- HY-N2486R
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-
-
- HY-17409R
-
-
-
- HY-N0202
-
-
-
- HY-N7085
-
-
-
- HY-N4107R
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-
-
- HY-B2163
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-
-
- HY-N0108
-
-
-
- HY-N6973
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-
-
- HY-W050154R
-
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Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
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Parasite
Tyrosinase
NF-κB
CDK
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Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .
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- HY-N7085R
-
|
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Structural Classification
Natural Products
Rutaceae
Plants
Citrus medica Linn. var. sarcodactylis (Noot.) Swingle
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ERK
JNK
p38 MAPK
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Citropten (Standard) is the analytical standard of Citropten. This product is intended for research and analytical applications. Citropten (5, 7-dimethoxycoumarin) is one of the coumarin derivatives. Citropten is an effective oral anticancer agent. Citropten has anti-proliferative activity against A2058 and B16 melanoma cells. Citropten exerts anti-inflammatory effects through the NFκB and MAPK signaling pathways. Citropten acts as an antidepressant through heat shock protein-70, monoamine oxidase-A and inhibition of apoptosis .
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-
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- HY-N0202R
-
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Structural Classification
Terpenoids
Sesquiterpenes
Source classification
Astragalus caprinus L.
Plants
Compositae
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ERK
Apoptosis
p38 MAPK
Src
Akt
STAT
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Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
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-
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- HY-B2163R
-
|
|
Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
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PPAR
Reactive Oxygen Species
STAT
NF-κB
Apoptosis
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Astaxanthin (Standard) is the analytical standard of Astaxanthin. This product is intended for research and analytical applications. Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant. Astaxanthin inhibits NF-κB and down-regulates VEGF in blood glucose. Astaxanthin exerts anti-cancer cell proliferation, increases apoptosis, impairs migration and invasion by activating PPARγ and reducing the expression of STAT3. Astaxanthin also has neuroprotective and anti-inflammatory activity and can be used in studies of cancer, diabetic retinopathy, cardiovascular disease, and in the coloring of animal feed .
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- HY-W050154
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- HY-N6746
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-
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- HY-N7110
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-
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-112094S
-
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WNK-IN-11-d3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor. WNK-IN-11-d3 is effective at regulating cardiovascular homeostasis[1].
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-
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- HY-17412S1
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Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
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-
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- HY-157585S
-
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21-Dehydro Budesonide-d8-1 is deuterated labeled dehydrogenated Budesonide (HY-13580). Budesonide is an orally available glucocorticoid receptor agonist with anti-cancer activity. 21-Dehydro Budesonide-d8-1 acts as a probe for glucocorticoid receptors and is used in isotope tracing studies .
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-
-
- HY-17412S
-
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Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
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-
-
- HY-117281S1
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Moexipril-d3 is deuterated labeled Moexipril (HY-117281). Moexipril is an orally active inhibitor of angiotensin-converting enzyme (ACE), and becomes effective by being hydrolyzed to moexiprila hydrochloride. Moexipril exhibits antihypertensive and neuroprotective effects - .
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-
- HY-13571AS1
-
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Beclometasone dipropionate-d10 is the deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
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-
-
- HY-13571AS
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Beclometasone dipropionate-d6 is deuterium labeled Beclometasone dipropionate. Betamethasone dipropionate, the proagent of Betamethasone, is an orally active and potent glucocorticoid with anti-inflammatory and immunosuppressive activity. Betamethasone appears to be an effective inhibitor of LPS-induced inflammation and MMP release[1][2].
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- HY-B0615AS
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Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
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-
- HY-10053S1
-
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Maropitant- 13C,d3 is the 13C- and deuterium labeled Maropitant. Maropitant is a selective and orally active neurokinin (NK1) receptor antagonist. Maropitant acts by blocking the binding of substance P within the emetic center and the chemoreceptor trigger zone (CRTZ). Maropitant is highly effective in preventing vomiting[1][2].
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-
- HY-13676S
-
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Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
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- HY-13676S1
-
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Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway[1][2][3][4][5].
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-
- HY-B0688S
-
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Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases[2][3][4][5].
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-
- HY-17364S
-
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Temozolomide-d3 is the deuterium labeled Temozolomide. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects[1][2].
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- HY-B0976AS
-
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Fenoterol-d6 (hydrobromide) (Th-1165a-d6) is the deuterium labeled Fenoterol hydrobromide. Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research[1][2].
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-
-
- HY-13011S
-
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|
Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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-
-
- HY-13011S1
-
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Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively[1]. Alectinib demonstrates effective central nervous system (CNS) penetration[2].
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-
- HY-B0688S1
-
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|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities[1]. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al[2][3].
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-
- HY-50878S
-
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Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
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-
-
- HY-B0688S2
-
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Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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-
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- HY-50878AS
-
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Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
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- HY-10122S
-
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Silodosin-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[1][3].
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- HY-N6746S1
-
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Citrinin- 13C13 (NSC 186- 13C13) is the 13C labeled Citrinin (HY-N6746). Citrinin (NSC 186) is a mycotoxin that causes food contamination and has different toxic effects. Citrinin is an effective oral anticancer agent. Citrinin has various regulatory effects on mouse immune system, including regulating the number of immune cells, inducing apoptosis and autophagy of immune cells, altering toll-like receptor expression and cytokine production. Citrinin can induce oxidative stress and lead to early apoptosis of oocytes. Low doses of Citrinin have neuroprotective effects against glutamate-induced excitotoxicity in rat cortical neurons. In addition, Citrinin also has antibacterial activity .
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-
| Cat. No. |
Product Name |
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Classification |
-
- HY-145259
-
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Alkynes
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HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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