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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC79587 BMY 20844
BMY 20844 is an orally active platelet cAMP phosphodiesterase inhibitor with anti-thrombosis activity. BMY 20844 can elevate cAMP levels and activate protein kinase in platelets. BMY 20844 can be used for the research of cardiovascular disease.
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DC79586 MDOLL-0286
MDOLL-0286 is a selective Poly(ADP-ribose) Glycohydrolase (PARG) (ARH3) inhibitor with an IC50 of 2.3μM. MDOLL-0286 can inhibit ARH3’s poly-ADP-ribose hydrolytic activity on cellular substrates. MDOLL-0286 can inhibit DNA damage response. MDOLL-0286 can be used for the research of cancer .
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DC79585 PARP14 inhibitor 2
PARP14 inhibitor 2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of <30 nM. PARP14 inhibitor 2 inhibits the mono-ADP-ribosyltransferase activity of PARP14 and regulates IFN-γ and IL-4 signaling, reversing protumor macrophage polarization and inhibiting anti-tumor inflammatory responses. PARP14 inhibitor 2 is promising for research of PARP14-related diseases such as tumors, atopic dermatitis and autoimmune diseases.
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DC79583 Otviciclib
Otviciclib (Compound 86) is a CDK inhibitor. Otviciclib has potent anti-proliferative activity against solid tumor cells (such as HCT116, NCIH82 and DU145 cells) with no significant toxicity to normal cells, and effectively induces the G2/M phase cells arrest and apoptosis. Otviciclib has a broad-spectrum anticancer activity, such as colon, pancreatic and lung cancer.
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DC79582 AXT-914
AXT-914 is a Calcium-sensing receptor (CaSR) inhibitor. AXT-914 has antiviral activity against the coronavirus HCoV 229E and SARS-CoV2. AXT914 reduces cytosolic calcium signalling activity of CaSR mutations. AXT-914 can be used for Bartter syndrome type 5 and autosomal dominant hypocalcemia (ADH) and coronavirus infections research.
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DC79581 PSD-506
PSD-506 (RO 3202904) is a muscarinic M2/M3 antagonist. PSD-506 has the potential to be used in studies of bladder overactivity and urinary incontinence.
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DC79580 MT-21
MT-21 is an Apoptosis inducer and adenine nucleotide translocase inhibitor. MT-21 induces Apoptosis by activating JNK via the Krs/MST protein. MT-21 activates caspase-3 via caspase-9. MT-21 induces the release of cytochrome c. MT-21 can be used in the research of tumors.
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DC79579 BRL 55834
BRL 55834 is an orally and potent potassium channel activator. BRL 55834 exhibits great bronchodilator potency but reduces tendency to lower arterial blood pressure. BRL 55834 has the potential to use as a bronchodilator.
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DC79578 RWJ 29009
RWJ 29009 is a highly selective ATP-sensitive potassium channel agonist. RWJ 29009 activates potassium channel in vascular smooth muscle cells, promoting potassium efflux and membrane hyperpolarization to induce coronary and peripheral vasodilation. RWJ 29009 is promising for research of cardiovascular diseases such as acute myocardial ischemia and hypertension.
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DC79577 LRH-0003
LRH-0003 is an inhibitor of the Macrodomain 1 (Mac1) of nonstructural protein 3 (NSP3) from SARS-CoV-2, with an IC50 value of 1.7 μM. LRH-0003 can be used for the research antiviral infection targeting SARS-CoV-2.
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DC79576 GNE-5152
GNE-5152 is an orthosteric SARM1 base-exchange (BE) inhibitor. GNE-5152 sustainably activates SARM1 at subinhibitory concentrations under mildly activating conditions, and this synergistic adverse effect increases NAD consumption, induces axon degradation and neurodegeneration and releases neurofilament-light (NfL) in cortical neurons. GNE-5152 can be used for neurodegenerative diseases research.
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DC79575 DMP-851
DMP-851 is a cyclic urea HIV protease inhibitor, with a Ki of 0.021 nM. DMP-851 shows antiviral activity against laboratory strains of HIV-l and HIV-2 as well as against primary clinical isolates derived from Zidovudine-resistant samples (A018C, E, WR 10983).
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DC79574 Ispinesib mesylate
Ispinesib (SB-715992) mesylate is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.
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DC79573 Adavosertib-C3-NH-Boc
Adavosertib-C3-NH-Boc is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for Wee1 and a PROTAC linker, which recruits E3 ligases. Adavosertib-C3-NH-Boc can be used for synthesis of PROTAC Pomalidomide-C3-adavosertib
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DC79572 BMS-812204
BMS-812204 is a highly selective CB-1 receptor antagonist. BMS-812204 is promising for research of obesity and metabolic disorders.
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DC79571 Palbociclib-C4-Boc
Palbociclib-C4-Boc is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for CDK4/6 Palbociclib and a PROTAC linker, which recruits E3 ligases. Palbociclib-C4-Boc can be used for synthesis of PROTAC BSJ-03-204
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DC79569 Epibenzomalvin E
Epibenzomalvin E is an isomer of Benzmalvin E. Benzomalvin E is an indoleamine 2,3-dioxygenase inhibitor.
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DC79568 BIEGi-1
BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC).
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DC79567 Ranbezolid hydrochloride
Ranbezolid (RBx7644 free base) is an orally active, oxazolidinone antibiotic against Gram-positive and Gram-negative anaerobes including Staphylococcus aureus, Staphylococcus epidermidis and Bacteroides fragilis. Ranbezolid can inhibit the 50s ribosomal subunit with an IC50 of 17 μM for bacterial ribosomes. Ranbezolid interferes cell wall and lipid synthesis. Ranbezolid can rapidly kill bacteria, significantly reduce bacterial load, and has better cardiovascular safety. Ranbezolid can be used for the study of antibiotics for anaerobic bacteria.
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DC79564 NSC 727357
NSC 727357 is a DNA intercalator and topoisomerase inhibitor with antitumor activity. NSC 727357 can inhibit cells proliferation and induce G1 phase arrest. NSC 727357 can be used for the research of cancer, such as melanoma.
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DC79563 (S)-Padsevonil
(S)-Padsevonil is the S-enantiomer of Padsevonil).Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models.
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DC79562 RO-488684
RO-488684 is a benzodiazepine receptor agonist. RO-488684 can be used for research on sleep and conscious sedation.
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DC79561 L-657743
L-657743 is a highly potent, highly selective, and orally active α2-adrenoceptor antagonist. L-657743 can be used in the research of neurological diseases such as depression.
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DC79560 FK-664
FK-664 is a leukotriene inhibitor. FK-664 enhances ventricular contractility and shortens the time to peak tension in cardiac cells. FK-664 reduces mean circulating pressure (MCP) in a canine model of heart failure. FK-664 can be used in research on cardiovascular diseases such as heart failure.
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DC79555 PDIC-NN dimethanesulfonate
PDIC-NN dimethanesulfonate (PDIC-NS) is a STING activator with anticancer activity. PDIC-NN dimethanesulfonate promotes the content and biostability of endogenous cyclic dinucleotides (CDNs). PDIC-NN dimethanesulfonate triggers ROS burst and causes serious damage to mitochondria. PDIC-NN dimethanesulfonate induces cell apoptosis and inhibits DNA replication. PDIC-NN dimethanesulfonate activates cGAS-STING signaling pathway, enhances the immunogenicity of tumor cells and activates a robust innate immune response.
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DC79554 S7958
S7958 is a selective and orally active antagonist of the TAS2R8 bitter taste receptor, with its IC50 being 0.06 μM. S7958 only has a weak inhibitory effect on TASR8 and TAS2R39, and has no significant impact on other receptors. S7958 significantly inhibits the perception of bitterness caused by substances such as coffee and drug active ingredients (API) by selectively antagonizing the human bitter taste receptor TAS2R8. S7958 can be used in the medical field to improve the research on the bitterness of oral preparations.
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DC79553 Di-Val-L-dC
Di-Val-L-dC, a prodrug of L-deoxycytidine, is a selective and specific anti-HBV agent.
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DC79552 dMeThPmR
dMeThPmR, a ribonucleoside derivative, is a potent and selective human nucleoside transporter 1 (hCNT1) inhibitor (Ki/sub> = 0.3-0.98 μM). dMeThPmR exhibit weak inhibitory activity on hCNT2 (IC50 = 133 μM) and hCNT3 (Ki = 32.7 μM). dMeThPmR can protect cells from the toxicity of nucleoside drugs. dMeThPmR can be used for the research of cancer.
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DC79551 BEA 005
BEA 005 is an antivirus agent. BEA 005 can block early systemic and mucosal infections with SIV and HIV-2.
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DC79550 MeThPmR
MeThPmR, a ribonucleoside derivative, is a potent and selective human nucleoside transporter 1 (hCNT1) inhibitor (Ki/sub> = 0.16-0.69 μM). MeThPmR exhibit weak inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR can protect cells from the toxicity of nucleoside drugs. MeThPmR can be used for the research of cancer.
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