Cat. No. | Product Name | Field of Application | Chemical Structure |
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DC26184 | DBPR112 Featured |
DBPR112 is a potent EGFR mutation inhibitor against EGFRL858R/T790M double mutations with IC50 of 48 nM and also exhibits 10-fold potency better than Osimertinib, against EGFR and HER2 exon 20 insertion mutations.
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DC26181 | M8891 Featured |
M8891 is a methionine aminopeptidase-2 (MetAP-2) selective inhibitor with Ki and IC50 of 4.33 nM and 54 nM, respectively.
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DC26178 | BAY-298 Featured |
BAY-298 is a potent, and selective antagonists of the luteinizing hormone receptor with IC50 of 96 nM, 23 nM and 78 nM against human, rat, and cynomolgus monkey LH receptors.
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DC26177 | VUF16839 Featured |
VUF16839 is a high-affinity non-imidazole histamine H3 receptor agonist with pKi of 8.5 and pEC50 of 9.5, which shows weak activity on CYP enzymes and good metabolic stability.
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DC26190 | DS54360155 Featured |
DS54360155 is an orally potent analgesic without μ-opioid receptor agonist activity.
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DC26187 | AGX51 Featured |
AGX51 is a small-molecule Id antagonist and inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduced viability.
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DC65286 | SWE101 Featured |
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DC12579 | GS-6207 Featured |
GS-6207 (GS6207, GS-CA1) is a potent, selective inhibitor of HIV-1 capsid function with potency and potential to be clinically effective against a broad range of HIV-1 strains..
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DC34379 | 3AC Featured |
3AC is an inhibitor of SH2 domain-containing inositol-5’-phosphatase 1 (SHP-1). It is selective for SHP-1 over SHP-2 and phosphatase and tensin homolog (PTEN). 3α-Aminocholestane induces hyperactivation of the tyrosine kinase SYK in patient-derived Ph+ acute lymphoblastic leukemia (ALL) cells and selectively induces cytotoxicity in these cells over mature B cell lymphoma cells. It reduces leukemia burden and increases survival in a tyrosine kinase inhibitor-resistant patient-derived Ph+ ALL mouse xenograft model when administered at a dose of 50 mg/kg. 3α-Aminocholestane reduces cell viability of OPM2 multiple myeloma (MM) cells in a concentration-dependent manner and of RPMI8226 MM cells when used at concentrations greater than or equal to 12.5 μM. It halts the cell cycle at the G0/G1 or G2/M stages in the highly proliferative OPM2 or less proliferative RPMI8226 cell lines, respectively. It induces apoptosis via activation of caspase-3, caspase-9, and poly(ADP-ribose) polymerase (PARP) in OPM2 cells but not in RPMI8226 cells. 3α-Aminocholestane reduces tumor burden and increases survival in an OPM2 mouse xenograft model.
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DC34549 | Nimbolide Featured |
Nimbolide is a natural inhibitor of pancreatic cancer growth and metastasis through ROS-mediated apoptosis. It inhibits epithelial-to-mesenchymal transition.
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DC65284 | NC-1 Featured |
NC-1 is a novel highly active allosteric inhibitor of protein tyrosine phosphatase, non-receptor type 22 (PTPN22) which is a lymphoid-specific tyrosine phosphatase (LYP).
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DC65283 | neocarzilin A Featured |
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DC26207 | OP-3633 Featured |
OP-3633 is a potent steroidal glucocorticoid receptor (GR) antagonist with IC50 of 29 nM and shows excellent selectivity against GR over progesterone receptors (PR) and androgen receptors (AR).
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DC26205 | UDM-001651 Featured |
UDM-001651 is a potent , selective and orally active Protease-Activated Receptor 4 (PAR4) Antagonist with in Vivo Antithrombotic Efficacy (IC50 = 2.4 nM). UDM-001651 was evaluated in a monkey thrombosis model and shown to have robust antithrombotic efficacy and no prolongation of kidney bleeding time. This combination of excellent efficacy and safety margin strongly validates PAR4 antagonism as a promising antithrombotic mechanism.
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DC26194 | VU6003586 Featured |
VU6003586 is a novel allosteric modulators of mGlu5 with EC50 of 174 nM.
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DC26193 | Ziresovir (RO-0529, AK0529) Featured |
Ziresovir (RO-0529, AK0529) is a potent, selective and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein inhibitor with EC50 of 3 nM.
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DC47113 | DS44960156 Featured |
DS44960156 is a selective Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor, with IC50 values of 1.6 μM and >30 μM for MTHFD2 and MTHFD1, respectively.
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DC65281 | DS39201083 Featured |
DS39201083 is a potent novel analgesic without mu opioid agonist activity. DS39201083 had a unique bicyclic skeleton and was a more potent analgesic than conolidine, as revealed in the acetic acid-induced writhing test and formalin test in ddY mice. The compound showed no agonist activity at the mu opioid receptor.
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DC20245 | BRD0539 Featured |
BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.
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DC70727 | RA306 Featured |
RA306 (RA-306) is a selective, potent, orally active, ATP-competitive CaMKII inhibitor, inhibits CaMKII delta (IC50=15 nM), gamma (IC50=25 nM), and alpha (IC50=61 nM) isoforms.RA306 displays a good selectivity profile vs. kinases and non-kinase targets, as compared with KN-93.RA306 also displays a good cellular activity in cardiomyocytes from human, rat, and mice, with IC50s in the 200 nM range.Isoproterenol-induced phosphorylation of Thr17-PLN, normalized to total PLN, was fully inhibited by RA306 in a dose-dependent manner, with IC50s of 140 nM in rat, 205 nM in mouse, and 220 nM in human cardiomyocytes.
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DC12608 | BPN14770 Featured |
BPN14770 (BPN-14770) is an allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 and 7.4 nM for human PDE4D7 and PDE4D3 respectively, displays 16-fold less potent against monomeric form of PDE4D lacking the UCR1 dimerization domain (PDE4D2
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DC20262 | LY3154207 Featured |
LY3154207 is a potent and selective dopamine receptor D1 positive allosteric modulator for the treatment of Parkinson's disease dementia.
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DC20260 | AL-335 Featured |
AL-335 is a potent inhibitor of hepatitis C virus (HCV) NS5B polymerase with IE50 values as low as 70 nM. AL-335 is potentially useful for the Treatment of Hepatitis C Infection. AL-335 demonstrated high levels of the nucleoside triphosphate in vitro in primary human hepatocytes and Huh-7 cells as well as in dog liver following a single oral dose. AL-335 was selected for the clinical development where it showed promising results in phase 1 and 2 trials.
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DC20257 | KMN-159 Featured |
KMN-159 is a potent prostaglandin E2 type 4 (EP4) receptor agonist with Ki of 0.38 nM and shows five fold increase in potency versus KMN-80.
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DC12484 | KZR-616 Featured |
KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit.
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DC20249 | NRX-1933 Featured |
NRX-1933 is an enhancer of an E3 ligase-substrate interaction.
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DC20248 | NRX-1532 Featured |
NRX-1532 is an enhancer of an E3 ligase-substrate interaction.
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DC20247 | (R,R)-BNC375 Featured |
(R,R)-BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs.
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DC65280 | DS21360717 Featured |
DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
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DC65279 | NPD2381 Featured |
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