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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC59016 Ensitrelvir (S-217622) Featured
S-217622 is the first oral non-covalent, non-peptidic SARS-CoV-2 3CL protease inhibitor with IC50 of 0.096 μM. S-217622 displays antiviral activity in vitro towards a range of SARS-CoV-2 variants and coronavirus families, favorable drug metabolism and pha
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DC31069 RBN-2397 Featured
RBN-2397 is a potent, accross species and orally active NAD+ competitive inhibitor of PARP7 (IC50<3 nM). RBN-2397 selectively binds to PARP7 (Kd=0.001 μM) and restores interferon (Type I) signaling. RBN-2397 has the potential for the study of advanced or
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DC31012 Solabegron Featured
Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. Solabegron (GW 427353) is being developed for the treatment of over
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DC5199 S-Ruxolitinib (INCB018424) Featured
S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3.
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DC8225 Smoothened Agonist (SAG) free base Featured
SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM).
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DC11450 Selpercatinib(LOXO-292) Featured
Selpercatinib is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.
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DC12503 STD1T Featured
STD1T (USP2a inhibitor STD1T) is a hit-to-lead, small-molecule inhibitor of USP2a with IC50 of 3.3 uM in Ub-AMC assays, displays no activity against USP7 at 10 uM.
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DC7613 STATTIC Featured
Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1.
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DC9615 SR3335 Featured
SR3335 (ML-176) is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays.
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DC7956 SP2509 Featured
SP2509 is a novel histone demethylase LSD1 (KDM1A) antagonist with IC50 of 13 nM; no inhibition on MAO-A and MAO-B.
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DC7506 Sotrastaurin Featured
Sotrastaurin(AEB-071) is a potent and selective pan-PKC inhibitor, mostly for PKCθ with Ki of 0.22 nM; inactive to PKCζ.
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DC7501 SKLB1002 Featured
SKLB1002 is a novel and potent VEGFR-2 inhibitor with an IC50 value of 32 nM.
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DC10632 Sitravatinib (MGCD516) Featured
Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
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DC7294 SGX-523 Featured
SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.
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DC8444 Sabutoclax Featured
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
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DC12163 S55746 (BLC201) Featured
S55746 (BLC201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BLC201) has antitumor activity with low toxicity[1].
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DCAPI1593 Rupatadine Featured
Rupatadine is a dual histamine H1 and PAF antagonist
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DC7985 RU 24969 hemisuccinate Featured
RU 24969 hemisuccinate is a potent SR-1A/SR-1B and moderate SR-2C agonist that may also release serotonin.
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DCAPI1434 Romidepsin(FK-228) Featured
Romidepsin strongly inhibits HDAC1 and HDAC2 with IC50 of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC50 25 nM and 790 nM, respectively.
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DC11325 RN-1734 Featured
RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.
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DC7268 Risperidone(R 64 766)
Risperidone(R 64 766) is a serotonin 5-HT2 receptor blocker(Ki= 0.16 nM) and a potent dopamine D2 receptor antagonist(Ki= 1.4 nM).
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DC8876 Rimonabant(SR141716) Featured
Rimonabant(SR141716) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
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DC9383 Rimonabant (Hydrochloride) Featured
Rimonabant Hcl(SR141716A) is a selective central cannabinoid (CB1) receptor inverse agonist with Ki of 1.8 nM.
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DC11392 SEC inhibitor KL-2 Featured
SEC inhibitor KL-2 is a peptidomimetic inhibitor of super elongation complex (SEC) and transcription elongation by Pol II, disrupts cyclin T1-AFF4 interaction (Ki=1.50 uM) within SEC; disrupts the interaction between the SEC scaffolding protein AFF4 and P
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DC8191 Sparsentan(PS433540) Featured
Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively[1].
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DC22635 SPDP Featured
SPDP (SPDP Crosslinker) is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. It is a glutathione cleavable ADC linker u
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DC80060 p-Tolyl-β-D-glucuronide Featured
p-Cresol glucuronide is a metabolite of p-cresol, a uremic toxin formed by bacterial fermentation of proteins in the large intestine. It is formed from p-cresol primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A6, but also by UGT1A9, in huma
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DC44535 PF-05221304(Clesacostat) Featured
PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polyp
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DC34338 Pyrintegrin Featured
Pyrintegrin is a cell-permeable promoter of the adhesion of individually dissociated hESCs on matrigel- or laminin-, but not gelatin-coated surfaces, substantially reducing trypsinization-induced apoptosis.
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DC28735 PK150 Featured
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus
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