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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC77837 RMC5127
RMC5127 is a first-in-class, orally bioavailable mutant-selective tri-complex inhibitor of the GTP-bound (ON) form of RASG12V. It non-covalently binds to cyclophilin A (CypA), forming a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex, sterically inhibiting RAS binding. It inhibits the RAS pathway in KRASG12V-mutant cancer cells, reducing proliferation, inducing apoptosis, and showing strong potential for use in RASG12V-mutated cancer research.
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DC77836 TNG348
TNG348 is an orally bioavailable allosteric inhibitor targeting the ubiquitin-specific protease USP1. It selectively and potently blocks USP1 activity, preventing deubiquitination of proliferative PCNA and FANCD2, which disrupts DNA repair mechanisms. TNG348 demonstrates inhibitory effects against BRCA1/2-mutated and homologous recombination-deficient (HRD) breast and ovarian cancers .
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DC77835 BI033
BI033 is a selective inhibitor of BTB and CNC homology 1 (BACH1) specifically binds to BACH1's N-terminal with a Kd of 9.0 uM. It disrupts the BACH1–HDAC1 interaction, enhances H3K27 acetylation at BACH1 target genes, and upregulates angiogenic genes, suggesting its therapeutic potential for myocardial infarction and ischemic vascular disease.
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DC77834 Peptide 4
Peptide 4 is a complex synthetic peptide molecule commonly used as a research chemical or therapeutic agent due to its potential to mimic biological peptides and modulate specific molecular targets.
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DC77833 CT1113
CT1113 is a potent dual inhibitor of USP25 and USP28 that effectively reduces c-MYC levels and exhibits strong anti-tumor activity. It can be used in research on colon and pancreatic cancers.
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DC77832 Taurolithocholic acid
Taurolithocholic acid is a taurine-conjugated tertiary bile acid. It induces apoptosis in hepatoma cell lines via caspase-3/7 activation and serves as a model to study the endocrine and metabolic roles of bile acids in enterohepatic circulation and liver physiology.
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DC77831 Vicadrostat
Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.
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DC77830 PB94
PB94 is a potent and selective inhibitor of HDAC11 with an IC50 of 108 nM and exhibits >40-fold selectivity over other HDAC isoforms. It ameliorates neuropathic pain in mouse models and can be radiolabeled with carbon-11 as [¹¹C]this compound for PET imaging, demonstrating significant brain uptake and potential for in vivo imaging applications.
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DC77829 SKLB-11A
SKLB-11A is a selective, first-in-class allosteric activator of SIRT3 that binds with a Kd of 4.7 μM and enhances its deacetylase activity with EC50 of 21.95 μM. It improves cardiac function and alleviates myocardial damage in vivo.
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DC77828 BIEGi-1
BIEGi-1 is a potent and selective binary inhibitor of EGFR that effectively blocks EGFR-catalyzed nucleotide exchange and disrupts the EGFR–Rheb interaction. It robustly inhibits both EGFR kinase activity and mTORC1 signaling in EGFR-mutant cancer cells. This compound exhibits significant anti-proliferative effects with an IC50 of 17 nM for PC9 and 20 nM for HCC827.
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DC77827 BSJ-5-63
BSJ-5-63 is a potent PROTAC degrader of CDK12, CDK7, CDK9. BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K, while also suppressing the mRNA expression of BRCA1 and BRCA2. BSJ-5-63 demonstrates anticancer properties and has the potential for the research of prostate cancer.
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DC75934 (-)-Luteoskyrin
(-)-Luteoskyrin has a wide range of antibacterial activity, such as against malaria (with an IC50 of 0.51 μg/mL), tuberculosis (MIC of 6.25 μg/mL), and it also shows antibacterial effects (with MIC for Gram-positive bacteria ranging from 0.39 to 1.56 μg/mL, and for Gram-negative bacteria from 3.13 to 12.50 μg/mL), as well as antifungal activity (with MIC against plant pathogens ranging from 3.13 to 50μg/mL). (-)-Luteoskyrin exhibits cytotoxicity against NCI-H187 cells, with an IC50 range of 0.16–17.99 μg/mL.
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DC40420 ARCC-4 Featured
ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
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DC26122 Pomalidomide-C2-NH2 hydrochloride Featured
Pomalidomide-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
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DC11573 E3 Ligand-Linker Conjugate 7 Featured
An E3 ligase ligand-linker conjugate for PROTAC..
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DC42552 Pomalidomide-PEG2-azide Featured
Pomalidomide-PEG2-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
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DC21962 TL13-12 Featured
TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide.
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DC21893 dBET57 Featured
dBET57 is a novel BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2..
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DC40447 N-piperidine Ibrutinib hydrochloride Featured
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.
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DC40428 Pomalidomide 4'-alkylC5-acid Featured
Pomalidomide 4'-alkylC5-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.
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DC42553 Pomalidomide-PEG3-azide Featured
Pomalidomide-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
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DC49083 PROTAC-O4I2 Featured
PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.
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DC44858 Thalidomide-O-C4-COOH Featured
Thalidomide-O-C4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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DC76881 GK420 Featured
GK420 (AVX420) is a potent inhibitor of cytosolic phospholipase A2α (cPLA2α), with the XI(50) of 0.0016. GK420 inhibits arachidonic acid release with the EC50 of 0.09 μM. GK420 plays an important role in cancer research.
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DC47206 Thalidomide-5-CH2-NH2 hydrochloride Featured
Thalidomide-5-CH2-NH2 (hydrochloride) is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-CH2-NH2 (hydrochloride) can be connected to the ligand for protein by a linker to form PROTACs.
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DC77714 S3226 Featured
S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.
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DC11847 AZD-2716 Featured
AZD2716(AZD-2716) is a novel potent, selective, orally bioavailable sPLA2 inhibitor with excellent plasma sPLA2 inhibition (IC50=0.1 nM).
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DC74167 SC-919 Featured
SC-919 (SC919) is a potent, selective inhibitor of IP6K (Inositol hexakisphosphate kinase) with IC50 of <5.2, <3.8 and 0.65 nM for human IP6K1/2/3, respectively.
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DC22516 Nanvuranlat (JPH203) Featured
JPH203 (KYT-0353) is a potent, selective L-type amino acid transporter 1 (LAT1, SLC7A5) inhibitor with IC50 of 60 nM (leucine uptake inhibition), but not LAT2.
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DC31420 JPH203 dihydrochloride Featured
JPH203, also known as KYT-0353, is a potent and selective LAT1 selective ( L-type amino acid transporter 1) inhibitor. JPH203 can very potently inhibit l-leucine uptake. JPH203 inhibits YD-38 cell growth. JPH203 up-regulated the population of apoptotic Y
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