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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC12200 PACAP (6-38), human, ovine, rat TFA
PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
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DC8716 NU6300
NU6300 is a non-covalent ATP-competitive CDK2 inhibitor (IC50 = 0.16 mM).
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DC10302 N-deacetylated BMS-202
N-deacetylated BMS-202 is the deacetylated of BMS-202. BMS-202 is an inhibitor of the PD-l/PD-Ll interaction, mainly used for cancer treatment.
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DC12172 L-JNKI-1
L-JNKI-1 is a cell-permeable peptide inhibitor specific for JNK.
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DC12095 GRGDSP TFA
GRGDSP (TFA) is an integrin inhibitor.
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DC12343 GNE 220 Hydrochloride
GNE 220 (Hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
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DC12257 Gln-AMS TFA
Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor. Gln-AMS inhibits glutaminyl-tRNA synthetase (GlnRS) with a Ki of 1.32 µM.
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DC20087 GKI-1
GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 µM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 µM, but only weakly affected PKA.
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DC12300 G3-C12 TFA
G3-C12 (TFA) is a galectin-3 binding peptide, with high affinity (Kd) of 88 nM, but shows no affinity for other galectin family members or to other lectins.
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DC12249 E3 ligase Ligand 1 dihydrochloride
E3 ligase Ligand 1 dihydrochloride is a Hippel-Landau (VHL) E3 ligase-binding moiety based on PROTAC technology.
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DC12329 ChX710
ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
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DC20119 Carnostatine (SAN9812)
Carnostatine (SAN9812) is a specific and highly selective carnosinase (CN1) inhibitor with a Ki of 11 nM.
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DC20034 Boc-MLF TFA
Boc-MLF (TFA) is a peptide, used as a specific formyl peptide receptor (FPR) antagonist, also inhibits the signaling through formyl peptide receptor like 1 (FPRL1) at higher concentrations.
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DC20114 ATWLPPR Peptide TFA
ATWLPPR Peptide TFA, a heptapeptide, acts as a selective neuropilin-1 inhibitor, inhibits VEGF165 binding to NRP-1, used in the research of angiogenesis. ATWLPPR Peptide TFA has potential in reducing the early retinal damage caused by diabetes.
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DC12067 4'-Methylchrysoeriol
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
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DC10428 (1S,3R,5R)-PIM447 dihydrochloride
(1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
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DC39041 BMS 247616 (S1 antitumor agent) Featured
S-1 is a novel oral fluorouracil antitumor drug that combines three pharmacological agents: tegafur (FT), a prodrug of 5-fluorouracil (5-FU); 5-chloro-2,4-dihydroxypyridine (CDHP), an inhibitor of dihydropyrimidine dehydrogenase, and potassium oxonate (Ox
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DC43941 Ecamsule.2Na
Ecamsule.2Na is the Sodium salt form of Ecamsule. Ecamsule is an active ingredient of sunscreens that protects the skin from sunburn and erythema.
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DC43942 Polidocanol
Polidocanol (Polyoxyethylene lauryl ether, Polyoxyethyleneglycol Dodecyl Ether, Brij30, Laureth-23, Varithena) is a sclerosant used for treating uncomplicated spider veins and reticular veins in the lower extremities.
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DC43977 L-Palmitoylcarnitine TFA
L-Palmitoylcarnitine TFA, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia.
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DC43988 GW806742X hydrochloride
GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochlorid
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DC43996 NAZ2329
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 bind
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DC43997 Epsilon-V1-2
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
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DC70212 ASH1L inhibitor AS-99
ASH1L inhibitor AS-99 (AS-99) is a first-in-class, potent, selective inhibitor of ASH1L histone methyltransferase with IC50 of 0.79 uM.AS-99 strongly bind to the ASH1L SET domain with Kd values of 0.89 uM.AS-99 displayed no significant inhibition (>100-fold selectivity) at 50 uM against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2.AS-99 inhibits the growth of leukemia cells (MV4;11, MOLM13, and KOPN8) harboring different MLL1 translocations with the GI50 values of 1.8-3.6 uM, showed a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, without toxicity in normal cells.AS-99 impairs transcriptional program of MLL fusion proteins and reduces leukemia burden.AS-99 reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
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DC47225 AS-99 TFA
AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.
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DC47935 NJH-2-057
NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a drug used to treat cystic fibrosis that binds ΔF508-CFTR.
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DC71755 Sipagladenant Featured
Sipagladenant (Compound I) is an orally active adenosine receptor A2A inverse agonist. Sipagladenant can be used in frontal lobe dysfunction research.
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DC74523 XY-07-35 Featured
XY-07-35 is a potent, selective HDAC6 proteolysis targeting chimera (PROTAC) degrader with IC50 of 48.5 nM.
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DC43769 2OH-BNPP1 Featured
2OH-BNPP1 is an inhibitor of BUB1 kinase, a Ser/Thr kinase, used for the treatment of cancer.
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DC47754 Disitamab vedotin Featured
Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent monomethyl auristatin E. Disitamab vedotin enhances antitumor immunity.
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