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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
760 Results for "
Compound 4
" in MedChemExpress (MCE) Product Catalog:
Products (760)
760 Results for "Compound 4" in MCE Product Catalog:
Cat. No.: HY-123599
CAS No.: 1884209-98-6
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IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC50=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target .
Cat. No.: HY-153605
CAS No.: 2222930-49-4
EGFR-IN-77 (Compound 4a) is a selective EGFR T790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFR T790M/L858R, 0.477 μM against EGFR L858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFR L858R/T790M double-mutant non-small cell lung cancer .
Cat. No.: HY-159577
CAS No.: 2896739-91-4
Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine .
Cat. No.: HY-170958
Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
Cat. No.: HY-170977
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JAK1/STAT3-IN-1 (compound 4f) is an anti-AD (atopic dermatitis) agent by inhibiting JAK1/STAT3 signaling pathway. JAK1/STAT3-IN-1 inhibits NO generation with an IC50 of 2.17 μM. JAK1/STAT3-IN-1 improves the skin condition of AD-like mice, reduces inflammatory infiltration, inhibits the expressions of p-JAK1/JAK1 and p-STAT3/STAT3, and mitigates the excessive immune response on Calcipotriol (HY-10001) (MC903)-induced AD-like mice .
Cat. No.: HY-173163
CAS No.: 2811663-45-1
(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) (Compound 4a) is a Gram-negative outer membrane permeabilizer with synergistic antibacterial activity through the blockage on LptA/LptC interaction via targeting Met47 in LptA. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) potentiates pol B against both wild-typed and MDR A. baumannii and E. coli strains. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) can be used as antibiotic adjuvants against MDR Gram-negative bacteria .
Cat. No.: HY-179504
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PDE4B-IN-6 (compound 4i) is a potent and selective PDE4B inhibitor with an IC50 of 7.42 nM. PDE4B-IN-6 shows ~195- and ~169-fold selectivity for PDE4B over PDE4A (IC50 = 1540 nM) and PDE4C (IC50 = 1260 nM), respectively. PDE4B-IN-6 increases cAMP level and suppresses TNF-α expression. PDE4B-IN-6 shows favorable antioxidant profiles and low cytotoxicity. PDE4B-IN-6 can be used for chronic obstructive pulmonary disease (COPD) research .
Cat. No.: HY-180824
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P38-α MAPK-IN-11 (Compound 4C) is a selective inhibitor of P38α MAPK that can cross the blood-brain barrier with an IC50 value of 43 nM. P38-α MAPK-IN-11 has extremely low inhibitory activity against other MAPK subtypes, namely p38β, p38γ, and p38δ, with IC50 values of > 100 nM, > 100 nM, and 48.6 mM respectively. P38-α MAPK-IN-11 exhibits outstanding neuroprotective effects and anti-neuroinflammatory effects in Alzheimer's disease-like rat models. P38-α MAPK-IN-11 can be used for the study of Alzheimer's disease .
Cat. No.: HY-182275
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PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
Cat. No.: HY-187390
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BRD4 RIMTAC-1 is a BRD4 PROTAC degrader based on the RIPK1-mediated targeted chimera (RIMTAC) technology. It hijacks the endogenous RIPK1-VHL complex via the RIPK1 inhibitor moiety to indirectly recruit the VHL E3 ligase, forming a BRD4-Compound 10-RIPK1-VHL quaternary complex, and degrades BRD4 through the ubiquitin-proteasome system (UPS). BRD4 RIMTAC-1 exhibits selectivity over other BET proteins, induces concentration- and time-dependent, reversible post-translational degradation of BRD4 without altering the target mRNA level. BRD4 RIMTAC-1 potently induces endogenous BRD4 degradation in RAW264.7 and HEK-293T cells, with DC50 values of 179.1 nM and 54.12 nM, respectively. BRD4 RIMTAC-1 can be used for the research of cancer and inflammation-related diseases .
Cat. No.: HY-156096
CAS No.: 3033039-28-7
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HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
Cat. No.: HY-178119
HER4/HER2-IN-1 (Compound 4b) is a HER4/HER2 inhibitor. HER4/HER2-IN-1 inhibits the proliferation of HER2-positive cells. HER4/HER2-IN-1 reduces the total expression level of HER2 in A431 cells, while the phosphorylated HER2 (p-HER2) does not decrease. HER4/HER2-IN-1 lowers the level of cell cycle protein D1 (cyclin D1) and stimulates the cleavage of PARP. HER4/HER2-IN-1 can be used for the study of cancer, such as breast cancer .
Cat. No.: HY-W583350
CAS No.: 847616-84-6
Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) (Compound 4C) is a metal palladium (II) complex. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) exhibits potent anti-proliferative activity against cells such as MDA-MB-231 and HCT116, significantly inducing apoptosis. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) does not directly damage DNA or cause significant cell cycle arrest. Chloro(triphenylphosphine)[2-(2'-amino-1,1'-biphenyl)]palladium(II) can be used in studies on Cisplatin (HY-17394) resistance .
Cat. No.: HY-171591
CAS No.: 2810810-00-3
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SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases .
Cat. No.: HY-174170
CAS No.: 2248444-14-4
(S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide (compound 4) is a STING agonist containing a key amide benzimidazole (ABZI) component and shows reproducible inhibition of 3H-cGAMP binding to STING with an apparent inhibition constant IC50 of 14 μM. (S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide can be used for tumor research .
Cat. No.: HY-179042
CAS No.: 3100351-69-4
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TGF-β/Smad-IN-3 (Compound 4w) is an effective TGF-β/Smad inhibitor. TGF-β/Smad-IN-3 exerts anti-pulmonary fibrosis activity by simultaneously inhibiting the TGF-β/Smad and MAPK signaling pathways. TGF-β/Smad-IN-3 significantly inhibits collagen deposition induced by TGF-β1, with its IC50 value being 3.21 μM. TGF-β/Smad-IN-3 has an IC₅₀ of 46.77 nM for the autocrine motility factor (ATX). TGF-β/Smad-IN-3 significantly reduces the expression levels of α-SMA, COL1A1 and FN in TGF-β1-induced CCC-HPF-1 cells, and effectively inhibited TGF-β1-induced cell migration. TGF-β/Smad-IN-3 can be used for the study of pulmonary fibrosis .
Cat. No.: HY-169412
CAS No.: 2848599-79-9
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MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
Cat. No.: HY-W015777
CAS No.: 105-13-5
Synonyms: P-Methoxy-benzyl alcoho; (4-Methoxyphenyl)methanol
Cat. No.: HY-W015777R
CAS No.: 105-13-5
Synonyms: P-Methoxy-benzyl alcoho (Standard); (4-Methoxyphenyl)methanol (Standard)
Cat. No.: HY-N16980
CAS No.: 2292113-33-6
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
