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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
332 Results for "
specific substrate
" in MedChemExpress (MCE) Product Catalog:
Products (332)
332 Results for "specific substrate" in MCE Product Catalog:
63
Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8 + T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury .
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Lenalidomide hemihydrate (CC-5013 hemihydrate) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide hemihydrate induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide hemihydrate promotes IL-2 release and effector functions of CD8 + T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide hemihydrate can be used in research related to hematological malignancies, acute liver failure and acute kidney injury .
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28 Cited Publications
Cat. No.: HY-D0861A
CAS No.: 13368-13-3
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20 Cited Publications
Research Areas:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer .
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Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM). Butyrolactone 3 can be used in studies of cancer, metabolic, autoimmune and neurological diseases .
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12 Cited Publications
Research Areas:
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
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11 Cited Publications
Synonyms: 4-Iodo-6-phenylpyrimidine
Research Areas:
4-IPP (4-Iodo-6-phenylpyrimidine) is a specific suicide substrate and irreversible inhibitor of macrophage migration inhibitory factor (MIF) .
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11 Cited Publications
Cat. No.: HY-P0019
CAS No.: 66216-78-2
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11 Cited Publications
Cat. No.: HY-P0019A
CAS No.: 2070009-61-7
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7 Cited Publications
Cat. No.: HY-W011391
CAS No.: 67953-08-6
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na +-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na +-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells .
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4 Cited Publications
Synonyms: α-(Methylamino)isobutyric acid
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MeAIB (α-(Methylamino)isobutyric acid) is a specific?substrate for amino acid transport system A (ATA1). ATA mediate the uptake of short-chain neutral amino acids in a Na +-dependent manner .
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4 Cited Publications
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CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
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4 Cited Publications
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CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity .
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4 Cited Publications
Synonyms: NX-5948; BTK-IN-24
Research Areas:
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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3 Cited Publications
Cat. No.: HY-P0136
CAS No.: 125911-68-4
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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
