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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
23 Results for "
HTRF assay
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "HTRF assay" in MCE Product Catalog:
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4 Cited Publications
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CSK-IN-1 (compound 13) is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. CSK-IN-1 shows the ability to increase T cell proliferation induced by T cell receptor signaling .
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TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis .
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1 Cited Publications
Cat. No.: HY-121667
CAS No.: 777857-56-4
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Scaff10-8 is a RhoA inhibitor. Scaff10-8 binds to RhoA, inhibits AKAP-Lbc-mediated RhoA activation. Scaff10-8 can be used for research on diabetes insipidus and bipolar disorder .
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BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
Cat. No.: HY-162275
CAS No.: 861224-48-8
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JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
Cat. No.: HY-16999
CAS No.: 1309684-94-3
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RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
Cat. No.: HY-120647
CAS No.: 2113650-03-4
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BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
Cat. No.: HY-158685
CAS No.: 2360561-90-4
RG7112D is a potent MDM2 inhibitor with IC50s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC50=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .
Cat. No.: HY-12577
CAS No.: 1498300-31-4
TNKS1/2-IN-1 (Example 4) is a TNKS1 and TNKS2 inhibitor, with pIC50 values of 8.2 or 7.3 against TNKS1, and 7.1 or 7.7 against TNKS2. TNKS1/2-IN-1 inhibits the enzymatic activities of TNKS1 and TNKS2. TNKS1/2-IN-1 is applicable for cancer research .
Cat. No.: HY-179414
CAS No.: 3102130-17-3
KRAS G12D-IN-34 (Compound 13) is a KRAS (G12D) inhibitor with IC50 values for KRAS (G12D) and KRAS (WT) of 1.05 nM and 1.59 μM respectively. KRAS G12D-IN-34 can be used for research on non-small cell lung cancer .
Cat. No.: HY-169908
CAS No.: 3055844-98-6
STAT3-IN-37 (Compound 101) is the inhibitor for STAT3 with an IC50 of 15 nM (measuring by DNA-HTRF assay) or 2 nM (measuring by human whole blood SOCS3 qPCR assay) .
Cat. No.: HY-179180
CAS No.: 2891831-40-4
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PD-1/PD-L1-IN-59 (Compound MZ51) is a PD-1/PD-L1 inhibitor with an IC50 of 183 nM. PD-1/PD-L1-IN-59 can be used for the study of triple-negative breast cancer (TNBC) .
Cat. No.: HY-168582
CAS No.: 3058278-46-6
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IL-17-IN-2 (Example 51) is a potent inhibitor of IL-17, with the IC50 of < 0.4 μM in HTRF and NHK assay .
Cat. No.: HY-142743
CAS No.: 2223014-57-9
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Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC50s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer .
Cat. No.: HY-120879
CAS No.: 1609258-91-4
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PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a Ki of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC50 of 568 nM in HTRF assay .
Cat. No.: HY-157055
CAS No.: 2413100-40-8
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PD-1-IN-25 (compound 43) is a potent PD-1/PD-L1 interaction inhibitor with an IC50 value of 10.2 nM in the HTRF assay. PD-1-IN-25 can promote CD8+ T cell activation through inhibiting PD-1/PD-L1 cellular signaling. PD-1-IN-25 delays the tumor growth .
Cat. No.: HY-160733
CAS No.: 2879330-24-0
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Menin-MLL-IN-32 (compound 51) is a Menin-MLL interaction inhibitor with an IC50 of 0.042 nM in HTRF assay. Menin-MLL-IN-32 inhibits MEIS1 mRNA expression with an IC50 of 11 nM. Menin-MLL-IN-32 shows anti-proliferative effects, with IC50 values of 8 nM, 24 nM and 1900 nM for MOLM14 cells, OCI-AML3 cells and KO-52 cells, respectively. Menin-MLL-IN-32 can be used for the study of leukemia .
Cat. No.: HY-183439
CAS No.: 2365116-48-7
dTAG-Fluorescein is a fluorescent acceptor probe and heterobifunctional proteolysis targeting chimeric molecule (PROTAC) .dTAG-Fluorescein functions in Homogeneous Time Resolved Fluorescence (HTRF) competitive displacement binding assays to measure binding affinity to His-FKBP12(F36V) .dTAG-Fluorescein recruits von Hippel-Lindau or CRBN E3 ligase complexes to drive selective degradation of FKBP12 F36V-tagged proteins, with limited activity towards FKBP12 WT and IKZF1 .
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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
