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Results for "

HTRF

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Autophagy (3) c-Myc (1) Dopamine Receptor (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (3) Histone Demethylase (1) Histone Methyltransferase (1) HuR (1) Interleukin Related (2) LAG-3 (1) MAP4K (1) MDM-2/p53 (3) Molecular Glues (1) p38 MAPK (1) PAK (1) PARP (1) PD-1/PD-L1 (5) PROTACs (1) Ras (1) Src (1) STAT (2) STING (1) TAM Receptor (1) TNF Receptor (1) WDR5 (1)
By Research Areas:	Cancer (24) Inflammation/Immunology (10) Neurological Disease (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134471

TNF-α-IN-2 1 Publications Verification	TNF Receptor	Inflammation/Immunology Cancer
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 .

HY-162664

STING antagonist-1	STING	Inflammation/Immunology
STING antagonist-1 is an antagonist of STING with an IC₅₀ of 3.8 nM. STING antagonist-1 can be used in the research of autoimmune diseases, inflammatory diseases, and others .

HY-130254

CSK-IN-1 3 Publications Verification	Src	Inflammation/Immunology Cancer
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 .

HY-18874

p38-α MAPK-IN-1 2 Publications Verification	p38 MAPK Autophagy	Others
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC₅₀ of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay .

HY-120635

BMS-1001 hydrochloride	PD-1/PD-L1	Inflammation/Immunology Cancer
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 .

HY-162275

JMJD1C-IN-1	Histone Demethylase Histone Methyltransferase STAT	Cancer
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC₅₀ = 0.59 μM, K_d = 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 .

HY-163759

HuR degrader 2	Molecular Glues HuR	Cancer
HuR degrader 2 (Compound 3) is a molecule glue, which targets RNA-binding protein Hu antigen R (HuR) and degrades 30% HuR at 0.1 μM. HuR degrader 2 inhibits the proliferation of cancer cell Colo-205, with IC₅₀≤200 nM. HuR degrader 2 exhibits a high affinity with cereblon, with an HTRF ratio < 0.02 .

HY-16999

RO8994	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
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 .

HY-153728

WM-586 1 Publications Verification	WDR5	Cancer
WM-586 is a covalent WDR5 inhibitor. WM-586 specifically decreases WDR5 and MYC interaction with an IC₅₀ of 101 nM. WM-586 is used in research on a variety of cancers including neuroblastoma, breast cancer, bladder cancer and colorectal cancer .

HY-158685

RG7112D	MDM-2/p53	Cancer
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 .

HY-120647

BMS-1001	PD-1/PD-L1	Inflammation/Immunology Cancer
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 .

HY-12577

TNKS1/2-IN-1	PARP	Cancer
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 .

HY-179414

KRAS G12D-IN-34	Ras	Cancer
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 .

HY-169908

STAT3-IN-37	STAT	Cancer
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) .

HY-160585

PD-L1/PD-1-IN-1	PD-1/PD-L1	Inflammation/Immunology Cancer
PD-L1/PD-1-IN-1 (compound 8j) is a potent inhibitor of PD-L1/PD interaction, with IC₅₀ ＜ 1 nM. PD-L1/PD-1-IN-1 plays an important role in anti-tumor research .

HY-155507

c-Myc inhibitor 11	c-Myc	Cancer
c-Myc inhibitor 11 (Compound 67e) is a c-MYC inhibitor (pEC₅₀: 6.4). c-Myc inhibitor 11 has high clearance levels, moderate volume of distribution and short half-life in rat pharmacokinetic assay. c-Myc inhibitor 11 can be used for cancer research .

HY-179180

PD-1/PD-L1-IN-59	PD-1/PD-L1	Cancer
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) .

HY-168582

IL-17-IN-2	Interleukin Related	Inflammation/Immunology
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 .

HY-162544

PROTAC HPK1 Degrader-2	PROTACs MAP4K	Cancer
PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, with the DC₅₀ of 23 nM in human PBMC. PROTAC HPK1 Degrader-2 plays an important role in cancer research .

HY-142743

Y08175	Epigenetic Reader Domain	Cancer
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 .

HY-169306

IL-17A inhibitor 4	Interleukin Related	Inflammation/Immunology
IL-17A inhibitor 4 (Example 449) is a potent IL-17A inhibitor. IL-17A inhibitor 4 inhibits HTRF and NHK cells viability with IC₅₀s of 0.028 and 0.0047 μM, respectively .

HY-120879

PF2562	Dopamine Receptor	Neurological Disease
PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a K_i of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC₅₀ of 568 nM in HTRF assay .

HY-128761

CBP/p300-IN-2	Epigenetic Reader Domain	Cancer
CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC₅₀ values of 1.07 nM and 5.96 nM for CBP/HTRF and Myc, respectively. CBP/EP300-IN-2, example 25, is extracted from patent WO2017205538A1 .

HY-139458

MDM2-IN-21	MDM-2/p53	Cancer
MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer .

HY-162940

MerTK/Axl-IN-1	TAM Receptor	Inflammation/Immunology Cancer
MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC₅₀s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .

HY-157055

PD-1-IN-25	PD-1/PD-L1	Cancer
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 .

HY-160733

Menin-MLL-IN-32	Epigenetic Reader Domain	Cancer
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 .

HY-180900

Z3071585108	LAG-3	Inflammation/Immunology
Z3071585108 is a small molecule binder of the LAG-3 D1 domain with K_d values measured for the MST-TRIC channel and spectral shift detection of 59.2 and 56.1 μM respectively. Z3071585108 partially inhibits the binding of LAG-3 to MHCII, with an EC₅₀ of 42.9 μM. Z3071585108 can be used for the study of small molecule immunotherapies targeting LAG-3 .

HY-183867

ATG5 PPI-IN-6	Autophagy	Others
ATG5 PPI-IN-6 (Compound 17a) is an inhibitor of ATG5 interactions with other proteins, with an IC₅₀ value of 26.92 μM against ATG5-ATG16L1 and 16.34 μM against ATG5-TECAIR. ATG5 PPI-IN-6 inhibits Autophagy in cells .

HY-183838

Autophagy-IN-11	Autophagy	Cancer
Autophagy-IN-11 is an ATG5-targeting autophage inhibitor. Autophagy-IN-11 disrupts protein-protein interactions between ATG5 and ATG16L1, and between ATG5 and TECAIR. Autophagy-IN-11 can be used for cancer research .

HY-111103A

CZh226 hydrochloride	PAK	Cancer
CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC₅₀ of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma .

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HTRF

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