Search Result
Results for "
MM.1S
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-149924
-
|
PROTACs
IAP
|
Cancer
|
CST626 (Compound 9) is a pan-IAP degrader PROTAC. CST626 degrades XIAP, cIAP1 and cIAP2 with DC50s of 0.7, 2.4, and 6.2 nM in MM.1S cells, respectively [1].
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- HY-145322
-
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Casein Kinase
Molecular Glues
|
Cancer
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TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma [1].
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- HY-145321
-
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Phosphodiesterase (PDE)
Molecular Glues
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Cancer
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TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma [1].
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- HY-164099
-
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HDAC
Monoamine Oxidase
Histone Demethylase
|
Cancer
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LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma [1] .
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- HY-161101
-
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PROTACs
IKZF Family
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Cancer
|
MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC50 value of 1.385 nM in MM.1S cells [1].
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- HY-157216
-
|
HDAC
|
Cancer
|
HDAC1 Degrader-1 (compound 1a) is an HDAC1 degrader with anticancer activity. HDAC1 Degrader-1 significantly reduces HDAC1 levels in MM.1S multiple myeloma cells [1].
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- HY-172430S
-
|
TNF Receptor
|
Cancer
|
Epaldeudomide (Compound A406) is the inhibitor for TNF-α (>50% inhibition rate at 100 nM). Epaldeudomide inhibits the proliferation of cancer cells MM.1S (IC50 < 300 nM), WSU-DLCL-2 (IC50 < 100 nM) and Rec-1 (IC50 < 100 nM). Epaldeudomide exhibits antineoplastic activity [1].
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- HY-155671
-
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HDAC
|
Cancer
|
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitory activity in RPMI8266, U266 and MM.1S cells with IC50 values of 0.17, 0.7 and 0.42 μM, respectively [1].
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- HY-144763
-
|
Apoptosis
|
Cancer
|
XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research [1].
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- HY-172159
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HDAC
Apoptosis
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Cancer
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FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) [1].
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- HY-132857A
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PROTACs
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Neurological Disease
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ZXH-4-130 TFA is a highly potent and selective degrader of CRBN. ZXH-4-130 is a CRBN-VHL compound (hetero-PROTAC). ZXH-4-130 TFA induces ~80% CRBN degradation at 10 nM in MM1.S cells [1].
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- HY-145667
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Biotin-JQ1
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Epigenetic Reader Domain
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Cancer
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Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with high affinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM [1].
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- HY-115445
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LCS-1
1 Publications Verification
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Apoptosis
SOD
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Cancer
|
LCS-1 is a superoxide dismutase 1 (SOD1) inhibitor. LCS-1 inhibits SOD1 activity with an IC50 value of 1.07 μM. LCS-1 induces the early- and late-stage apoptosis of multiple myeloma (MM.1S) cells [1] .
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- HY-159964
-
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Deubiquitinase
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Cancer
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USP7-IN-16 (Compound 61) is a selective USP7 inhibitor with IC50 values of 5.5 nM in the FLINT assay and 2.1 nM in MM.1S cells. USP7-IN-16 exhibits antitumor activity in mice and is a promising candidate for research in the field of oncology [1].
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- HY-144369
-
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Proteasome
|
Cancer
|
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research [1].
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- HY-125051
-
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JAK
FLT3
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Cancer
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SG3-179 is a potent inhibitor against the BET bromodomain proteins. SG3-179 is also a JAK2 and FLT3 inhibitor. SG3-179 causes a rapid reduction in HOXB13 protein expression. SG3-179 is promising for research of multiple myeloma (MM1.S) [1] .
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-
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- HY-132998
-
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PROTACs
HDAC
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Cancer
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HDAC6 degrader-1 (Compound NP8) is the PROTAC degrader for HDAC6 with a DC50 of 3.8 nM in cell MM.1S [1].(Blue: ligand for E3 ligase Pomalidomide (HY-10984); Black: linker (HY-140213); Pink: ligand for target protein Nexturastat A (HY-16699))
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- HY-173315
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Epigenetic Reader Domain
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Cancer
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pan-BET/BD2-IN-1 (compound 6b) is a selective extra-terminal (BET) protein inhibitor (BRDT-1 Ki = 1.05 μM and BRD4-1 Ki = 0.68 μM). pan-BET/BD2-IN-1 inhibits MM.1S cancer cell growth with an IC50 of 2.6 μM [1].
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- HY-102047
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Histone Demethylase
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Cancer
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KDOAM-25 is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells [1].
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- HY-102047A
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Histone Demethylase
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Cancer
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KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells [1].
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- HY-102047B
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Histone Demethylase
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Cancer
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KDOAM-25 citrate is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 71 nM, 19 nM, 69 nM, 69 nM for KDM5A, KDM5B, KDM5C, KDM5D, respectively. KDOAM-25 citrate increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells [1].
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- HY-161250
-
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PROTACs
|
Cancer
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Pomalidomide-NH-PEG6-amide-C2-CPI-1612 (compound 22 (dCE-1)) is a CBP/EP300 degrader, which contains a CRBN ligands Pomalidomide, a 24-atom linker with 6 PEG units and a HAT inhibitor CPI-1612. Pomalidomide-NH-PEG6-amide-C2-CPI-1612 exhibits antiproliferative effects in cells multiple myeloma cells LP1 (with a DC50 of 1.2 μM), MM1S and various cancer cell lines, especially the leukemia cells [1].
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- HY-172360
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-
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- HY-172369
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-
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- HY-172359
-
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PROTACs
HDAC
|
Cancer
|
PROTAC HDAC6 degrader 4 (Compound 17c) is the PROTAC degrader for HDAC6 with a DC50 of 14 nM. PROTAC HDAC6 degrader 4 exhibits inhibitory activit against HDAC1, HDAC2, HDAC3 and HDAC6 with IC50s of 2.2, 2.37, 0.61 and 0.295 μM, respectively [1]. (Pink: ligand for target protein HDAC6 ligand-3 (HY-172360); Black: linker (HY-138387); Blue: ligand for cereblon E3 ligase (HY-W093272))
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- HY-172368
-
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PROTACs
Histone Methyltransferase
IKZF Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research [1]. (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
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-
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- HY-160502
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PROTACs
|
Cancer
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CST967 (Compound 17) is a USP7 PROTAC degrader, and increasing the PROTAC concentration can enhance the degradation rate of USP7. CST967 can be used in cancer research [1].
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- HY-149930
-
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JNK
Apoptosis
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Cancer
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YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner [1].
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- HY-168863
-
|
PROTACs
HDAC
Apoptosis
|
Cancer
|
FF2049 is a selective HDAC PROTAC degrader (DC50 = 257 nM for HDAC1). FF2049 promotes ubiquitination and degradation of HDAC. FF2049 promotes Apoptosis. FF2049 can be used for the research of hematological and solid cancer (Pink: POI ligand 1 (HY-168864); Blue: E3 ligase FEM1B ligand (HY-168865)) [1].
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- HY-153226
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-
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- HY-168864
-
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Ligands for Target Protein for PROTAC
HDAC
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Cancer
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POI ligand 1 is a template for the non-selective HDAC inhibitor Vorinostat (HY-10221). POI ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC HDAC degraders with antitumor activity. POI ligand 1 can be used for the synthesis of FF2049 (HY-168863) [1].
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- HY-143715
-
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Ligands for E3 Ligase
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Cancer
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Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
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- HY-173266
-
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PROTACs
HDAC
|
Neurological Disease
Cancer
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TO-1187 is a selective HDAC6 PROTAC degrader (DC50: 5.81 nM). TO-1187 promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors (Pink: HDAC6 ligand (HY-173386); Blue: CRBN ligand (HY-41547); Black: linker (HY-140212)) [1].
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- HY-138691B
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JADA82 dihydrochloride; PCK82 dihydrochloride
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Histone Demethylase
|
Cancer
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JQKD82 (JADA82) dihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 dihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma [1].
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- HY-142704
-
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Epigenetic Reader Domain
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Cancer
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BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC [1].
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- HY-142705
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Epigenetic Reader Domain
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Cancer
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BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC [1].
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- HY-125927
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8-NH2-Ado
|
DNA/RNA Synthesis
Akt
mTOR
Autophagy
Apoptosis
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Cancer
|
8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity [1] .
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-
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- HY-138691A
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JADA82 trihydrochloride; PCK82 trihydrochloride
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Histone Demethylase
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Cancer
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JQKD82 (JADA82) trihydrochloride is a cell-permeable and selective KDM5 inhibitor. JQKD82 trihydrochloride increases H3K4me3 and can be used for the research of multiple myeloma [1].
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- HY-111790
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M3258
1 Publications Verification
|
Proteasome
Apoptosis
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Cancer
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells [1] .
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-
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- HY-138691
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JADA82; PCK82
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Histone Demethylase
|
Cancer
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JQKD82 (JADA82) is a cell-permeable and selective KDM5 inhibitor. JQKD82 increases H3K4me3 and can be used for the research of multiple myeloma [1].
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- HY-171139
-
|
PROTACs
HDAC
|
Cancer
|
PROTAC HDAC6 degrader 2 (Compound 1) is a HDAC6 PROTAC degrader, with IC50 of 0.643 μM. PROTAC HDAC6 degrader 2 promotes ubiquitination and degradation of HDAC6. PROTAC HDAC6 degrader 2 can be used for the research of haematological and solid cancers (Pink: HDAC6 ligand (HY-171141); Blue: E3 ligase CRBN ligand (HY-10984)) [1].
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-
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- HY-145320
-
-
-
- HY-15728
-
IY-5511
|
Bcr-Abl
Apoptosis
STAT
JAK
Prion Protein
|
Infection
Neurological Disease
Cancer
|
Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC50 of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases [1] .
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-
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- HY-105019A
-
Melphalan flufenamide hydrochloride
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells [1] .
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-
-
- HY-105019
-
Melphalan flufenamide
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells [1] .
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-
-
- HY-15473A
-
ML120B dihydrochloride
|
IKK
|
Inflammation/Immunology
Cancer
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis [1] .
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-
-
- HY-163856
-
|
Apoptosis
CDK
|
Cancer
|
CDK7-IN-30 (Compound 22) is a CDK7 inhibitor (IC50 = 7.21 nM) that effectively inhibits the phosphorylation of RNA Polymerase II and CDK2. CDK7-IN-30 CDK7-IN-30 can induce cell apoptosis and has anti-cancer activity and can be used in cancer research [1].
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-
-
- HY-176428
-
|
PROTACs
MNK
Apoptosis
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
PROTAC MNK1 degrader-1 is a selective MNK1 PROTAC degrader with a DC50 of 11.92 nM, and a Dmax > 96% in MV4-11 cells. PROTAC MNK1 degrader-1 significantly reduces p-eIF4E (IC50: 22.07 nM), induces apoptosis, and arrests the cell cycle at the G1 phase. PROTAC MNK1 degrader-1 has potent antitumor activity. PROTAC MNK1 degrader-1 has robust antileukemic efficacy in MV4-11 xenograft mice model with acceptable drug safety [1]. Pink: MNK1 ligand (HY-176429); Blue: CRBN ligase ligand (HY-A0003); Black: linker (HY-Y1139); CRBN + linker: HY-176430
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-
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- HY-13560
-
AVN-944
4 Publications Verification
VX-944
|
Arenavirus
DNA/RNA Synthesis
Apoptosis
Caspase
Bcl-2 Family
|
Infection
Cancer
|
AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research [1] .
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-105019
-
Melphalan flufenamide
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide), a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells [1] .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-172430S
-
|
Epaldeudomide (Compound A406) is the inhibitor for TNF-α (>50% inhibition rate at 100 nM). Epaldeudomide inhibits the proliferation of cancer cells MM.1S (IC50 < 300 nM), WSU-DLCL-2 (IC50 < 100 nM) and Rec-1 (IC50 < 100 nM). Epaldeudomide exhibits antineoplastic activity [1].
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Cat. No. |
Product Name |
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Classification |
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- HY-172360
-
|
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Alkynes
|
HDAC6 ligand-3 is a ligand for HDAC6 that can be used as target protein ligand for synthesis of PROTAC HDAC6 degrader 4 (HY-172359) [1].
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