9月
α-Glucosidase-IN-34；化合物 α-Glucosidase-IN-34α-Glucosidase-IN-34 (2024/9/14)
簡介：α-glucosidase-in-34 (compound 7f) is a potent inhibitor of α-glucosidase, exhibiting an ic50 of 2.90 μm, and is applicable in research related to type 2 diabetes and hyperglycemia [1].
α-Glucosidase-IN-33；化合物 α-Glucosidase-IN-33α-Glucosidase-IN-33 (2024/9/14)
簡介：α-glucosidase-in-33 (compound 7c), with an ic50 of 2.39 μm, is a potent inhibitor of α-glucosidase and is relevant in research on type 2 diabetes and hyperglycemia [1].
HSP90-IN-25；化合物 HSP90-IN-25HSP90-IN-25 (2024/9/14)
簡介：hsp90-in-25 (compound 4a) is an inhibitor targeting hsp90, specifically impeding its atpase function [1].
EGFR-IN-86；化合物 EGFR-IN-86EGFR-IN-86 (2024/9/14)
簡介：egfr-in-86 (compound 4i), an egfr inhibitor (ic50: 1.5 nm), demonstrates potent activity against glioblastoma by inducing apoptosis and causing g2/m phase cell cycle arrest in u87 cells [1].
HDAC8-IN-5；化合物 HDAC8-IN-5HDAC8-IN-5 (2024/9/14)
簡介：hdac8-in-5 (compound 6a), with an inhibitory concentration (ic50) of 28 nm, is a potent hdac8 inhibitor suitable for cancer research [1].
MAO-B-IN-24；化合物 MAO-B-IN-24MAO-B-IN-24 (2024/9/14)
簡介：mao-b-in-24 (compound 11h) is a selective, reversible, competitive inhibitor of mao-b with an ic50 value of 1.60 μm. it also exhibits inhibitory effects on mao-a with an ic50 of 22.42 μm. at a concentration of 10 μm, mao-b-in-24 reduces the activities of ache and bche to 54.58% and 88.43%, respectively [1].
Nidufexor；化合物NidufexorNidufexor (2024/9/14)
簡介：nidufexor is an agonist for the farnesoid x receptor (fxr).
MAO-B-IN-23；化合物 MAO-B-IN-23MAO-B-IN-23 (2024/9/14)
簡介：mao-b-in-23, also known as compound 11f, is a reversible and competitive monoamine oxidase b (mao-b) inhibitor with an ic50 value of 1.44 μm and a ki of 0.51 μm [1].
cGAS-IN-1；化合物 cGAS-IN-1cGAS-IN-1 (2024/9/14)
簡介：cgas-in-1 (compound c20), a flavonoid that acts as a cyclic gmp-amp synthase (cgas) inhibitor, demonstrates ic50 values of 2.28 μm for human cgas and 1.44 μm for mouse cgas. by inhibiting the abnormal activation of cgas linked to numerous immune-mediated inflammatory diseases, cgas-in-1 possesses potential anti-inflammatory properties [1].
SIRT5 inhibitor 9；化合物 SIRT5 inhibitor 9SIRT5 inhibitor 9 (2024/9/14)
簡介：sirt5 inhibitor 9 (compound 14), with an ic50 of 4.07 μm, is a competitive inhibitor of the sirtuin sirt5, exhibiting potential anticancer properties [1].
SIRT5 inhibitor 8；化合物 SIRT5 inhibitor 8SIRT5 inhibitor 8 (2024/9/14)
簡介：sirt5 inhibitor 8 (compound 10) serves as a competitive inhibitor of sirtuin sirt5, exhibiting an ic50 of 5.38 μm, and possesses anticancer potential [1].
Anticancer agent 157；化合物 Anticancer agent 157Anticancer agent 157 (2024/9/14)
簡介：anticancer agent 157 (compound 15) is a nitric oxide (no) inhibitor with ic50 values of 0.62 μg/ml, exhibiting both anti-inflammatory and anticancer effects. it interacts with inducible no synthase (inos) and caspase 8, which facilitates apoptosis through nuclear fragmentation and chromatin condensation. additionally, anticancer agent 157 effectively inhibits ht29 colon cancer cells (ic50 =2.45 μg/ml), hep-g2 liver cancer cells (ic50 =3.25 μg/ml), and b16-f10 murine melanoma cells (ic50 =3.84 μg
WK499；化合物 WK499WK499 (2024/9/14)
簡介：bcl6-in-10 (compound wk499) is an inhibitor of bcl6, disrupting its interaction with the smrt protein and promoting apoptosis, cell cycle arrest, and dna damage. it effectively hampers the proliferation of various aml cell lines, with ic50 values of 0.91, 1.63, 1.026, 7.42, 0.87, and 0.85μm for oci-aml3, thp1, molm13, hl60, kg1, and nb4 cells, respectively [1].
PI3K-IN-47；化合物 PI3K-IN-47PI3K-IN-47 (2024/9/14)
簡介：pi3k-in-47 (compound 27) is a potent bivalent inhibitor targeting the phosphoinositide 3-kinases (pi3k) family, exhibiting inhibitory concentration (ic50) values of 0.44 nm for pi3kα, and 7.18 nm, 13.92 nm, 22.83 nm for pi3kβ, pi3kγ, and pi3kδ respectively. it is effective in inducing g1 phase cell cycle arrest, and exhibits anti-neoplastic properties by restraining colony formation and cell migration. additionally, pi3k-in-47 has demonstrated the ability to suppress tumor growth in hgc-27 xenog
HPK1-IN-39；化合物 HPK1-IN-39HPK1-IN-39 (2024/9/14)
簡介：hpk1-in-39 (compound 10n), a selective inhibitor of hematopoietic progenitor kinase 1 (hpk1) with an inhibitory concentration (ic50) of 29 nm, impedes the phosphorylation of slp76. this compound is applicable in the research of cancer immunotherapy [1].
BRD4 Inhibitor-28；化合物 BRD4 Inhibitor-28BRD4 Inhibitor-28 (2024/9/14)
簡介：brd4 inhibitor-28 (compound 18), an orally active molecule, selectively inhibits the bromodomains of brd4 (brd4-bd1 and brd4-bd2) with ic50 values of 15 and 55 nm, respectively. it also demonstrates inhibition of brd2-bd1, brd3-bd1, and brdt-bd1 with ic50 values of 19, 25, and 68 nm, respectively. furthermore, this compound exhibits anti-melanoma activity [1].
EGFR/BRAFV600E-IN-3；化合物 EGFR/BRAFV600E-IN-3EGFR/BRAFV600E-IN-3 (2024/9/14)
簡介：egfr/brafv600e-in-3 is an inhibitor targeting egfr, brafv600e, and egfrt790m with ic50 values of 57 nm, 68 nm, and 9.70 nm, respectively. it induces apoptosis and exhibits promising antioxidant activity [1].
Afuresertib hydrochloride化合物Afuresertib hydrochlorideAfuresertib|||PKC|||Protein kinase C (2024/9/14)
簡介：afuresertib hydrochloride is an inhibitor of akt kinase (kis of 0.08/2/2.6 nm for akt1/akt2/akt3 respectively)
EGFR/BRAFV600E-IN-2；化合物 EGFR/BRAFV600E-IN-2EGFR/BRAFV600E-IN-2 (2024/9/14)
簡介：e07 aptamer, targeting the human epidermal growth factor receptor (hegfr), competes with epidermal growth factor (egf) for binding to a unique epitope on egfr. this aptamer not only binds to egfr-expressing cells but also inhibits receptor autophosphorylation and thwarts tumor cell proliferation in three-dimensional matrices, positioning it as a useful tool for tumor disease research [1].
MAO-IN-3；化合物 MAO-IN-3MAO-IN-3 (2024/9/14)
簡介：mao-in-3 (compound 5), a reversible and competitive monoamine oxidase (mao) inhibitor with inhibition constants (k i) of 0.6 μm for mao a and 0.2 μm for mao b, effectively suppresses ln-229 glioblastoma cell proliferation, as denoted by an inhibitory concentration (ic50) of 0.8 μm. this compound holds potential application in cancer research [1].
BC-05；化合物 BC-05BC-05 (2024/9/14)
簡介：bc-05, an orally active inhibitor targeting cd13 and the proteasome, displays potent inhibition with ic50 values of 0.13 μm against human cd13 and 1.39 μm for the 20s proteasome. it is utilized in the research of multiple myeloma [1].
EP12；化合物 EP12EP12 (2024/9/14)
簡介：ep12, a c-myc inhibitor and g4 stabilizer, induces apoptosis and dna damage in multiple myeloma cells while obstructing p65/p50 nuclear translocation by disrupting the nf-κb signaling pathway, effectively inhibiting multiple myeloma growth [1].
FGFR1/VEGFR2-IN-1；化合物 FGFR1/VEGFR2-IN-1FGFR1/VEGFR2-IN-1 (2024/9/14)
簡介：fgfr1/vegfr2-in-1 (compound 2b) is an inhibitor of both fgfr1 and vegfr2, applicable in cancer research [1].
MET/PDGFRA-IN-2；化合物 MET/PDGFRA-IN-2MET/PDGFRA-IN-2 (2024/9/14)
簡介：met/pdgfra-in-2 (compound 8h) serves as an inhibitor of met and pdgfra proteins, promoting apoptosis in cells and impeding the proliferation of met-positive cells with ic50 values of 9.7, 6.1, 12.0, 11.5, 8.6, and 34.4 μm for aspc-1, ebc-1, mkn-45, mia-paca-2, ht-29, and k562 cells, respectively [1].
MET/PDGFRA-IN-1；化合物 MET/PDGFRA-IN-1MET/PDGFRA-IN-1 (2024/9/14)
簡介：met/pdgfra-in-1 (compound 8c) serves as an inhibitor of met and pdgfra proteins, displaying an ic50 of 36 μm against met. it impedes met phosphorylation, thereby promoting apoptosis, and curtails the proliferation of various met-positive cell lines, with ic50 values of 15.3 μm for aspc-1, 19.0 μm for ebc-1, 22.0 μm for mkn-45, 25.6 μm for mia-paca-2, 21.0 μm for ht-29, and 31.5 μm for k562 [1].
α-Synuclein inhibitor 9；化合物 α-Synuclein inhibitor 9α-Synuclein inhibitor 9 (2024/9/14)
簡介：α-synuclein inhibitor 9 (compound 20c) is a molecule that targets and binds to cavities within mature α-synuclein fibrils, diminishing their β-sheet content. it effectively inhibits the aggregation of a53t α-synuclein and exhibits neuroprotective properties, enhancing brain functionality and alleviating motor impairments. this compound is utilized in research related to parkinson´s disease (pd). [1]
Nrf2-IN-3；化合物 Nrf2-IN-3Nrf2-IN-3 (2024/9/14)
簡介：nrf2-in-3 (compound r16), a nrf2 inhibitor, binds to keap1 mutants (g333c mkeap1) thereby restoring the impaired keap1/nrf2 interactions. this restoration sensitizes keap1-mutant cancer cells to chemotherapeutic agents, such as cisplatin and gefitinib, by reestablishing the functionality of the mkeap1/nrf2 complex [1].
Carbonic anhydrase inhibitor 15；化合物 Carbonic anhydrase inhibitor 15Carbonic anhydrase inhibitor 15 (2024/9/14)
簡介：carbonic anhydrase inhibitor 15 (compound 8), with an inhibitory constant (k_i) of 8.5 nm for hca ii, exhibits analgesic effects [1].
NS 1738；化合物NS 1738NSC 213859；NSC 213859 (2024/9/14)
簡介：ns 1738 (nsc-213859) is a positive allosteric modulator of the α7-containing neuronal nicotinic acetylcholine receptors (nachrs)
HDAC6-IN-19；化合物 HDAC6-IN-19HDAC6-IN-19 (2024/9/14)
簡介：hdac6-in-19 (compound 14g), an hdac6 inhibitor with an ic50 of 2.68 nm, additionally inhibits hdac1, hdac2, and hdac3, with ic50 values of 61.6 nm, 98.7 nm, and 103 nm, respectively. this compound effectively suppresses the proliferation of various cancer cell lines, such as leukemia, colon cancer, melanoma, and breast cancer [1].
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