About 32 results found for searched term "F-CRI1" (0.075 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M20941 | Raloxifene | Estrogen Receptor |
| Keoxifene, Pharoxifene, LY-139481, LY-156758, CCRIS-7129 | ||
| Raloxifene is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. | ||
| M42059 | F-CRI1 | STING |
| F-CRI1 is a potent STING agonist with a Kd value of 40.62 nM. | ||
| M25448 | Dehydrolithocholic acid | ROR |
| 3-Oxo-5β-cholanoic acid | ||
| Dehydrolithocholic acid is a bile acid metabolite, which inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM). | ||
| M1976 | Pomalidomide | Ligand for E3 Ligase |
| Actimid, CC-4047 | ||
| Pomalidomide is the third-generation immunomodulatory agent, functions through interacting with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors. Pomalidomide is a second generation immunomodulator, TNF-α inhibitor with IC50 of 13 nM. | ||
| M2008 | ICG-001 | Wnt/beta-catenin |
| PRI-724 isomer | ||
| ICG-001 is a novel small molecule inhibitor of TCF/beta-catenin-mediated transcription. ICG-001 specifically binds to cyclic AMP response element-binding protein with an IC50 of 3 μM. | ||
| M2027 | Tenovin-1 | p53 |
| Tenovin-1 is a small molecule activator of p53 transcriptional activity. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor. | ||
| M2198 | Curcumin | Histone Acetyltransferase |
| Indian Saffron; Turmeric yellow; Natural Yellow 3; Diferuloylmethane | ||
| Curcumin (Diferuloyl), a natural phenolic compound, is a p300/CREB binding protein specific inhibitor that inhibits histone/non-histone acetylation and histone acetyltransferase-dependent chromatin transcription. Curcumin inhibited NF-κ B and MAPKs, and had anti-inflammatory, antioxidant, anti-proliferation and anti-angiogenesis effects. Curcumin induces Nrf2 protein stabilization through Keap1 cysteine modification. | ||
| M2294 | Brefeldin A | ATPase |
| BFA; Cyanein; Decumbin | ||
| Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity. | ||
| M2350 | (S)-crizotinib | MTH1 |
| (S)-crizotinib, the (S)-enantiomer of crizotinib, is a potent MTH1 (NUDT1) inhibitor with IC50 of 72 nM. | ||
| M2475 | Bucladesine Sodium Salt | PKA |
| Dibutyryl-cAMP sodium salt; DC2797; Sodium dibutyryl cAMP | ||
| Bucladesine, a membrane permeable selective activator of PKA, has a critical role in up-regulation of ChAT and VAChT gene expression in PC12 cells by activation of extracellular signal regulated kinase (ERK) in Ca2+- and PKA-dependent manner. | ||
| M2575 | Dapivirine | Reverse Transcriptase |
| TMC120; R147681 | ||
| Dapivirine is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM. Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations. | ||
| M2786 | JSH-23 | NF-κB |
| Jsh-23 is a NF-κB inhibitor, inhibited NF-κB transcriptional activity in lipopolysaccharid-stimulated macrophages RAW 264.7 with IC50 of 7.1 μM. Jsh-23 inhibited the nuclear translocation of NF-κB P65 without affecting the degradation of IκBα. | ||
| M2896 | OAC1 | Others |
| OAC1 (Oct4-activating compound 1) is a potent Oct4 activator that activates both the Oct4 and Nanog promoters, promotes induced multifunctional stem cell (iPSC) formation, and activates OCT4 through upregulation of HOXB4 expression.Additionally, OAC1 increases the transcription of the Oct4-Nanog-Sox2 triplet and TET1 and promotes cell reprogramming by increasing efficiency and shortening reprogramming time. and TET1 transcription, and may promote cell reprogramming by increasing efficiency and shortening reprogramming time. | ||
| M2980 | Rilpivirine (R278474) | Reverse Transcriptase |
| R278474, TMC278 | ||
| Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). | ||
| M3352 | Lamivudine (BCH-189) | Reverse Transcriptase |
| BCH-189 | ||
| Lamivudine (BCH-189) is an orally active nucleoside reverse transcriptase inhibitor (NRTI) with an IC50 of 2.7 mM. Lamivudine can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus. Lamivudine salicylate can penetrate the CNS. | ||
| M3381 | Nevirapine | Reverse Transcriptase |
| BI-RG 587; NSC 641530; NVP | ||
| Nevirapine (NSC 641530) is a potent, specific non-nucleoside reverse transcriptase inhibitor (NNRTIs) that non-competitively inhibits human immunodeficiency virus type 1 (HIV-1) reverse transcriptase with a Ki of 220 nM. Nevirapine (NSC 641530) can be used in AIDS-related researchs. | ||
| M25394 | BPTF-IN-1 | Epigenetic Reader Domain |
| compound AU1 | ||
| BPTF-IN-1 (compound AU1) is a selective bromodomain and PHD finger containing transcription factor (BPTF) bromodomain inhibitor with a Kd of 2.8 μM. BPTF-IN-1 shows to be selective for BPTF over BRD4 bromodomain. | ||
| M3892 | BMH-21 | DNA/RNA Synthesis |
| BMH-21 is a first-in-class DNA intercalator that binds to high-frequency GC-rich sequences in ribosomal DNA genes and can effectively and rapidly inhibit the transcription of RNA polymerase I (Pol I), leading to degradation of the Pol I catalytic subunit RPA194 and non-phosphorylation of histone H2AX. H2AX is not phosphorylated.BMH-21 has broad and potent antitumor activity in NCI60 cancer cell line and inhibits tumor growth in vivo. | ||
| M4075 | Ginsenoside-Rd | NF-κB |
| Gypenoside VIII | ||
| Ginsenoside Rd inhibited NF-κB transcriptional activity induced by TNFα with IC50 of 12.05±0.82 μM. Ginsenoside Rd inhibited the expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibited CYP2D6, CYP1A2, CYP3A4 and CYP2C9 with IC50 of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM and 85.1±9.1 μM, respectively. | ||
| M4574 | Wedelolactone | Caspase |
| Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11. | ||
| M4717 | Usnic-acid | Antibiotic |
| Usnic acid is a lichen secondary metabolite with a unique dibenzofuran skeleton. Usnic acid has excellent anti-cancer and antibacterial properties. Usnic acid significantly inhibited ranKL-mediated osteoclast formation and function by decreasing transcription and translational expression of NFATc1. | ||
| M5605 | Efavirenz | Reverse Transcriptase |
| Sustiva, Stocrin, DMP-266 | ||
| Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture. | ||
| M6704 | EHT 1864 2HCl | Ras |
| EHT 1864 is a potent inhibitor of Rac family GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. | ||
| M6813 | iCRT 14 | Wnt/beta-catenin |
| iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase. | ||
| M7504 | CIL56 (CA3) | Ferroptosis |
| CIL56 (CA3) is a potent and selective ferroptosis inducer, it has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. | ||
| M8594 | BRD3308 | HDAC |
| BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23 times more selective to HDAC3 than HDAC1 (IC50:1.26 μM) or HDAC2 (IC50:1.34 μM). BRD3308 inhibits pancreatic β cell apoptosis induced by inflammatory cytokines or glucolipid toxic stress and increases functional insulin release. BRD3308 also activates HIV-1 transcription and disrupts HIV-1 latency. | ||
| M8641 | LP117 | Others |
| LP117 is a pirinixic acid derivative that interferes with ATP-binding cassette (ABC) transporter ABCB1-mediated substrates transport, including vincristine, vinorelbine, paclitaxel, and actinomycin D, but not doxorubicin, rhodamine 123, or JC-1. | ||
| M8672 | CeMMEC13 | DNA/RNA Synthesis |
| CeMMEC13 is a potent inhibitor of the second bromodomain of the transcription initiation factor TAF1 with an an IC50 value of 2. | ||
| M8679 | IMR-1 | Notch |
| IMR-1 is a first-in-class, cell-permeable inhibitor of the Notch transcription activation complex, with an IC50 of 26 μM. IMR-1 prevents Maml1 from recruiting to the Notch ternary complex (NTC) in chromatin, inhibits transcription of Notch target genes, and has antitumor activity. | ||
| M8692 | ML385 | Keap1-Nrf2 |
| ML-385 | ||
| ML385 was a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM. ML385 inhibits Nrf2 transcription factor activity by binding to Neh1. | ||
| M8699 | EPI-001 | Androgen Receptor |
| EPI001 | ||
| EPI-001 is a specific inhibitor of the AR (androgen receptor) without inhibiting PR or GR transcriptional activities. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. | ||
| M8767 | MIND4-17 | Others |
| MIND4-17 is a potent NRF2 (nuclear factor erythroid 2-related factor 2) activator that covalently modifies a critical stress-sensor cysteine (C151) in the BTB domain of the E3 ligase substrate adaptor protein Kelch-like ECH-associated protein 1 (KEAP1), the primary negative regulator of NRF2. | ||
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