36801 Results for: "Stream Tables Earth Science Models&amp"

Supplier: Aladdin Scientific

CC-92480 CC-92480 is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity. TargetsCereblonIn vitroCC-92480 has a unique and rapid degradation profile: the enhanced efficiency to drive the formation of the protein−protein interaction between Aiolos and cereblon, inducing targeted docking to the CRL4-CRBN E3 ubiquitin ligase complex. The CC-92480-dependent binding of Aiolos/Ikaros to CRBN leads to polyubiquitination and ultimately proteasome-mediated degradation of protein. Rapid and extensive loss of Aiolos/Ikaros in sensitive cells, such as multiple myeloma cells, results in apoptosis and subsequent cell death.

Supplier: Aladdin Scientific

CC-92480 CC-92480 is a novel protein degrader and a cereblon E3 ligase modulator (CELMoD) that has anti-myeloma activity. TargetsCereblonIn vitroCC-92480 has a unique and rapid degradation profile: the enhanced efficiency to drive the formation of the protein−protein interaction between Aiolos and cereblon, inducing targeted docking to the CRL4-CRBN E3 ubiquitin ligase complex. The CC-92480-dependent binding of Aiolos/Ikaros to CRBN leads to polyubiquitination and ultimately proteasome-mediated degradation of protein. Rapid and extensive loss of Aiolos/Ikaros in sensitive cells, such as multiple myeloma cells, results in apoptosis and subsequent cell death.

Supplier: Aladdin Scientific

AZD1390 is a first-in-class orally available and CNS penetrantATMinhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.TargetsATM (Cell-based assay) 0.78 nM In vitro AZD1390 blocks ATM-dependent DDR (DNA damage response) pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 results in increased genome instability.In vivoAZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog).

Supplier: Aladdin Scientific

AZD1390 is a first-in-class orally available and CNS penetrantATMinhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases.TargetsATM (Cell-based assay) 0.78 nM In vitro AZD1390 blocks ATM-dependent DDR (DNA damage response) pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type. AZD1390 results in increased genome instability.In vivoAZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog).

Supplier: Aladdin Scientific

BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity.TargetsBUB1 (Cell-free assay) 6.1 nM In vitro BAY 1816032 is a novel, bioavailable inhibitor of the catalytical activity of the mitotic checkpoint protein BUB1, which is involved in centromere cohesion and attachment error correction.

Supplier: Aladdin Scientific

BAY-1816032 BAY-1816032 is a potent and oral available inhibitor of budding uninhibited by benzimidazoles 1 (BUB1) kinase with IC50 of 6.1 nM for recombinant catalytic domain of human BUB1. BAY-1816032 has antitumor activity.TargetsBUB1 (Cell-free assay) 6.1 nM In vitro BAY 1816032 is a novel, bioavailable inhibitor of the catalytical activity of the mitotic checkpoint protein BUB1, which is involved in centromere cohesion and attachment error correction.

Supplier: Aladdin Scientific

COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.Targetsp53 mutantsin vitroThe thiosemicarbazone COTI-2 is reported to promote refolding of mutant p53 and restore wild-type-p53 function. It is active against human tumour cell lines of various origins at nanomolar concentrations, induces cell death by apoptosis.

Supplier: Aladdin Scientific

COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.Targetsp53 mutantsin vitroThe thiosemicarbazone COTI-2 is reported to promote refolding of mutant p53 and restore wild-type-p53 function. It is active against human tumour cell lines of various origins at nanomolar concentrations, induces cell death by apoptosis.

Supplier: Aladdin Scientific

AM 095 AM095 is an antagonist of the LPA type 1 receptor with IC50 values of 0.98 and 0.73 μM for recombinant human and mouse LPA1, respectively. TargetsLPA1 receptorIn vitroAM095 is a potent LPA1 receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively, and exhibited no LPA1 agonism. In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM).

Supplier: Aladdin Scientific

ASLAN003 ASLAN003 (LAS 186323) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors. TargetsAP-1 ; human DHODH (Cell-free assay) ; 35 nM In vitro ASLAN003 is a highly potent dihydroorotate dehydrogenase inhibitor that induces differentiation, as well as reducing cell proliferation and viability, of AML cell lines and primary AML blasts including chemoresistant cells.

Supplier: Aladdin Scientific

ASLAN003 ASLAN003 (LAS 186323) is a potent and orally active inhibitor of DHODH (Dihydroorotate dehydrogenase) with IC50 of 35 nM for human DHODH enzyme activity. ASLAN003 impairs protein synthesis and induces the differentiation and apoptosis transcriptional program in acute myeloid leukemia (AML) cells via activation of AP-1 transcription factors. TargetsAP-1 ; human DHODH (Cell-free assay) ; 35 nM In vitro ASLAN003 is a highly potent dihydroorotate dehydrogenase inhibitor that induces differentiation, as well as reducing cell proliferation and viability, of AML cell lines and primary AML blasts including chemoresistant cells.

Supplier: Aladdin Scientific

AZ876 AZ876 is a novel high-affinity Liver X Receptor (LXR) agonist with Ki values of 0.007 μM and 0.011 μM for human LXRα and LXRβ respectively. TargetsLXRα ; LXRβ 0.007 μM(Ki); 0.011 μM(Ki)In vitroIn binding assays, AZ876 is 25-fold and 2.5-fold more potent than GW3965 on human (h)LXRα and hLXRβ respectively. In reporter transactivation assays, AZ876 is 196-fold and fivefold more potent than GW3965 on hLXRα and hLXRβ respectively. AZ876 is also more potent than GW3965 on mouse (m)LXRα (248-fold) and mlXRβ (10.5-fold).

Supplier: Aladdin Scientific

Acalabrutinib (ACP-196) Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.

Supplier: Aladdin Scientific

AZ876 AZ876 is a novel high-affinity Liver X Receptor (LXR) agonist with Ki values of 0.007 μM and 0.011 μM for human LXRα and LXRβ respectively. TargetsLXRα ; LXRβ 0.007 μM(Ki); 0.011 μM(Ki)In vitroIn binding assays, AZ876 is 25-fold and 2.5-fold more potent than GW3965 on human (h)LXRα and hLXRβ respectively. In reporter transactivation assays, AZ876 is 196-fold and fivefold more potent than GW3965 on hLXRα and hLXRβ respectively. AZ876 is also more potent than GW3965 on mouse (m)LXRα (248-fold) and mlXRβ (10.5-fold).

Supplier: Aladdin Scientific

Acalabrutinib (ACP-196) Acalabrutinib (ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 3 nM, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. ACP-196 has improved target specificity over ibrutinib with 323-, 94-, 19- and 9-fold selectivity over the other TEC kinase family members (ITK, TXK, BMX, and TEC, respectively) and no activity against EGFR.

Supplier: Aladdin Scientific

AZD8835 ia a novel mixed inhibitor ofPI3 KαandPI3 Kδwith IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity againstPI3 Kβ(IC50=431 nM) andPI3 Kγ(IC50=90 nM). TargetsPI3 Kδ (Cell-based assay); PI3 Kα (Cell-free assay); PI3 Kγ (Cell-based assay); PI3 Kβ (Cell-based assay) 5.7 nM; 6.2 nM; 90 nM; 431 nMIn vitroAZD8835 is a potent inhibitor of PI3 Kα (wild type, E545 K and H1047 R mutations) and PI3 Kδ with excellent selectivity vs. PI3 Kβ, PI3 Kγ and an excellent general kinase selectivity.

Supplier: Aladdin Scientific

ABX-1431 ABX-1431 is a highly potent, selective, and CNS-penetrant Monoacylglycerol lipase (MGLL) inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively.TargetshMGLL ; mMGLL 14 nM; 27 nMIn vitroABX-1431 is a potent human MGLL inhibitor (average IC50 = 0.014 μM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Treatment of intact human PC3 cells with ABX-1431 following a 30 min inhibitor incubation time causes concentration dependent inhibition of MGLL activity with an IC50 value of 0.0022 μM, which is ∼6-fold more potent than that observed In vitro.

Supplier: Aladdin Scientific

ABX-1431 ABX-1431 is a highly potent, selective, and CNS-penetrant Monoacylglycerol lipase (MGLL) inhibitor with IC50 values of 14 nM and 27 nM for hMGLL and mMGLL respectively.TargetshMGLL ; mMGLL 14 nM; 27 nMIn vitroABX-1431 is a potent human MGLL inhibitor (average IC50 = 0.014 μM) with >100-fold selectivity against ABHD6 and >200-fold selectivity against PLA2G7. Treatment of intact human PC3 cells with ABX-1431 following a 30 min inhibitor incubation time causes concentration dependent inhibition of MGLL activity with an IC50 value of 0.0022 μM, which is ∼6-fold more potent than that observed In vitro.

Supplier: Aladdin Scientific

Avadomide (CC-122) Avadomide (CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma (DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4 CRBN. Targets CRBN In vitro CC-122 is a novel agent for DLBCL with antitumor and immunomodulatory activity. In DLBCL cell lines, It binds CRBN and induces degradation or short hairpin RNA-mediated knockdown of Aiolos and Ikaros which correlates with increased transcription of interferon (IFN)-stimulated genes independent of IFN-α, -β, and -γ production and/or secretion and results in apoptosis in both activated B-cell (ABC) and germinal center B-cell DLBCL cell lines.

Supplier: Aladdin Scientific

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is aGSK-3α/βinhibitor withIC50of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of theWnt/beta-cateninsignaling pathway. CHIR-99021 significantly rescues light-inducedautophagyand augments GR, RORα and autophagy-related proteins.TargetsGSK-3β (Cell-free assay); GSK-3α (Cell-free assay) 6.7 nM; 10 nM In vitro CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM. In addition to simulating the actions of insulin, inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ).

Supplier: Aladdin Scientific

CHIR-99021 (CT99021) HCl is hydrochloride of CHIR-99021, which is aGSK-3α/βinhibitor withIC50of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2. CHIR-99021 is a potent pharmacological activators of theWnt/beta-cateninsignaling pathway. CHIR-99021 significantly rescues light-inducedautophagyand augments GR, RORα and autophagy-related proteins.TargetsGSK-3β (Cell-free assay); GSK-3α (Cell-free assay) 6.7 nM; 10 nM In vitro CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs CDC2 and ERK2, as well as other protein kinases. Furthermore, CHIR-99021 shows only weak binding to a panel of 22 pharmacologically relevant receptors and little inhibitory activity against a panel of 23 nonkinase enzymes. CHIR-99021 induces the activation of glycogen synthase (GS) in insulin receptor-expressing CHO-IR cells with EC50 of 0.763 μM. In addition to simulating the actions of insulin, inhibition of GSK-3 by CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. During any of the first 3 days of differentiation, CHIR-99021 treatment inhibits the preadipocyte differentiation with IC50 of 0.3 μM by blocking induction of CCAAT/enhancer-binding protein α (C/EBPα) and peroxisome proliferator-activated receptor γ (PPARγ).