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TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 μM . SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity .
DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells .
Anti-inflammatory agent 6 blocks the phosphorylation of I kappa b kinase α/β (IKKα/β), IκBα, and nuclear factor kB p65 (NF-κB p65) which is a key controller of inflammation, thereby showing anti-inflammatory potential.
β5i-IN-1 is a potent and selective inhibitor of β5i with a IC50 of 8.463 nM. β5i-IN-1 releases TNF-α and IL-6 and influences the transcriptional activity of NF-κB. β5i-IN-1 can be used in study idiopathic pulmonary fibrosis .
TNF-α-IN-19 is an inhibitor of TNFα that can block the interaction between TNFαRI, TRADD, and RIP1, the EC50 values for TNFα, IL-1β, and IL-1β/TNFα are 2.451, 3.792 and 1.54 μM, respectively. TNF-α-IN-19 only inhibits the degradation of IκBα when cells are stimulated by TNFα and not by IL-1β .
Urotensin I (Catostomus urotensin I), a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively .
8-NBD-cGMP is a fluorescent analog of cyclic guanosine monophosphate and a potent, membrane-permeable, fluorescent activator of cGMP-dependent protein kinase isozymes Iα and Iβ. 8-NBD-cGMP is barely fluorescent in aqueous solution but fluoresces strongly in hydrophobic environments such as hydrophobic protein binding sites
Urotensin I (Catostomus urotensin I) TFA, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively .
Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway .
XVA143, an α/βI-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo .
DACA (Standard) is the analytical standard of DACA. This product is intended for research and analytical applications. DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and DNA topoisomerase (topo) II. DACA stabilises topo I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research .
Human IFNAR2 mRNA encodes the human interferon alpha and beta receptor subunit 2 (IFNAR2) protein, a protein that belongs to the type II cytokine receptor family. IFNAR2 is a type I membrane protein that forms one of the two chains of a receptor for interferons alpha and beta. Binding and activation of the receptor stimulates Janus protein kinases, which in turn phosphorylate several proteins, including STAT1 and STAT2.
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
LM-189, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 can be used to develop the Gαi-biased β2AR agonists .
Anti-inflammatory agent 100 (Compound (+)-4S-23) is an anti-inflammatory agent. Anti-inflammatory agent 100 inhibits MAPK and NF-κB signaling, and also inhibits NF-κB pathway by suppressing the phosphorylation of IκB-α and blocking nuclear translocation of phosphorylated p65. Anti-inflammatory agent 100 inhibits NO production (IC50: 0.5 μM) and TNF-α, IL-6, IL-1β secretion .
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity .
Sp-8-pCPT-cGMPS is a potent cyclic guanosine monophosphate-gated channel agonist and a lipophilic activator of protein kinase G (types Iα, Iβ, and II) and protein kinase A type II with excellent cell membrane permeability and phosphodiesterase stability. Sp-8-pCPT-cGMPS can be used to study the role of cGMP in neural plasticity and synaptic transmission .
Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
LM-189 free base, a G protein alpha subunit I (Gαi)-biased agonist, is a Gαi-biased ligand of β2-adrenergic receptor (β2AR). LM-189 free base stabilizes a distinct conformation in TM6 and increases the dynamics of ICL2. LM-189 free base can be used to develop the Gαi-biased β2AR agonists .
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease .
CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells .
NF-κB-IN-15 (compound 14r) is a potent NF-κB inhibitor. NF-κB-IN-15 decreases the NO levels and inhibits the release of IL-6, TNF-α, and IL-1β in LPS (HY-D1056) -induced cells. NF-κB-IN-15 inhibits LPS-induced phosphorylation of p65 and degradation of IκBα. NF-κB-IN-15 shows anti-inflammatory activity has the potential for the research of acute lung injury (ALI) .
Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively) .
IDO1-IN-27 (Compound I-1) is a Indoleamine 2,3-Dioxygenase 1 (IDO1) inhibitor with an IC50 of 0.3951 μM for recombinant hIDO1. IDO1-IN-27 also inhibits hIDO1 expression in HeLa cells (EC50: 62 nM). IDO1-IN-27 effectively stimulates T cell proliferation by reducing the mRNA expression of pro-inflammatory factors (TNF-α, IL-6, and IL-1β) while concurrently inhibiting LLC cells growth .
ALK5-IN-10 (Compound 5d) is a TGF-β type I receptor kinase ALK5 inhibitor, with IC50s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer .
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively) .
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class IPI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
Pilaralisib (XL147; SAR245408) is a potent and highly selective class IPI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research .
Arotinolol-d5 (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
Arotinolol (Standard) is the analytical standard of Arotinolol. This product is intended for research and analytical applications. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
Buparlisib (Standard) is the analytical standard of Buparlisib. This product is intended for research and analytical applications. Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
Fimepinostat mesylate potently inhibits class IPI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
Fimepinostat (CUDC-907) potently inhibits class IPI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect .
Immunoproteasome activator 1 (compound A) is a selective immunoproteasome activator that increases the presentation of individual MHC-I–bound peptides by over 100-fold. Immunoproteasome activator 1 binds to the proteasome structural subunit PSMA1 and promotes the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes .
Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC50 of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2 .
Dactolisib (BEZ235) is an orally active and dual pan-class IPI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis .
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity . GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Sp-8-Br-PET-cGMPS is a membrane-permeable PKG agonist and a membrane-permeable inhibitor of retinal-type cGMP-gated ion channels, as well as an activator of cGMP-dependent protein kinases Iα and Iβ. Sp-8-Br-PET-cGMPS is resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, has no metabolic side effects, and is more lipophilic and permeable than Sp-8-pCPT-cGMPS. Sp-8-Br-PET-cGMPS can be used to study the role of cGMP signaling pathways in the nervous system .
Buparlisib (Hydrochloride) (Standard) is the analytical standard of Buparlisib (Hydrochloride). This product is intended for research and analytical applications. Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
AMG 511 is a potent and orally available pan inhibitor of class IPI3Ks, with Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model .
Pilaralisib (Standard) is the analytical standard of Pilaralisib. This product is intended for research and analytical applications. Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
Dichotomine C ((R)-(-)-Dichotomine C) is a β-carboline-type alkaloid with antiallergic effects. Dichotomine C inhibits the release of β-hexosaminidase in RBL-2H3 cells with an IC50 of 62 μM. Dichotomine C inhibits the releases of antigen-IgE-mediated TNF-α and IL-4 in RBL-2H3 cells with IC50s of 19 μM and 15 μM, respectively. Dichotomine C can be used for the study of type I allergic reactions .
ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis .
Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class IPI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
SN32976 is a potent and selective class IPI3K and mTOR inhibitor with IC50s of 15.1 nM, 461 nM, 110 nM, 134 nM and 194 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR, respectively. SN32976 shows high selectivity among other 442 kinases. SN32976 shows anticancer effects .
ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research .
Astragaloside II (Standard) is the analytical standard of Astragaloside II (HY-N0433). This product is intended for research and analytical applications. Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis .
IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43?nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150?nM) and mTOR (IC50=157?nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class IPI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a?Ki?of 17 nM for mTOR.
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class IPI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class IPI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity .
TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor that can be used for the research of idiopathic pulmonary fibrosis. TRPV1-IN-3 affects the expression of fibrosis markers collagen I and α-SMA by inhibiting the TGF-β/Smads and MAPK pathways, thereby exerting antifibrotic activity in vitro (IC50=0.51 μM). TRPV1-IN-3 significantly inhibits collagen deposition in lung tissue, improves the alveolar structure, and also increases the survival rate of mice with pulmonary fibrosis induced by Bleomycin (HY-108345) .
Apitolisib (Standard) is the analytical standard of Apitolisib. This product is intended for research and analytical applications. Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
Copanlisib (Standard) is the analytical standard of Copanlisib. This product is intended for research and analytical applications. Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class IPI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity .
Voxtalisib (Standard) is the analytical standard of Voxtalisib. This product is intended for research and analytical applications. Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively.
IN-1130 (Standard) is the analytical standard of IN-1130. This product is intended for research and analytical applications. IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
PIK-C98 is a potent and selective PI3K inhibitor, with IC50s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma .
Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis .
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model .
CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50 of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells .
Urotensin I (Catostomus urotensin I) TFA, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively .
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
Urotensin I (Catostomus urotensin I), a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively .
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research .
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis .
Microcolin H is a marine lipopeptide and phosphatidylinositol transfer protein ligand that targets PITPα/β. Microcolin H increases the conversion of LC3I to LC3II and reduces p62 levels in cancer cells, leading to autophagy cell death (Autophagy). Microcolin H effectively inhibits tumor development and has anti-proliferative activity in nude mouse subcutaneous tumor models .
1-Dehydro-[10]-gingerdione directly inhibits IKKβ activity by targeting the activation loop of IKKβ, thus disrupting IKKβ-catalysed IκBα phosphorylation in macrophages stimulated with agonists. 1-Dehydro-[10]-gingerdione inhibits LPS (HY-D1056)-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione has the potential for NF-κB-associated inflammation and autoimmune disorders research .
Harmane (Standard) is the analytical standard of Harmane. This product is intended for research and analytical applications. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect .
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
Dichotomine C ((R)-(-)-Dichotomine C) is a β-carboline-type alkaloid with antiallergic effects. Dichotomine C inhibits the release of β-hexosaminidase in RBL-2H3 cells with an IC50 of 62 μM. Dichotomine C inhibits the releases of antigen-IgE-mediated TNF-α and IL-4 in RBL-2H3 cells with IC50s of 19 μM and 15 μM, respectively. Dichotomine C can be used for the study of type I allergic reactions .
Astragaloside II (Standard) is the analytical standard of Astragaloside II (HY-N0433). This product is intended for research and analytical applications. Astragaloside II is an orally active Cycloartane-type triterpene glycoside. Astragaloside II can be extracted from Astragalus membranaceus. Astragaloside II inhibits Autophagy, decreases pro-inflammatory cytokines (IL-6, IL-1β), HIF-α, p-p65, p-IκB and increases SOD. Astragaloside II regulates immunity and reduces inflammatory responses. Astragaloside II can be used in the research of diseases such as liver cancer, osteoporosis, immunosuppressive diseases, and ulcerative colitis .
Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis .
IFNAR1, one of the subunit of IFN-α/β receptor, is a type I IFN receptor. IFNAR1 forms the heterodimeric receptor with IFNAR2. IFNAR1 mediates IFN-induced STAT signaling by interacting with tyrosine kinase 2 (Tyk2). Upon activation by these IFNs, IFNAR1 and IFNAR2 undergo a conformational change to promote a cascade of downstream signaling events, including the phosphorylation of Tyk2 and JAK1, STAT1 and STAT2. IFNAR1 Protein, Cynomolgus (HEK293, His) is a recombinant Cynomolgus IFNAR1 (A25-K437) with C-terminal 6*His tag, which is produced in HEK293 cells.
The ST6GAL1 protein is responsible for facilitating the transfer of sialic acid from CMP-sialic acid to galactose-containing receptor substrates. Sialic acid is an important component of a variety of glycoproteins and glycolipids, and ST6GAL1 protein-mediated sialic acid transfer plays a crucial role in regulating the structure and function of these molecules. ST6GAL1 Protein, Rat (HEK293, His) is the recombinant rat-derived ST6GAL1 protein, expressed by HEK293 , with N-His labeled tag.
ST6GAL1, a pivotal enzyme, facilitates glycosylation by transferring sialic acid from CMP-sialic acid to galactose-containing acceptor substrates. ST6GAL1 Protein, Human (HEK293, His) is the recombinant human-derived ST6GAL1 protein, expressed by HEK293 , with C-6*His labeled tag.
IFNAR1, one of the subunit of IFN-α/β receptor, is a type I IFN receptor. IFNAR1 forms the heterodimeric receptor with IFNAR2. IFNAR1 mediates IFN-induced STAT signaling by interacting with tyrosine kinase 2 (Tyk2). Upon activation by these IFNs, IFNAR1 and IFNAR2 undergo a conformational change to promote a cascade of downstream signaling events, including the phosphorylation of Tyk2 and JAK1, STAT1 and STAT2. IFNAR1 Protein, Human (HEK293, His) is a recombinant human IFNAR1 (K28-K436) with C-terminal 6*His tag, which is produced in HEK293 cells.
B2M is a component of MHC class I complexes that present peptide antigens to the immune system. HLA-A*0201 GP100 complex Protein, Human (Biotinylated, IMDQVPFSV, HEK293, Avi-His) is a recombinant protein dimer complex containing human-derived HLA-A*0201 GP100 complex protein, expressed by HEK293 , with C-Avi, C-10*His labeled tag.
The POMGNT1 protein crucially directs O-mannosyl glycosylation, which adds N-acetylglucosamine to O-linked mannose residues on glycoproteins. It catalyzes GlcNAc(beta1-2)Man(alpha1-)O-Ser/Thr on α-dystroglycan and other O-mannosylated proteins, laying the foundation for subsequent carbohydrate addition. POMGNT1 Protein, Human (HEK293, His) is the recombinant human-derived POMGNT1 protein, expressed by HEK293 , with C-6*His labeled tag.
Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively) .
Arotinolol-d5 (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively) .
PRKACA/PRKACB; PRKACA + PRKACB; PKA alpha + beta; PKA alpha; PKA beta; cAMP dependent protein kinase alpha catalytic subunit; cAMP dependent protein kinase beta catalytic subunit; cAMP dependent protein kinase catalytic subunit alpha; cAMP dependent protein kinase catalytic subunit beta; DKFZp781I2452; MGC102831; MGC41879; MGC48865; MGC9320; PKA C alpha; PKA C beta; PKACA; PKACB; PRKACA; PRKACB; Protein kinase A catalytic subunit alpha; Protein kinase A catalytic subunit; Protein kinase A catalytic subunit beta; Protein kinase cAMP dependent catalytic alpha; Protein kinase cAMP dependent catalytic beta; cAMP dependent protein kinase catalytic subunit alpha isoform 1; cAMP-dependent protein kinase catalytic subunit alpha; KAPCA_HUMAN; KAPCB_HUMAN; PKA C alpha; PKA C-alpha; PKACA; PRKACA; Protein kinase A catalytic subunit; Protein kinase cAMP dependent catalytic alpha.
WB, ELISA, IHC-P, IHC-F, ICC/IF
Human, Mouse
PKA alpha + beta Antibody is an unconjugated, approximately 40 kDa, rabbit-derived, anti-PKA alpha + beta polyclonal antibody. PKA alpha + beta Antibody can be used for: WB, ELISA, IHC-P, IHC-F, ICC, IF expriments in human, mouse, and predicted: rat background without labeling.
IKK alpha/beta Antibody (YA1871) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1871), targeting IKK alpha/beta, with a predicted molecular weight of 85 kDa (observed band size: 75,87 kDa). IKK alpha/beta Antibody (YA1871) can be used for WB, ICC/IF, IP experiment in human, mouse, rat background.
IFNAR1; IFNAR; Interferon alpha/beta receptor 1; IFN-R-1; IFN-alpha/beta receptor 1; Cytokine receptor class-II member 1; Cytokine receptor family 2 member 1; CRF2-1; Type I interferon receptor 1
WB, IP
Human
Interferon alpha/beta Receptor 1 Antibody (YA3112) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3112), targeting Interferon alpha/beta Receptor 1, with a predicted molecular weight of 64 kDa (observed band size: 110-130 kDa). Interferon alpha/beta Receptor 1 Antibody (YA3112) can be used for WB, IP experiment in human background.
IKK α/β Antibody (YA6151) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to IKK α/β. It can be applicated for WB, IHC-P, ICC/IF, IP, ELISA assays, in the background of human, mouse, rat.
S6K1 Antibody is an unconjugated, approximately 59 kDa, rabbit-derived, anti-S6K1 monoclonal antibody. S6K1 Antibody can be used for: WB, ICC/IF, IP expriments in human, rat, mouse background without labeling.
S6K1 Antibody (YA6220) is a rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to S6K1. It can be applicated for WB, IHC-P, ICC/IF, IP, ELISA assays, in the background of human, mouse, rat.
Human IFNAR2 mRNA encodes the human interferon alpha and beta receptor subunit 2 (IFNAR2) protein, a protein that belongs to the type II cytokine receptor family. IFNAR2 is a type I membrane protein that forms one of the two chains of a receptor for interferons alpha and beta. Binding and activation of the receptor stimulates Janus protein kinases, which in turn phosphorylate several proteins, including STAT1 and STAT2.
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