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(Rac)-SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor having 1,4-dihydropyrano[2,3-c]pyrazole structure. (Rac)-SHIN2 involves in folate or one-carbon metabolism pathways, prevents viral infection. SHMT1 and SHMT2 are the cytosolic and/or mitochondrial isoforms of serine hydroxymethyltransferase, respectively . (Rac)-SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM .
Prokineticin 2 Isoform 2 (human) is a hypothalamic neuropeptide. Prokineticin 2 Isoform 2 (human) decreases food intake and involves in thermoregulation and energy metabolism in rodents. Prokineticin 2 has the potential for the research of hyperglycemia, metabolic syndrome (MetS) and obesity .
Ledelabricin alfa is a human proteoglycan 4 (PRG4) isoform A variant. PRG4 is a joint/boundary lubricant. Ledelabricin Alfa can be used for the research arthropathy .
hCAIX/XII-IN-10 (compound DK-8) is a carbonic anhydrase inhibitor. hCAIX/XII-IN-10 has potent inhibitory activity against tumor-associated membrane-bound isoformshCA IX and XII, with Ki values of 32.5 nM and 29.2 nM .
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms .
Beta-defensin 103 isoform X1, pig is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens .
Beta-defensin 103 isoform X1, pig TFA is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens .
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .
DFP00173 is a potent and selective aquaporin-3 (AQP3) inhibitor. DFP00173 inhibits mouse and human AQP3 with an IC50 of ∼0.1-0.4 μM. DFP00173 is selective for AQP3 over the homologous AQP isoforms AQP7 and AQP9 .
AMPK-α1β1γ1 activator 1 (M1) is an acyl glucuronide metabolite of Indole-3-carboxylic Acid-based AMPK activator. AMPK-α1β1γ1 activator 1 can selectively activated human β1 isoforms with an EC50 value of 38.1nM. AMPK-α1β1γ1 activator 1 can direct binding with human AMPK α1β1γ1 isoform. AMPK-α1β1γ1 activator 1 can be used for the research of diabetic nephropathy .
Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
Zoniporide (CP-597396) hydrochloride is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM) .
Efdamrofusp alfa is a bispecific fusion protein. Efdamrofusp alfa is capable of neutralizing both VEGF isoforms and C3b/C4b. Efdamrofusp alfa can be used for the research of neovascular age-related macular degeneration (nAMD) and other complement-related ocular conditions .
NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats .
Epristeride (Standard) is the analytical standard of Epristeride. This product is intended for research and analytical applications. Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability .
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
UB-165 is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for [ 3H]-nicotine binding in rat brain .
Coumberone is a metabolic fluorogenic probe, and isoform-selective substrate for all AKR1C isoforms. Coumberone can be reduced by all four members of the AKR1C family to its fluorescent alcohol coumberol. Coumberone can be used for the research of AKR1C .
AZ-PFKFB3-67 quarterhydrate is potent and selective metabolic kinase PFKFB3 inhibitor, with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1 respectively .
hCAII-IN-7 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor with Kis of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively .
BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717))
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrial membrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases .
Tetrahydrobiopterin ((Rac)-Sapropterin) is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XII inhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitory activity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .
Palmitoleoyl-CoA triammonium is the triammonium salt form of Palmitoleoyl-CoA (HY-137782). Palmitoleoyl-CoA triammonium can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA triammonium induces the cardiac mitochondrial membrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA triammonium regulates metabolism via allosteric control of AMPK β1-isoforms .
Palmitoleoyl-CoA lithium is the lithium salt form of Palmitoleoyl-CoA (HY-137782). Palmitoleoyl-CoA lithium can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA lithium induces the cardiac mitochondrial membrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA lithium regulates metabolism via allosteric control of AMPK β1-isoforms .
Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
[Asn18] Endothelin-1, human is a peptide. Endothelin-1 is a major isoform of Endothelin and plays an important role for regulation of vascular function .
RB394 is a potent dual sEH/PPARγ modulator isoform that promotes adipocyte browning and exhibits cardioprotective activity, and can be used to suppress metabolic syndrome.
α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoformphosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM .
Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation .
Para-aminoblebbistatin is a highly water soluble, non-fluorescent and photostable C15 amino-substituted derivative of blebbistatin; inhibits various (myosin II) isoforms both in vitro and in vivo.
(Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes .
(Z)-Pseudoginsenoside Rh2 is the (Z) isoform of Pseudoginsenoside Rh2 (HY-125825), which is synthesized from Ginsenoside Rh2, possesses anti-cancer activitied .
NG-Amino-L-arginine hydrochloride induces inactivation of the citrulline-forming activity of the nNOS, iNOS, and eNOSisoforms with Ki values of 0.3 μM, 3 μM, and 2.5 μM, respectively .
(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
Dexamethasone oxetanone (Dex-Ox), a derivative of the glucocorticoid-selective steroid Dexamethasone (Dex), is an antiglucocorticoid. Dexamethasone oxetanone is an antiprogestin with significant agonist activity with progesterone receptor (PR) A and B isoforms .
26:0 Coenzyme A (Hexacosanoyl coenzyme A triammonium) is a type of coenzyme A that can serve as a substrate for 1-acylglycerol-3-phosphate-O-acyltransferase isoform 11 (AGPAT11) .
Bergapten (Standard) is the analytical standard of Bergapten. This product is intended for research and analytical applications. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYPisoforms.
N-desmethyl Eletriptan is a metabolite of Eletriptan (HY-A0039). It is formed from eletriptan primarily by the cytochrome P450 (CYP) isoform CYP3A4 in human liver microsomes.
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
trans-hydroxy Glimepiride is an active metabolite of the sulfonylurea Glimepiride (HY-B0104). It is formed from glimepiride primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9.
hCAI/II-IN-9 is a carbonic anhydrase inhibitor with inhibitory activity against human carbonic anhydrase isoforms I, II, IX, and XII. The inhibition constants (Ki) of hCAI/II-IN-9 for hCA I are in the range of 7.9-894 nM, for hCA II are in the range of 7.5-1645 nM, for hCA IX are in the range of 5.0-240 nM, and for hCA XII are in the range of 0.47-2.83 nM. hCAI/II-IN-9 may have potential applications in inhibiting a variety of pathologies involving these carbonic anhydrase isoforms .
(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca 2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function .
(+)-Leucocyanidin is the isoform of Leucocyanidin (HY-119580), is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models .
(E/Z)-NSAH is an isoform of NSAH (HY-114503), which is reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2) .
hCAIX/XII-IN-11 (Compound 6c) is an inhibitor of hCA IX and hCA XII with a Ki value of 0.7 μM for both the isoforms. hCAIX/XII-IN-11 can be used for anticancer research .
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
Cilostazol-d11 is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
α-Tocotrienol is an isoform of vitamin E and found in vegetables, fruits, seeds, nuts, grains, and oils. Vitamin E plays a role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
KL201 a circadian clock modulator, is a isoform-selective cryptochrome 1 (CRY1) stabilizer. KL201 has no stabilizing effect on CRY2. KL201 lengthens the period of circadian rhythms in cells and tissues .
(S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism .
S32826 is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes .
Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
SIRT4-IN-1 (compound 69) is selective sirtuin 4 (Sirt4) inhibitor with an IC50 of 16 μM.SIRT4-IN-1 shows no relevant effects on other sirtuin isoforms .
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer .
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
HDAC6-IN-12 (compound GZ) is a potent HDAC6 inhibitor. HDAC6-IN-12 has anticancer activity through merges into DNA strands causing DNA damage. HDAC6-IN-12 can be used for cancer research .
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
NOS-IN-1 is a potent and orally active NO synthase (NOS)isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively .
Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia .
Carbonic anhydrase inhibitor 21 (Compound 5h) is a selective carbonic anhydrase (hCA IX) inhibitor, with a Ki of 15.1 nM, and is highly selective against other investigated isoform. Carbonic anhydrase inhibitor 21 can be used for anticancer research .
Cilostazol (Standard) is the analytical standard of Cilostazol. This product is intended for research and analytical applications. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM .
Tenapanor (AZD1722) is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor has the potential for the research of hyperphosphatemia .
L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
S32826 disodium is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes .
Aprutumab (BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has the potential for solid tumors research .
Tenapanor (AZD1722) hydrochloride is a potent and orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor hydrochloride reduces intestinal phosphate absorption predominantly through reduction of passive paracellular phosphate flux. Tenapanor hydrochloride has the potential for the research of hyperphosphatemia .
(Rac)-PF-4136309 is an isoform of PF-4136309 (HY-13245), which is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
(Rac)-Lartesertib ((Rac)-M4076; (Rac)-ATM Inhibitor-5) is an isoform of Lartesertib (HY-150617), which is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1) .
Carbonic anhydrase inhibitor 19 (compound 26a) inhibits the Glaucoma related isoformshCA II and hCA XII with Kis of 9.4 nM and 6.7 nM, respectively. Carbonic anhydrase inhibitor 19 reveals an intraocular pressure (IOP) lowering effect .
Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP)isoform CYP2C8 inhibitor with an IC50 of 4.07 μM .
SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity .
INY-05-040 is a AKT degrader that can selectively and quickly degrade all three AKTisoforms. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines, with anti-cancer activity .
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
(−)-C75 is a isoform of C75 (HY-12364), which is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC50 of 35 μM . C75 is a potent CPT1A activator .
(2R,3S)-Emricasan ((2R,3S)-PF 03491390) is an isomer of Emricasan (HY-10396). Emricasan is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors .
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy .
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
(S)-Lansoprazole (Levolansoprazole) is an isoform of Lansoprazole (HY-13662), which is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
(Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia .
SSOe26 sodium is a 15mer antisense oligonucleotide targeting?HER4. SSOe26 sodium induces exon 26 skipping, leading to the generation of a novel mRNA transcript that excludes exon 26 (CYT2 isoform). SSOe26 sodium decreases tumour growth in mouse xenografts.
Dopamine 4-O-sulfate is an inactive metabolite of the catecholamine dopamine. It is formed from dopamine by the sulfotransferase (SULT) isoform SULT1A3. Dopamine 4-O-sulfate is found at lower levels in the brain and circulation than dopamine 3-O-sulfate.
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3 .
(Rac)-SAG is an isoform of SAG (HY-12848). SAG is a potent Smoothened (Smo) receptor agonist (EC50=3 nM; Kd=59 nM). SAG activates the Hedgehog signaling pathway and counteracts Cyclopamine (HY-17024) inhibition of Smo .
BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue BRD4 degrader. BRD4 degrader-1 targets DCAF16 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
GprA is a new synthetic agonist of G-protein-coupled receptor 120/free fatty acid receptor 4 (GPR120/FFAR4), with an AC50 of 203 nM on human GPR120 full isoform. GprA can be used in the research for NAFLD .
PKR activator 3 is a pyruvate kinase isoformPKR activator extracted from patent WO2014139144A1, compound 160. PKR activator 3 can be used for the research of PKR function related diseases, including cancer, diabetes, obesity, autoimmune disorders, and benign prostatic hyperplasia .
Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoformCYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
NOS-IN-3 (Compound 9a) is a potent, selective, imidamide derived NOS inhibitor with an IC50 against iNOS of 4.6 μM, without inhibiting eNOS. NOS-IN-3 has little toxicity and can be studied in the research of inducible isoform involved diseases, such as septic shock .
Cathepsin K inhibitor 6 (compound 19) is an inhibitor of cathepsin K (Cat K) with an IC50 of 17 nM. Cathepsin K inhibitor 6 also has inhibitory effects on other isoforms, with IC50s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively .
d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
Larotrectinib (Standard) is the analytical standard of Larotrectinib. This product is intended for research and analytical applications. Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
(Rac)-Norcantharidin ((Rac)-NCTD) is the isoform of Norcantharidin, which is a synthetic and demethylated anticancer agent derived from Cantharidin (HY-N0209). Norcantharidin has lighter side effects and stronger bioactivity than Cantharidin. And Norcantharidin inhibits cell proliferation, migration and metastasis, and causes apoptosis and autophagy .
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease .
CRT5, a pyrazine benzamide, is a potent and selective inhibitor for all three isoforms of PKD in endothelial cells treated with VEGF (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively). CRT5 decreases VEGF-induced endothelial migration, proliferation and tubulogenesis .
Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function .
Carbonic anhydrase inhibitor 18 (Compound 9) is a human carbonic anhydrase (hCA) isoform inhibitor, with Kis of 604.8, 333.6, 1.9 and 6.7 nM for hCA I, hCA II, hCA IX and hCA XII, respectively. Carbonic anhydrase inhibitor 18 can be used for the research of cancer .
TIM-098a is a selective AAK1 inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitory activity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity .
Carbonic anhydrase inhibitor 5 is a potent and selective human carbonic anhydrase (hCA) inhibitor with IC50s of 42.9, 47,6 and 6.7 nM for hCA II, hCA IX and hCA XII, respectively .
NoxA1ds is a highly efficacious and selective Nox1 (NADPH oxidase isoform 1) inhibitor. NoxA1ds establishes a critical interaction site for Nox1-NOXA1 binding required for enzyme activation. NoxA1ds can be used for the research of hypertension, atherosclerosis and neoplasia .
sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity .
Ranibizumab (RG-6321) (anti-VEGF) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165) . Ranibizumab (anti-VEGF) slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research .
SAICAR-d is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions[1][2].
NOX2-IN-1 (compound 10) is an inhibitor of nicotinamide adenine dinucleotide phosphate oxidase isoform 2 (NOX2). NOX2-IN-1 targets the p47phox−p22phox protein−protein interaction with favorable binding affinities and cellular activities .
Levoleucovorin (Calcium) (Standard) is the analytical standard of Levoleucovorin (Calcium). This product is intended for research and analytical applications. Levoleucovorin Calcium (Calcium levofolinate), a levo isoform of Leucovorin Calcium (HY-13664), possesses antineoplastic effects. Levoleucovorin Calcium is also an augmentor of 5-fluorouracil (HY-90006) cytotoxicity against cancer .
(S)-Mephenytoin (Standard) is the analytical standard of (S)-Mephenytoin. This product is intended for research and analytical applications. (S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism .
CK2-IN-11 (32) is an allosteric CK2 inhibitor, with high selectivity for CK2 with IC50 values of 19.3 nM and 15.6 nM for the CK2α2β2 and the CK2α′2β2 isoforms, respectively .
VRK1/CK1-IN-1 (compound 36) is a dual inhibitor of vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with the Ki of 37.9 nM for VRK1 and IC50s of 17 nM and 15 nM for δ and ε isoforms of CK1, respectively .
PPARα agonist 2 (compound 4u) is a potent and selective PPARα agonist with an EC50 of 37 nM. PPARα agonist 2 exhibits >2,700-fold selectivity for PPARα over other PPAR isoforms. PPARα agonist 2 has the potential for retinal disorders research .
Secologanin (Standard) is the analytical standard of Secologanin. This product is intended for research and analytical applications. Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
5-Hydroxydiclofenac is a major metabolite of Diclofenac (HY-15036). 5-Hydroxydiclofenac is formed by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C189, CYP2C19, and CYP2C8. 5-Hydroxydiclofenac shows apoptotic effects in hepatocytes .
PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoformVps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM .
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD) .
KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoformCLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM) .
HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC50 of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells .
Clindamycin sulfoxide is an active metabolite of the antibiotic Clindamycin (HY-B1455). It is formed via S-oxidation of clindamycin primarily by the cytochrome P450 (CYP) isoform CYP3A4. Clindamycin sulfoxide inhibits the growth of P. prevotti, B. fragilis, and C. sordelli in vitro with MIC values of 2, 2, and 1 mg/L, respectively.
α-Tocotrienol (Standard) is the analytical standard of α-Tocotrienol. This product is intended for research and analytical applications. α-Tocotrienol is an isoform of vitamin E and found in vegetables, fruits, seeds, nuts, grains, and oils. Vitamin E plays a role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies .
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity .
Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies .
hCAII-IN-6 (Compound S-13) is a potent human carbonic anhydrase II (hCA II) inhibitor with a Ki of 4.4 nM. hCAII-IN-6 also inhibits other hCAs isoforms I, IV and IX, with Ki values of 9.2 nM, 480.2 nM and 14.7 nM, respectively. hCAII-IN-6 can be used for glaucoma research .
HDAC6-IN-11 (Compound 9) is a selective HDAC6 inhibitor with the IC50 value of 20.7 nM. HDAC6-IN-11 has more than 300-fold selectivity over HDAC other isoforms. HDAC6-IN-11 shows anti-proliferative activities against cancer cells .
hCAIX/XII-IN-6 is an orally active carbonic anhydrase (CA) inhibitor. hCAIX/XII-IN-6 inhibits human CA isoforms hCA I, II, IV, IX, and XII with Ki values of 6697 nM, 2950 nM, 4093 nM, 4.1 nM and 7.7 nM, respectively. hCAIX/XII-IN-6 can be used for the research of rheumatoid arthritis (RA) .
JBI-589 is a non-covalent PAD4isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3 .
Carbonic anhydrase inhibitor 9 is a potent carbonic anhydrase (CA) inhibitor with Kis of 56.4 and 56.9 nM for hCA II and IX, respectively. Antiproliferative activity .
Cav 3.2 inhibitor 2 is a Cav3.2 T-type Ca 2+ channels inhibitor with an IC50 of 0.09339 μM under -80mV holding potential. Cav 3.2 inhibitor 2 potently suppresses T-channel-dependent somatic and visceral pain in mice. Cav 3.2 inhibitor 2 can be used for the research of intractable pain .
BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSKisoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively .
SJFα is a 13-atom linker PROTAC based on von Hippel-Lindau ligand. SJFα degrades p38α with a DC50 of 7.16 nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM .
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease .
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca 2+ ATPase (SERCA) with IC50s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity .
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) IIIisoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation .
CDK2-IN-12 (compound 10b) is a potent CDK2 inhibitor, with an IC50 of 11.6 μM. CDK2-IN-12 inhibits hCA (carbonic anhydrase) isoforms I, II, IX and XII, with KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 shows anticancer activity .
HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen
bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively .
Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor. Eniporide specifically inhibits the NHE-1 isoform. Eniporide improves cardiac performance inhibition associated with myocardial ischemia/reperfusion in animals, and limits infarct size in experimental models. Eniporide regulates cardiac performance and high-energy phosphate content in clinically relevant pig models of CPB and cardiac arrest .
Gemfibrozil (Standard) is the analytical standard of Gemfibrozil. This product is intended for research and analytical applications. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells .
(S)-6-O-Desmethylnaproxen ((S)-6-Desmethyl Naproxen) is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (+)-naproxen ((S)-naproxen). (S)-6-O-Desmethylnaproxen is formed from (S)-naproxen by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2C9.
Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment .
hCAIX-IN-11 (Compound 5d) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 32.7 and 623.5 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
hCAIX-IN-10 (Compound 6i) is a selective carbonic anhydrase IX and XII inhibitor with Ki s of 61.5 and 586.8 nM for hCA IX and hCA XII, respectively. hCA IX and hCA XII are transmembrane isoforms which have been characterized as biomarkers for several types of tumors. The hCA XII assists in maintenance of acid-base homoeostasis in normal as well as tumor cells .
JNJ-49095397 (RV568) is an inhaled narrow-spectrum kinase inhibitor (NSKI) against both the α and γ isoforms of p38 MAPK. JNJ-49095397 also inhibits SRC kinase family, specifically haematopoietic kinase (HCK) JNJ-49095397 shows potent anti-inflammatory effects and can be used for the research of chronic obstructive pulmonary disease (COPD) and asthma .
PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955isoforms, respectively .
PROTAC CDK9 degrader-6 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-6 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-6 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955isoforms, respectively .
Pioglitazone ketone is an active metabolite of the PPARγ agonist Pioglitazone (HY-13956). Formation of pioglitazone ketone occurs primarly through cytochrome P450 (CYP) isoform CYP2C8-mediated metabolism of pioglitazone. Pioglitazone ketone (100 mg/kg in the diet) reduces blood glucose levels in a KKAy mouse model of type 2 diabetes.
16α-hydroxy Dehydroepiandrosterone is a metabolite of the endogenous steroid hormone dehydroepiandrosterone. 16α-hydroxy Dehydroepiandrosterone is formed from dehydroepiandrosterone via 16-hydroxylation by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP3A5 in adult human liver microsomes, as well as by fetal recombinant CYP3A7. It is a precursor to fetal estrogens, including estriol.
Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases .
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6isoform 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 .
(S)-CE-123 is a potent, selective, and novel atypical dopamine transporter (DAT) inhibitor with an EC50 of 2.76 μM in uptake inhibition assays conducted in HEK293 cells stably expressing human isoforms of DAT. (S)-CE-123, a Modafinil analogue, is able to penetrate the blood–brain barrier. (S)-CE-123 improves cognitive and motivational processes in experimental animals .
22-HDHA is an oxidation product of docosahexaenoic acid.1 In vitro, it is formed upon incubation of rat liver microsomes with DHA and NADPH and also by the human cytochrome P450 (CYP) isoform CYP4F3B in BTI-TN-5B1-4 microsomes. Serum levels of 22-HDHA increase following dietary DHA supplementation in humans.
PX-866-17OH is the metabolite of PX-866 (Sonolisib, HY-N6775) and a pan-isoform inhibitor of PI3K with IC50s of 14, 57, 131, and 148 nM against PI3Kα, PI3Kβ, PI3Kɣ, and PI3Kδ, respectively .
PAD3-IN-1 (compound 14b) is an inhibitor of protein arginine deiminase (PAD) and is more than 10-fold more selective for PAD3 than PAD 1, 2, and 4. And PAD3 is a PAD isoform associated with neurodegenerative responses to spinal cord injury, and PAD3-IN-1 could be used to study PAD-related neurological diseases .
Methyl-L-NIO (compound 2d) hydrochloride is a potential selective inhibitor (IC50: 70 μM) of dimethylarginine dimethylaminohydrolase hDDAH. Methyl-L-NIO also has inhibitory activity against NO synthase. The inhibition rates of Methyl-L-NIO on different isoforms of NO synthase at a concentration of 100 μM are 77% (nNOS), 20% (eNOS), and 72% (iNOS) respectively; the inhibition rates at a concentration of 1 mM are 100% (nNOS), 85% (eNOS), 100% (iNOS) .
D-688 is an inhibitor of Tau and Aβ. D-688 can reverse Aβ1–42-induced toxicity in SH-SH5Y cells and has significant neuroprotective properties. D-688 can improve the survival rate of Drosophila melanogaster expressing the human tau protein isoform (2N4R) .
APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes .
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
(1R,2R)-ML-SI3 is an isomer of ML-SI3 and a potent inhibitor of three isoforms of TRPML. (1R,2R)-ML-SI3 inhibits TRPMLs with IC50s of 1.6 μM (TRPML1), 2.3 μM (TRPML2), and 12.5 μM (TRPML3), respectively .
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM .
Eicosapentaenoic acid (EPA) is converted to epoxyeicosatetraenoic acids (EpETEs) by several cytochrome P450 isoforms. The major product of this epoxygenase pathway, (±)17(18)-EpETE, relaxes vascular and airway smooth muscle by activating large conductance Ca 2+-activated K + (BKCa) channels by directly interacting with BKα channel subunits. (±)8(9)-EpETE is an epoxygenase pathway product produced from EPA by CYP450 both in vitro and in vivo.
LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively .
MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively . Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation .
CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
AS-041164 is a potent, selective and orally active PI3Kγisoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects .
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation .
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases .
4-(Chloromethyl)-7-hydroxycoumarin (compound 4) is a hydroxycoumarin derivative with potent antioxidant effect and high hydroxyl radical-scavenging property. 4-(Chloromethyl)-7-hydroxycoumarin contains a methyl group and a chlorine group in the heterocyclic ring. A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties has been investigated as potent inhibitors of the zinc enzyme carbonic anhydrase, expecially tumor-associated isoforms CA IX and XII .
VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer . VVD-118313 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(rel)-ML-SI3 is one of the active ingredients of ML-SI3 (HY-139426) (another component is (cis)-ML-SI3) that targets three isoforms of TRPML. (rel)-ML-SI3 is an inhibitor of TRPML1 and TRPML3 (IC50=3.1 μM/28.5 μM), and a potent activator of TRPML2 (EC50=3.3 μM) .
(1S,2S)-ML-SI3 is a trans-isomer of ML-SI3 that targets all three isoforms of TRPML. (1S,2S)-ML-SI3 is an activator of TRPML2 and TRPML3 (EC50=2.7 μM/10.8 μM) and a potent inhibitor of TRPML1 (IC50=5.9 μM) .
(S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems .
7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies .
Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM. .
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively .
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) .
(R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4 .
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC)isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4isoform .
hCAI/II-IN-6 is an orally active human carbonic anhydrase (CA) inhibitor. hCAI/II-IN-6 selectively inhibits hCA II and hCA VII isoforms with Ki values of 220, 4.9, 6.5 and ＞50000 nM for hCA I, hCA II , hCA VII and hCA XII respectively. hCAI/II-IN-6 shows anticonvulsant activity and anti maximal electroshock (MES) activity in vivo. hCAI/II-IN-6 can be used for the research of epilepsy .
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
all-trans-5,6-epoxy Retinoic acid (5,6-epoxy RA) is an agonist of all isoforms of the retinoic acid receptor (RAR; EC50s=77, 35, and 4 nM for RARα, RARβ, and RARγ, respectively). 5,6-epoxy RA (1 μM) also induces growth arrest of MCF-7 and NB4 cells in vitro. It is a natural metabolite of all-trans retinoic acid, which is a metabolite of vitamin A.
Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Anhydroerythromycin A (Standard) is the analytical standard of Anhydroerythromycin A. This product is intended for research and analytical applications. Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
DNMT1/HDAC-IN-1 (compound (R)-23a) is a DNMT1/HDAC dual inhibitor (HDAC1:IC50=0.05 μM), HDAC1 is a major HDACisoform that interacts with DNMT1 in multiple protein complexes for transcriptional silencing of TSGs. DNMT1/HDAC-IN-1 can reshape the tumor immune microenvironment and induce tumor regression, and effectively reverse cancer-specific epigenetic abnormalities .
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1][2].
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1isoforms δ and ε .
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1isoforms δ and ε .
MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities .
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1isoforms δ and ε .
MPT0G211 mesylate is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291 nM). MPT0G211 mesylate displays >1000-fold selective for HDAC6 over other HDAC isoforms. MPT0G211 mesylate can penetrate the blood-brain barrier. MPT0G211 mesylate ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 mesylate has anti-metastatic and neuroprotective effects. Anticancer activities .
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm，Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
TRAP1-IN-1 (compound 35) is a potent and selective inhibitor of TRAP1，a mitochondrial isoform of Hsp90. TRAP1-IN-1 has >250-fold TRAP1 selectivity over Grp94，and disrupts TRAP1 tetramer stability，induces TRAP1 client protein degradation. TRAP1-IN-1 also inhibits mitochondrial complex I of oxidative phosphorylation OXPHOS，disrupts the mitochondrial membrane potential，and enhances glycolysis metabolism .
(S)-6-O-Desmethylnaproxen (Standard) is the analytical standard of (S)-6-O-Desmethylnaproxen. This product is intended for research and analytical applications. (S)-6-O-Desmethylnaproxen ((S)-6-Desmethyl Naproxen) is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (+)-naproxen ((S)-naproxen). (S)-6-O-Desmethylnaproxen is formed from (S)-naproxen by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2C9.
AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
Samotolisib (LY3023414) potently and selectively inhibits class I PI3Kisoforms, 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 .
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ) .
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XIIisoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect .
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Anti-inflammatory agent 67 (compound 7a) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), and has anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 67 has IC50s of 10.4 μM and 50 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 67 binding to different isoforms of carbonic anhydrase are 48.3 nM (CA I), 42.2 nM (CA II), 52.3 nM (CA IX), and 13.3 nM (CA XII) .
Anti-inflammatory agent 68 (compound 7b) is a dual inhibitor of carbonic anhydrase and COX-2, a sulfonamide derivative of Polmacoxib (HY-16726), with anti-inflammatory properties and analgesic activity. Anti-inflammatory agent 68 has IC50s of 12.6 μM and 60 nM for COX-1 and COX-2, respectively. The Ki of anti-inflammatory agent 68 binding to different isoforms of carbonic anhydrase are 52.6 nM (CA I), 79.1 nM (CA II), 58.1 nM (CA IX), and 17.2 nM (CA XII) .
rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide (HY-15206). It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.
AS601245 TFA is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 TFA exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties .
Alagebrium bromide is a cross-link breaker. This study investigated the role of advanced glycation end products (AGEs) in mediating protein kinase C (PKC) isoform expression in diabetic nephropathy. In vitro, vascular smooth muscle cells cultured in high glucose (25-mmol/l) showed increased translocation and expression of PKC-α compared with cells cultured in low glucose (5-mmol/l). Coculture with ALT-711 more effectively attenuated the increased expression and translocation of PKC-α compared with aminoguanidine, an inhibitor of AGE formation. Streptozotocin-induced diabetic rats were randomized to no treatment, ALT-711 treatment, or aminoguanidine treatment. Diabetes induced an increase in PKC-α as well as -βI, -βII, and -ε isoforms. ALT-711 and aminoguanidine treatment, both of which attenuated renal AGE accumulation, abolished these increases in PKC expression. However, only ALT-711 reduced the translocation of phosphorylated PKC-α from the cytoplasm to the membrane. ALT-711 treatment attenuated the expression of vascular endothelial growth factor (VEGF) and extracellular matrix proteins (fibronectin and laminin) and was associated with a reduction in albuminuria. Aminoguanidine had no effect on VEGF expression, although a reduction in fibronectin and laminin was observed. These findings suggest that AGEs are important stimulators of PKC activation, particularly PKC-α, in patients with diabetic nephropathy, which can be directly inhibited by ALT-711.
TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation .
BI 653048 phosphate is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 phosphate inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 phosphate is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC50 value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC50>30 μM) . BI 653048 is extracted from patent WO2005028501A1 (Compound 103), is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes .
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research .
JNK3 inhibitor-4 is a potent inhibitor of JNK3 (IC50=1.0 nM) based on 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile. JNK3 inhibitor-4 shows excellent selectivity over other protein kinases including isoformsJNK1 (IC50=143.9 nM) and JNK2 (IC50=298.2 nM) . JNK3 inhibitor-4 has neuroprotective effect and predicated blood-brain barrier permeability .
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively .
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC50s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC50: 61 nM) and DNA-PK (IC50: 525 nM) .
Binucleine 2 is an isoform-specific and ATP-competitive inhibitor of Drosophila Aurora B kinase (Ki=0.36 μM), a kinase involved in cell division. It is specific for Drosophila Aurora B kinase, inhibiting it in a dose-dependent manner, with minimal inhibition of human or X. laevis Aurora B kinases at concentrations up to 100 μM. Binucleine 2 induces mitotic and cytokinesis defects in Drosophila Kc167 cells. It prevents Drosophila S2 cells from assembling a contractile ring during cell division when used at a concentration of 40 μM but does not affect ring ingression, suggesting that Aurora B kinase activity is not required for that step.
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitory activity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages .
MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC50s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC50s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction .
SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
Z-L(D-Val)G-CHN2 is the isoform of Z-LVG-CHN2 (HY-108137). Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC50=190 nM) via inhibition of SARS-COV-2 3CL pro protease .
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
PI5P4Ks-IN-2 is a inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ). PI5P4Ks-IN-2 targets to PI5P4K isoforms with pIC50 values of <4.3 (PI5P4Kα), <4.6 (PI5P4Kβ), 6.2 (PI5P4Kγ), 0.32 (PI5P4Kγ+), respectively .
RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
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 .
C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
Cacaoidin is a glycosylated lantibiotic isolated from a Streptomyces cacaoi strain. Cacaoidin has potent antibacterial activity against Gram-positive pathogens including Clostridium difficile .
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 .
5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone.
MCE Targeted Diversity Library contains 2,312 compounds, covering more than 1000 targets and isoforms, such as GPCRs, Ion channel, variety of kinases, etc. 1-3 compounds with high potency and selectivity were carefully selected for each target and isoform. The bioactivity information of each compound has been clearly reported in the literatures. This library is a concise collection of small molecule compounds with comprehensive target coverage, which can be used for phenotypic screening at low cost.
MCE Novel Bioactive Compound Library consists of 1,268 bioactive compounds with validated bioactivities tested by cell-based assays or biochemical assays. All compounds in this library are structurally novel and bioactivity diverse which makes it easier to discover new lead compounds. MCE Novel Bioactive Compound Library, as a supplement of MCE bioactive compound library (HY-L001), is a useful tool to screen new lead compounds.
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 4,918 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes
Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 1,550 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 2,227 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 µM (Ex=485nm，Em=535nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrial membrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .
Eniporide (EMD 96785) is a Na(+)/H(+) exchange (NHE) inhibitor. Eniporide specifically inhibits the NHE-1 isoform. Eniporide improves cardiac performance inhibition associated with myocardial ischemia/reperfusion in animals, and limits infarct size in experimental models. Eniporide regulates cardiac performance and high-energy phosphate content in clinically relevant pig models of CPB and cardiac arrest .
Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2) .
Prokineticin 2 Isoform 2 (human) is a hypothalamic neuropeptide. Prokineticin 2 Isoform 2 (human) decreases food intake and involves in thermoregulation and energy metabolism in rodents. Prokineticin 2 has the potential for the research of hyperglycemia, metabolic syndrome (MetS) and obesity .
Beta-defensin 103 isoform X1, pig is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens .
Beta-defensin 103 isoform X1, pig TFA is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens .
Jingzhaotoxin-III is a potent and selective blocker of Nav1.5 channels, with an IC50 of 348 nM, and shows no effect on other sodium channel isoforms. Jingzhaotoxin-III can selectively inhibit the activation of cardiac sodium channel but not neuronal subtypes, and hopefully represents an important ligand for discriminating cardiac VGSC subtype .
[Asn18] Endothelin-1, human is a peptide. Endothelin-1 is a major isoform of Endothelin and plays an important role for regulation of vascular function .
STAD 2 is a potent and selective disruptor of PKA-RII, with a Kd of 6.2 nM. STAD 2 disrupts interactions between PKA and AKAP in an isoform-selective manner. STAD 2 displays antimalarial activity through a PKA-independent mechanism .
Phoenixin-14 (PNX-14) is one of the endogenous active isoform, and generates anxiolytic effect via the activation of the AHA GnRH system in mice. Phoenixin-14 inhibits ischemia/reperfusion-induced cytotoxicity in microglia .
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3 .
NoxA1ds is a highly efficacious and selective Nox1 (NADPH oxidase isoform 1) inhibitor. NoxA1ds establishes a critical interaction site for Nox1-NOXA1 binding required for enzyme activation. NoxA1ds can be used for the research of hypertension, atherosclerosis and neoplasia .
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3 .
Cacaoidin is a glycosylated lantibiotic isolated from a Streptomyces cacaoi strain. Cacaoidin has potent antibacterial activity against Gram-positive pathogens including Clostridium difficile .
Aprutumab (BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has the potential for solid tumors research .
Ranibizumab (RG-6321) (anti-VEGF) is a humanized anti-VEGF monoclonal antibody fragment and can recognize all VEGF-A isoforms (VEGF110, VEGF121, and VEGF165) . Ranibizumab (anti-VEGF) slows vision loss in vivo and is used for wet age-related macular degeneration (AMD) research .
Ledelabricin alfa is a human proteoglycan 4 (PRG4) isoform A variant. PRG4 is a joint/boundary lubricant. Ledelabricin Alfa can be used for the research arthropathy .
Efdamrofusp alfa is a bispecific fusion protein. Efdamrofusp alfa is capable of neutralizing both VEGF isoforms and C3b/C4b. Efdamrofusp alfa can be used for the research of neovascular age-related macular degeneration (nAMD) and other complement-related ocular conditions .
Tetrahydrobiopterin ((Rac)-Sapropterin) is a cofactor of the aromatic amino acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.
α-Tocotrienol is an isoform of vitamin E and found in vegetables, fruits, seeds, nuts, grains, and oils. Vitamin E plays a role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer .
Palmitoleoyl-CoA can be activated and transported into the mitochondria for metabolism, specifically for β-oxidation. Palmitoleoyl-CoA induces the cardiac mitochondrial membrane permeability transition, which causes mitochondrial dysfunction. Palmitoleoyl-CoA regulates metabolism via allosteric control of AMPK β1-isoforms .
(Z)-Pseudoginsenoside Rh2 is the (Z) isoform of Pseudoginsenoside Rh2 (HY-125825), which is synthesized from Ginsenoside Rh2, possesses anti-cancer activitied .
Bergapten (Standard) is the analytical standard of Bergapten. This product is intended for research and analytical applications. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYPisoforms.
Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
Aprutumab (BAY 1179470) is a fully human FGFR2 monoclonal antibody, which binds to the FGFR2 isoforms FGFR2-IIIb and FGFR2-IIIc. Aprutumab has the potential for solid tumors research .
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum . Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoformCYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM) .
d-Sophoridine ((+)-Sophoridine) is the dextro isoform of Sophoridine (HY-N1373), which is a quinolizidine alkaloid isolated from Leguminous plant Sophora flavescens. Sophoridine induces apoptosis. Sophoridine has the potential to be a novel, potent and selective antitumor agent candidate for pancreatic cancer with well-tolerated toxicity .
(Rac)-Norcantharidin ((Rac)-NCTD) is the isoform of Norcantharidin, which is a synthetic and demethylated anticancer agent derived from Cantharidin (HY-N0209). Norcantharidin has lighter side effects and stronger bioactivity than Cantharidin. And Norcantharidin inhibits cell proliferation, migration and metastasis, and causes apoptosis and autophagy .
Levoleucovorin (Calcium) (Standard) is the analytical standard of Levoleucovorin (Calcium). This product is intended for research and analytical applications. Levoleucovorin Calcium (Calcium levofolinate), a levo isoform of Leucovorin Calcium (HY-13664), possesses antineoplastic effects. Levoleucovorin Calcium is also an augmentor of 5-fluorouracil (HY-90006) cytotoxicity against cancer .
Secologanin (Standard) is the analytical standard of Secologanin. This product is intended for research and analytical applications. Secologanin, a secoiridoid glucoside, is a pivotal terpenoid intermediate in the biosynthesis of biologically active monoterpenoid indole alkaloids such as reserpine, ajmaline, and vinblastine. Secologanin synthase (cytochrome P450 isoform CYP72A1) catalyzes the oxidative cleavage of loganin into Secologanin .
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD) .
α-Tocotrienol (Standard) is the analytical standard of α-Tocotrienol. This product is intended for research and analytical applications. α-Tocotrienol is an isoform of vitamin E and found in vegetables, fruits, seeds, nuts, grains, and oils. Vitamin E plays a role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca 2+ ATPase (SERCA) with IC50s between 5 μM and 50 μM for differing isoforms. Paxilline possesses significant anticonvulsant activity .
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
Gitogenin (Standard) is the analytical standard of Gitogenin. This product is intended for research and analytical applications. Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC)isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells .
Anhydroerythromycin A (Standard) is the analytical standard of Anhydroerythromycin A. This product is intended for research and analytical applications. Anhydroerythromycin A is a degradation product of the macrolide antibiotic erythromycin. Anhydroerythromycin A is formed via degradation of erythromycin in acidic aqueous solutions in vitro as well as in vivo. Anhydroerythromycin A is active against S. aureus and B. cereus in vitro (MICs = 12.5 and 6.25 μg/ml, respectively). Anhydroerythromycin A also inhibits steroid 6β-hydroxylase activity associated with the cytochrome P450 (CYP) isoform CYP3A in human liver microsomes.
Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ) .
Centrin-2 protein plays a critical role in microtubule-organized centromere structure, directing centriole duplication, spindle formation, and regulation of cytokinesis. It ensures genome stability by interacting with CALM1 and CCP110. Centrin-2 Protein, Human (His) is the recombinant human-derived Centrin-2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of Centrin-2 Protein, Human (His) is 171 a.a., with molecular weight of ~20 kDa.
PDK1 protein is a key kinase that controls glucose and fatty acid metabolism by phosphorylating pyruvate dehydrogenase subunits PDHA1 and PDHA2. This molecular switch inhibits pyruvate dehydrogenase, fine-tunes metabolite flux and downregulates aerobic respiration. PDK1 Protein, Human (sf9, His) is the recombinant human-derived PDK1 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of PDK1 Protein, Human (sf9, His) is 408 a.a., with molecular weight of ~45 kDa.
VEGF145 Protein, with limited expression, exhibits specialized distribution and is not broadly present in tissues. Its restricted occurrence implies a specific, context-dependent role in physiological processes. Further research is needed to unveil the specific cellular contexts and functions where VEGF145 actively participates, providing insights into its potential contributions to localized biological activities. VEGF165 Protein, Human (HEK293, C-His) is the recombinant human-derived VEGF165 protein, expressed by HEK293 , with C-10*His labeled tag. The total length of VEGF165 Protein, Human (HEK293, C-His) is 165 a.a., with molecular weight of 20-23 kDa.
PDK4 Protein phosphorylates PDHA1 and PDHA2, inhibiting pyruvate dehydrogenase activity. This reduces glucose utilization, enhances fat metabolism, and helps maintain blood glucose levels during fasting. PDK4 also regulates fatty acid oxidation and biosynthesis, generates reactive oxygen species, protects epithelial cells, and regulates cell proliferation through metabolic regulation. PDK4 Protein, Human (GST) is the recombinant human-derived PDK4 protein, expressed by E. coli , with N-GST labeled tag. The total length of PDK4 Protein, Human (GST) is 411 a.a., .
PDK3 is a metabolic regulator that inhibits pyruvate dehydrogenase through PDHA1 phosphorylation to fine-tune glucose metabolism and affect aerobic respiration. Phosphorylation of PDHA2 adds another layer of control. PDK3 Protein, Mouse (His) is the recombinant mouse-derived PDK3 protein, expressed by E. coli , with N-His labeled tag.
PDK4 protein is a key kinase that regulates glucose and fatty acid metabolism by phosphorylating pyruvate dehydrogenase subunits PDHA1 and PDHA2.This inhibits pyruvate dehydrogenase activity, modulates metabolite flux and inhibits aerobic respiration.PDK4 Protein, Mouse (sf9, His-GST) is the recombinant mouse-derived PDK4 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Centrin-2 protein plays a critical role in microtubule-organized centromere structure, directing centriole duplication, spindle formation, and regulation of cytokinesis. It ensures genome stability by interacting with CALM1 and CCP110. Centrin-2 Protein, Human (HEK293, His) is the recombinant human-derived Centrin-2 protein, expressed by HEK293 , with C-His labeled tag. The total length of Centrin-2 Protein, Human (HEK293, His) is 172 a.a., with molecular weight of ~21.2 kDa.
Intercellular adhesion molecule 4 isoform 3 is expressed on RBCs, erythroid precursor cells, and on other blood cells including T and B cells. Intercellular adhesion molecule 4 isoform 3 belongs to the immunoglobulin superfamily (IgSF) consisting of five members designated ICAM1 to ICAM5. Intercellular adhesion molecule 4 isoform 3 is part of the Rh macromolecular complex consisting of Rh polypeptides (RhD and RhCE) and the Rh-associated glycoprotein (RhAG). Intercellular adhesion molecule 4 isoform 3 maintains close contact between the RBC surface and vascular endothelium and also plays a role in various normal and pathologic conditions, including erythropoiesis and microvascular occlusions during painful crises of sickle cell disease, respectively. ICAM-4 Protein, Human (HEK293, Fc) is the recombinant human-derived ICAM-4 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of ICAM-4 Protein, Human (HEK293, Fc) is 250 a.a., with molecular weight of ~55 & 33 KDa, respectively.
SIRP beta 1 protein negatively regulates receptor tyrosine kinase signaling and recruits SYK for myeloid cell activation. It interacts with TYROBP as a homodimer, facilitating SYK recruitment. This intricate molecular interplay is crucial for modulating myeloid cell activation and regulating cellular signaling. SIRP beta 1 occupies a central position in protein interactions that contribute to its functional role. SIRP Beta 1 Protein, Human (HEK293, His-Avi) is the recombinant human-derived SIRP Beta 1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of SIRP Beta 1 Protein, Human (HEK293, His-Avi) is 340 a.a., with molecular weight of 52-60 kDa.
SIRP beta 1 protein negatively regulates receptor tyrosine kinase signaling and recruits SYK for myeloid cell activation. It interacts with TYROBP as a homodimer, facilitating SYK recruitment. This intricate molecular interplay is crucial for modulating myeloid cell activation and regulating cellular signaling. SIRP beta 1 occupies a central position in protein interactions that contribute to its functional role. SIRP Beta 1 Protein, Human (Biotinylated, HEK293, C-His-Avi) is the recombinant human-derived SIRP Beta 1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of SIRP Beta 1 Protein, Human (Biotinylated, HEK293, C-His-Avi) is 340 a.a., with molecular weight of 55-65 kDa.
EIF5A2 is a translation factor critical for promoting elongation and termination, helping stalled ribosomes encounter specific amino acid environments. EIF5A2 is located between the ribosome exit (E) and peptidyl (P) sites and rescues stalled ribosomes, especially those translating polyproline-containing peptides. EIF5A2 Protein, Human (His) is the recombinant human-derived EIF5A2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of EIF5A2 Protein, Human (His) is 153 a.a., with molecular weight of ~22.0 kDa.
SIRP Beta 1 Protein, an immunoglobulin-like cell surface receptor, crucially negatively regulates receptor tyrosine kinase-coupled signaling processes. It modulates cellular responses to stimuli like cell adhesion, growth factors, or insulin, contributing to maintaining cellular homeostasis and finely tuning signaling pathways associated with receptor tyrosine kinases. SIRP Beta 1 Protein, Human (isoform 3, HEK293, His-Avi) is the recombinant human-derived SIRP Beta 1 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of SIRP Beta 1 Protein, Human (isoform 3, HEK293, His-Avi) is 342 a.a., with molecular weight of 60-70 kDa.
SIRP Beta 1 Protein, an immunoglobulin-like cell surface receptor, crucially negatively regulates receptor tyrosine kinase-coupled signaling processes. It modulates cellular responses to stimuli like cell adhesion, growth factors, or insulin, contributing to maintaining cellular homeostasis and finely tuning signaling pathways associated with receptor tyrosine kinases. SIRP Beta 1 Protein, Human (Biotinylated, isoform 3, HEK293, His-Avi) is the recombinant human-derived SIRP Beta 1 protein, expressed by HEK293 , with C-His, C-Avi labeled tag. The total length of SIRP Beta 1 Protein, Human (Biotinylated, isoform 3, HEK293, His-Avi) is 342 a.a., with molecular weight of 55-68 kDa.
The FGF-11 isoform 1 protein is thought to play an important role in the development and function of the nervous system. Its presence indicates involvement in complex processes responsible for establishing and maintaining neural structure and activity. Animal-Free FGF-11 isoform 1 Protein, Human (His) is the recombinant human-derived animal-FreeFGF-11 isoform 1 protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free FGF-11 isoform 1 Protein, Human (His) is 225 a.a., with molecular weight of ~25.81 kDa.
FGF-11 isoform 2 protein is a member of the fibroblast growth factor family, characterized by broad mitotic and cell survival activities, affecting embryonic development, cell growth, morphogenesis, tissue repair, and tumor growth. Its specific function has not yet been determined, but the expression pattern of its mouse homolog suggests a role in nervous system development. Animal-Free FGF-11 isoform 2 Protein, Human (His) is the recombinant human-derived animal-FreeFGF-11 isoform 2 protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free FGF-11 isoform 2 Protein, Human (His) is 166 a.a., with molecular weight of ~19.34 kDa.
The COX4I1 protein is a component of cytochrome c oxidase, the final enzyme in the mitochondrial electron transport chain responsible for oxidative phosphorylation. COX4I1 Protein, Human (His-SUMO) is the recombinant human-derived COX4I1 protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of COX4I1 Protein, Human (His-SUMO) is 147 a.a., with molecular weight of ~33.2 kDa.
Casein kinase I gamma-2 Protein, Human (His) is an approximately 55.0 kDa human casein kinase I isoform gamma-2 protein with a His-flag expressed in E. coli. Human Casein kinase I isoform gamma-2 may exhibit overexpression during tumorigenesis and belongs to the CKI family.
B7-2/CD86 Protein, Cynomolgus/Rhesus Macaque (HEK293, His), a second CTLA4 ligand expressed on murine B cells, can serve as a costimulatory molecule for T cell activation.
The PIP4K2A protein phosphorylates phosphatidylinositol 5-phosphate to form phosphatidylinositol 4,5-bisphosphate. PIP4K2A Protein, Human (HEK293, His) is the recombinant human-derived PIP4K2A protein, expressed by HEK293 , with C-6*His labeled tag.
GPNMB, also known as Osteoactivin, is suggested to potentially function as a melanogenic enzyme. GPNMB/Osteoactivin Protein, Human (Isoform 2, HEK293, His) is the recombinant human-derived GPNMB/Osteoactivin protein, expressed by HEK293 , with C-His labeled tag. The total length of GPNMB/Osteoactivin Protein, Human (Isoform 2, HEK293, His) is 453 a.a., with molecular weight of 85-90 kDa.
GPNMB, also known as Osteoactivin, is suggested to potentially function as a melanogenic enzyme. GPNMB/Osteoactivin Protein, Human (Isoform 2, HEK293, Fc) is the recombinant human-derived GPNMB/Osteoactivin protein, expressed by HEK293 , with C-hFc labeled tag. The total length of GPNMB/Osteoactivin Protein, Human (Isoform 2, HEK293, Fc) is 453 a.a., with molecular weight of ~107.5 kDa.
GABARAP Protein is essential for regulating ubiquitination and degradation of TIAM1, a guanyl-nucleotide exchange factor (GEF) involved in RAC1 activation and downstream signaling. The D6/7 E3 ubiquitin ligase complex, where GABARAP is a key component, contributes to diverse biological processes, including cytoskeletal organization, cell migration, proliferation, and apoptosis. GABARAP Protein, Human (His-MBP) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, N-MBP labeled tag. The total length of GABARAP Protein, Human (His-MBP) is 117 a.a., with molecular weight of 49-58 kDa.
EIF4A2, an ATP-dependent RNA helicase, is a vital subunit of the eIF4F complex, pivotal in cap recognition and mRNA binding to ribosomes. In translation initiation, EIF4A2 crucially unwinds RNA secondary structures in mRNA 5'-UTRs. This activity facilitates small ribosomal subunit binding and efficient scanning for the initiator codon, orchestrating translation initiation. EIF4A2 Protein, Human (GST) is the recombinant human-derived EIF4A2 protein, expressed by E. coli, with N-GST labeled tag. The total length of EIF4A2 Protein, Human (GST) is 407 a.a., with molecular weight of 73.4 kDa.
GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (GST) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-GST labeled tag. The total length of GABARAP Protein, Human (GST) is 117 a.a., with molecular weight of ~37.0 kDa.
FGF-14 Protein likely plays a crucial role in the development and functioning of the nervous system, contributing to intricate processes underlying neural structure and activity. Its interaction with SCN8A suggests potential involvement in modulating this sodium channel's activity, emphasizing its intricate role in neurophysiology. FGF-14 Protein, Human (isoform 1B) is the recombinant human-derived FGF-14 protein, expressed by E. coli , with tag free.
Neuregulin-4 (NRG4) Protein, a low-affinity ligand for the ERBB4 tyrosine kinase receptor, serves as a signaling molecule that recruits ERBB1 and ERBB2 coreceptors. This recruitment leads to ligand-stimulated tyrosine phosphorylation and activation of the ERBB receptors. NRG4 specifically interacts with the ERBB4 receptor, mediating cellular responses through its activation, without binding to ERBB1, ERBB2, and ERBB3 receptors. Neuregulin-4/NRG4 Protein, Human is the recombinant human-derived Neuregulin-4/NRG4 protein, expressed by E. coli , with tag free. The total length of Neuregulin-4/NRG4 Protein, Human is 61 a.a., with molecular weight of ~6.7 KDa.
GABARAP (gamma-aminobutyric acid receptor-associated protein) is a protein that performs multiple functions within cells. As a ubiquitin-like modifier, it participates in the intracellular transport of GABA(A) receptors and interacts with the cytoskeleton. GABARAP Protein, Human (His, Fc) is the recombinant human-derived GABARAP protein, expressed by E. coli , with N-His, C-hFc labeled tag. The total length of GABARAP Protein, Human (His, Fc) is 117 a.a., with molecular weight of ~50 kDa.
Follistatin (FST) is a regulator of TGFβ family signaling and acts by selectively binding to TGFβ family ligands and preventing ligand binding to the receptor complex. Follistatin has the ability to suppress the follicle stimulating hormone (FSH). Follistatin/FST Protein, Human (HEK293, His) is produced in HEK293 cells with six C-Terminal His-tags. It consists of 288 amino acids (G30-N317).
FSHR, a G protein-coupled receptor, specifically recognizes follitropin (FSH) and activates PI3K-AKT and ERK1/ERK2 pathways by promoting cAMP production. Operating as a homotrimer, FSHR binds the heterodimeric FSH hormone, forming a functional unit for signal transduction. Its regulatory mechanisms involve interaction with ARRB2, and independently of FSH stimulation, it engages with APPL2, demonstrating versatility in diverse cellular contexts. FSHR Protein, Human (His) is the recombinant human-derived FSHR protein, expressed by E. coli , with N-6*His labeled tag.
PITPNA Protein catalyzes phosphatidylinositol (PI) and phosphatidylcholine (PC) transfer between membranes, displaying a preference for shorter saturated or monosaturated acyl chains at sn-1 and sn-2 positions. For PC, the preference order is C16:1 > C16:0 > C18:1 > C18:0 > C20:4, and for PI, it is C16:1 > C16:0 > C18:1 > C18:0 > C20:4 > C20:3. PITPNA Protein, Human (His) is the recombinant human-derived PITPNA protein, expressed by E. coli , with N-6*His labeled tag. The total length of PITPNA Protein, Human (His) is 270 a.a., with molecular weight of 16 & 22 & 38 kDa, respectively.
CSNK1E protein is a casein kinase that preferentially phosphorylates acidic proteins such as casein. CSNK1E Protein, Human (sf9, GST) is the recombinant human-derived CSNK1E, expressed by Sf9 insect cells , with GST labeled tag. The total length of CSNK1E Protein, Human (sf9, GST) is 415 a.a.,
Casein kinase I α is a member of casein kinases that exhibits a preference for phosphorylation of acidic proteins such as casein. It phosphorylates many substrates, including CTNNB1 at "Ser-45" involved in Wnt signaling. Casein Kinase I alpha Protein, Human (sf9, GST) is the recombinant human-derived Casein Kinase I alpha protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of Casein Kinase I alpha Protein, Human (sf9, GST) is 337 a.a., with molecular weight of ~62 kDa.
The calcineurin A/PPP3CA protein is a calcium-dependent, calmodulin-stimulated phosphatase. PPP3CA inhibits MAP3K14/NIK signaling and SLC9A1 activity. PPP3CA is involved in processes such as kidney development, salivary enzyme secretion, hippocampal homosynaptic depotentiation, keratinocyte survival, bone formation, and T cell proliferation. Calcineurin A/PPP3CA Protein, Human (sf9, His) is the recombinant human-derived Calcineurin A/PPP3CA protein, expressed by Sf9 insect cells , with N-His labeled tag.
The CSNK1G1 protein is a member of the casein kinase family that preferentially phosphorylates acidic proteins, including casein, exhibiting broad substrate specificity. Functionally, it actively participates in the Wnt signaling pathway and regulates cellular responses. CSNK1G1 Protein, Human (sf9, GST) is the recombinant human-derived CSNK1G1, expressed by Sf9 insect cells , with GST labeled tag. The total length of CSNK1G1 Protein, Human (sf9, GST) is 421 a.a.,
PPM1A is a multifunctional enzyme whose enzymatic activity exhibits broad specificity. It acts as a negative regulator of TGF-β signaling by dephosphorylating SMAD2 and SMAD3, leading to their dissociation from SMAD4, nuclear export of SMAD, and termination of TGF-β-mediated signaling. PPM1A Protein, Mouse (His) is the recombinant mouse-derived PPM1A protein, expressed by E. coli , with C-His labeled tag.
The CSNK1G1 protein is a member of the casein kinase family that preferentially phosphorylates acidic proteins, including casein, exhibiting broad substrate specificity. Functionally, it actively participates in the Wnt signaling pathway and regulates cellular responses. CSNK1G1 Protein, Human (sf9, His-GST) is the recombinant human-derived CSNK1G1 protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
4-1BB (CD137; TNFRSF9), a receptor of TNFSF9/4-1BBL, belongs to the tumor necrosis factor (TNF) receptor superfamily. 4-1BB is helpful for T cell activation and development, and also induces peripheral mononuclear cell proliferation and migration to the tumor microenvironment. 4-1BB is also involved in enhancing Nrf2 and NF-κB pathway mediated apoptosis of endothelial cells. Mouse 4-1BB protein is a surface glycoprotein with a transmembrane domain (188-208 a.a.). 4-1BB/TNFRSF9 Protein, Mouse (isoform 2, HEK293, Fc) has 188 amino acids (V24-L211), produced by HEK293 cells with C-terminal rFc-tag.
AMELX Protein plays a central role in biomineralization, shaping crystallite formation during the secretory stage of tooth enamel development. Its pivotal function extends to structurally organizing and mineralizing developing enamel, emphasizing its significance in dental tissue architecture. Interactions with KRT5 suggest its involvement in molecular networks contributing to the orchestrated development and mineralization of tooth enamel. AMELX Protein, Human (His-SUMO) is the recombinant human-derived AMELX protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of AMELX Protein, Human (His-SUMO) is 175 a.a., with molecular weight of ~35.9 kDa.
The CK1γ3 protein is a serine/threonine protein kinase in the casein kinase family that prefers acidic proteins, including casein. It has broad substrate specificity and can phosphorylate a variety of proteins, affecting diverse cellular processes. CK1γ3 Protein, Human (Sf9) is the recombinant human-derived CK1γ3 protein, expressed by Sf9 insect cells , with tag free. The total length of CK1γ3 Protein, Human (Sf9) is 446 a.a., .
CYB5B Protein, Human (HEK293, His) is the recombinant human-derived CYB5B protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CYB5B Protein, Human (HEK293, His) is 107 a.a., with molecular weight of ~22.0 kDa.
Periostin/OSF-2 Protein, a multifaceted regulator, induces cell attachment and spreading, participates in cell adhesion, and enhances BMP1 incorporation into the fibronectin matrix. It forms a structural homodimer and interacts with BMP1 and fibronectin. This interplay positions Periostin as a key player in regulating cellular and tissue functions, including cell adhesion, tissue architecture, and extracellular matrix modulation. Periostin/OSF-2 Protein, Rat (HEK293, His) is the recombinant rat-derived Periostin/OSF-2 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Periostin/OSF-2 Protein, Rat (HEK293, His) is 777 a.a., with molecular weight of approximately 95 kDa.
The CK1d protein is an important serine/threonine protein kinase that complexly controls cellular processes such as Wnt signaling, DNA repair, and circadian rhythms. Its versatility is evident in phosphorylating a variety of proteins, including connexin-43/GJA1, MAP1A, p53/TP53, and YAP1. CK1d Protein, Human (Sf9, GST) is the recombinant human-derived CK1d protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of CK1d Protein, Human (Sf9, GST) is 414 a.a., .
The CK1γ3 protein is a serine/threonine protein kinase in the casein kinase family that prefers acidic proteins, including casein. It has broad substrate specificity and can phosphorylate a variety of proteins, affecting diverse cellular processes. CK1γ3 Protein, Human (Sf9, GST) is the recombinant human-derived CK1γ3 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of CK1γ3 Protein, Human (Sf9, GST) is 446 a.a., .
Microtubule-associated protein tau (MAPT) plays a key role in promoting microtubule assembly and stability, suggesting its potential contribution to the establishment of neuronal polarity.The C terminus binds to axonal microtubules, whereas the N terminus interacts with neuroplasmic membrane components, serving as a key linker protein between these structures.PNS-Tau/MAPT Protein, Mouse (HEK293, His) is the recombinant mouse-derived PNS-Tau/MAPT protein, expressed by HEK293 , with N-10*His labeled tag.
C protein cardiac muscle Isoform; C-protein; cardiac muscle Isoform; Cardiac MyBP C; Cardiac MyBP-C; Cardiac myosin binding protein C ; cardiac-type; CMH4; FHC; MYBP C; MYBPC; MYBPC3; Myosin binding protein C cardiac; Myosin binding protein C cardiac-type; Myosin-binding protein C; myosin-binding protein C cardiac type; MYPC3_HUMAN
MYBPC3 Protein, positioned in the crossbridge region of vertebrate striated muscle A bands, binds to myosin heavy chain (MHC), F-actin, and native thin filaments, influencing actin-activated myosin ATPase. Its presence suggests potential modulation of muscle contraction, indicating a functional impact on the contractile apparatus, or a structural role in muscle fibers. MYBPC3 Protein, Human (His-SUMO) is the recombinant human-derived MYBPC3 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag.
C protein cardiac muscle Isoform; C-protein; cardiac muscle Isoform; Cardiac MyBP C; Cardiac MyBP-C; Cardiac myosin binding protein C ; cardiac-type; CMH4; FHC; MYBP C; MYBPC; MYBPC3; Myosin binding protein C cardiac; Myosin binding protein C cardiac-type; Myosin-binding protein C; myosin-binding protein C cardiac type; MYPC3_HUMAN
MYBPC3 Protein, positioned in the crossbridge region of vertebrate striated muscle A bands, binds to myosin heavy chain (MHC), F-actin, and native thin filaments, influencing actin-activated myosin ATPase. Its presence suggests potential modulation of muscle contraction, indicating a functional impact on the contractile apparatus, or a structural role in muscle fibers. MYBPC3 Protein, Human (HEK293, His) is the recombinant human-derived MYBPC3 protein, expressed by HEK293 , with C-6*His labeled tag.
Microtubule-associated protein tau is a microtubule-associated protein found in large numbers in neurons of the central nervous system (CNS). MAPT promotes microtubule assembly and stability and may be involved in the establishment and maintenance of neuronal polarity. Overexpression of MAPT is associated with a poor prognosis of prostate cancer. MAPT has been linked to neurological disorders such as Alzheimer's and Parkinson's disease. Tau-F/2N4R Protein, Human (HEK293, His) is the recombinant human-derived Tau-F/2N4R protein, expressed by HEK293 , with N-10*His labeled tag.
Tau/MAPT proteins crucially promote microtubule assembly and stability, which are critical for neuronal polarity. Structurally, its C terminus binds to axonal microtubules and its N terminus binds to neuroplasmic membrane components, suggesting its role as a connexin connecting microtubules to the plasma membrane. Tau-A/MAPT Protein, Macaca mulatta (HEK293, His) is the recombinant Rhesus Macaque-derived Tau-A/MAPT protein, expressed by HEK293 , with N-10*His labeled tag.
Microtubule-associated protein tau (MAPT) critically promotes microtubule assembly and stability, influencing neuronal polarity by acting as an important junction protein. Its dual role involves C-terminal binding to axonal microtubules and N-terminal binding to neuroplasmic membrane components. Tau-A/SC1 Protein, Rat (HEK293, His) is the recombinant rat-derived Tau-A/SC1 protein, expressed by HEK293 , with N-10*His labeled tag.
C-type lectin domain-containing protein is a soluble mannose-binding protein in serum which belongs to the collectin family and is an important element in the innate immune system. C-type lectin domain-containing protein exerts mannose-binding, calcium-dependent protein binding and identical protein binding activity. MBL2/COLEC1 Protein, Mouse (HEK293) is the recombinant mouse-derived MBL2/COLEC1 protein, expressed by HEK293 , with tag free.
PPM1A is a multifunctional enzyme that negatively regulates multiple signaling pathways. It significantly attenuates TGF-β signaling by dephosphorylating SMAD2 and SMAD3, leading to their dissociation from SMAD4, nuclear export, and signal termination. PPM1A Protein, Human (His) is the recombinant human-derived PPM1A protein, expressed by E. coli , with C-6*His labeled tag.
CSNK1E protein is a casein kinase that preferentially phosphorylates acidic proteins such as casein. CSNK1E Protein, Human (His) is the recombinant human-derived CSNK1E protein, expressed by E. coli , with N-6*His labeled tag. The total length of CSNK1E Protein, Human (His) is 416 a.a., with molecular weight of ~51.3 kDa.
CSNK1E, a member of the casein kinase family, is characterized by its preferential phosphorylation of acidic proteins, particularly caseins. The protein plays a pivotal role in Wnt signaling, as evidenced by its phosphorylation of DVL1 and DVL2, contributing to the intricate regulation of this pathway. Beyond its involvement in Wnt signaling, CSNK1E serves as a central component of the circadian clock, influencing the circadian period length by orchestrating the speed and rhythmicity of PER1 and PER2 phosphorylation. Acting in equilibrium with PP1, it governs the nuclear transport and degradation of PER1 and PER2, thereby intricately regulating the circadian rhythm. Additionally, CSNK1E demonstrates its regulatory influence by inhibiting cytokine-induced granulocytic differentiation, further emphasizing its multifaceted roles in cellular processes. CSNK1E Protein, Human (P. pastoris, His) is the recombinant human-derived CSNK1E protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of CSNK1E Protein, Human (P. pastoris, His) is 416 a.a., with molecular weight of 49.3 kDa.
YWHAH proteins are adapter proteins in multiple signaling pathways that recognize phosphoserine or phosphothreonine motifs and regulate chaperone activity upon binding. It negatively regulates PDPK1 kinase activity and interacts with nuclear hormone receptors (AR, ESR1, ESR2, MC2R, NR3C1, NRIP1, PPARBP, THRA) and cofactors. 14-3-3 eta Protein, Human (GST) is the recombinant human-derived YWHAH protein, expressed by E. coli , with N-GST labeled tag.
Casein kinase I gamma-2 is a serine/threonine protein kinase that targets acidic proteins and phosphorylates a variety of substrates, such as COL4A3BP/CERT, MTA1 and SMAD3, especially destabilizing SMAD3 and inhibiting TGF- beta reaction. Hyperphosphorylation of COL4A3BP/CERT disrupts ER-to-Golgi transport and affects the synthesis of ceramide and sphingomyelin. Casein Kinase I gamma-2 Protein, Human (sf9, His) is the recombinant human-derived Casein Kinase I gamma-2 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of Casein Kinase I gamma-2 Protein, Human (sf9, His) is 398 a.a., with molecular weight of ~48 kDa.
As the catalytic subunit of phosphorylase b kinase (PHK), PHKG2 plays a crucial role in the neural and hormonal regulation of glycogenolysis (glycogen breakdown) by phosphorylating and activating glycogen phosphorylase. Furthermore, PHKG2 has a potential role in regulating testicular glycogenolysis. PHKG2 Protein, Human (Sf9, GST) is the recombinant human-derived PHKG2 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of PHKG2 Protein, Human (Sf9, GST) is 405 a.a., .
ATP5F1A is an important component of mitochondrial ATP synthase (complex V) that coordinates ATP production from ADP by utilizing the transmembrane proton gradient. As part of the F-type ATPase, the α and β subunits of ATP5F1A form the catalytic core to achieve ATP hydrolysis. ATP5F1A Protein, Human (His) is the recombinant human-derived ATP5F1A protein, expressed by E. coli , with N-6*His labeled tag. The total length of ATP5F1A Protein, Human (His) is 510 a.a., with molecular weight of ~59.2 kDa.
4-1BB/TNFRSF9 Protein, crucial with cytokine and protein binding, influences processes like interleukin regulation and cell proliferation.Located externally on the plasma membrane, its expression is notably high in the placenta adult (RPKM 139.4), emphasizing its significance in specific physiological contexts.As the ortholog to human TNFRSF9, it suggests evolutionary conservation of functions across species.4-1BB/TNFRSF9 Protein, Mouse (isoform 2, HEK293, His) is the recombinant mouse-derived 4-1BB/TNFRSF9 protein, expressed by HEK293 , with C-His labeled tag.
Mucin-1/MUC1 protein and its α subunit have dual functions of adhesion and anti-adhesion proteins, forming a protective layer on epithelial cells. At the same time, the β subunit and its C-terminal domain participate in cell signaling through phosphorylation and protein-protein interactions. Mucin-1/MUC1 Isoform Y Protein, Human (HEK293, Fc) is the recombinant human-derived Mucin-1/MUC1 Isoform Y protein, expressed by HEK293 , with C-hFc labeled tag. The total length of Mucin-1/MUC1 Isoform Y Protein, Human (HEK293, Fc) is 135 a.a., with molecular weight of 55-65 kDa.
The SLC15A2 protein is a proton-coupled amino acid transporter that prefers dipeptides and transports oligopeptides containing 2 to 4 amino acids. The stoichiometric ratio of protons to peptides is 2:1 or 3:1, which helps the kidneys absorb dipeptides and tripeptides. SLC15A2 Protein, Human (HEK293, His, MBP, FLAG) is the recombinant human-derived SLC15A2 protein, expressed by HEK293 , with N-MBP, C-Flag, N-8*His labeled tag. The total length of SLC15A2 Protein, Human (HEK293, His, MBP, FLAG) is 728 a.a., .
The SLC15A2 protein is a proton-coupled amino acid transporter that prefers dipeptides and transports oligopeptides containing 2 to 4 amino acids. The stoichiometric ratio of protons to peptides is 2:1 or 3:1, which helps the kidneys absorb dipeptides and tripeptides. SLC15A2 Protein, Human (Sf9, His, MBP, FLAG) is the recombinant human-derived SLC15A2 protein, expressed by Sf9 insect cells , with N-MBP, C-Flag, N-8*His labeled tag. The total length of SLC15A2 Protein, Human (Sf9, His, MBP, FLAG) is 728 a.a., .
The SLC15A2 protein is a proton-coupled amino acid transporter that prefers dipeptides and transports oligopeptides containing 2 to 4 amino acids. The stoichiometric ratio of protons to peptides is 2:1 or 3:1, which helps the kidneys absorb dipeptides and tripeptides. SLC15A2 Protein, Human (Sf9, His, Strep, FLAG) is the recombinant human-derived SLC15A2 protein, expressed by Sf9 insect cells , with N-Strep, C-Flag, N-8*His labeled tag. The total length of SLC15A2 Protein, Human (Sf9, His, Strep, FLAG) is 728 a.a., .
Protein Phosphatase 1G; Protein Phosphatase 1C; Protein Phosphatase 2C Isoform Gamma; PP2C-Gamma; Protein Phosphatase Magnesium-Dependent 1 Gamma; PPM1G; PPM1C
PP1MG Protein, a member of PPM family of serine/threonine phosphatases, has an important role in controlling cell cycle progression. PP1MG Proteinregulates the phosphorylation of SRSF3 in hepatocellular carcinoma (HCC) and contributes to the proliferation, invasion, and metastasis of HCC. PP1MG Protein forms a distinct holoenzyme complex with the PP2A regulatory subunit B56δ. B56δ‐PPM1G dephosphorylates α‐catenin at serine 641, which is necessary for the appropriate assembly of adherens junctions and the prevention of aberrant cell migration. PP1MG Protein, Human (His) is the recombinant human-derived PP1MG protein, expressed by E. coli , with C-6*His labeled tag. The total length of PP1MG Protein, Human (His) is 230 a.a., with molecular weight of ~30.0 kDa.
ERK3 Protein, an atypical MAPK, phosphorylates MAP2 and MAPKAPK5. Interacting with MAPKAPK5, ERK3/MAPK6 undergoes Ser-189 phosphorylation, facilitating MAPKAPK5 activation. Activated MAPKAPK5 reciprocally phosphorylates ERK3/MAPK6. The complex's precise functional implications, especially in cell cycle entry, remain elusive. ERK3 Protein, Human is the recombinant human-derived ERK3 protein, expressed by E. coli , with tag free. The total length of ERK3 Protein, Human is 319 a.a., .
ATP synthase alpha chain; ATP synthase alpha chain; mitochondrial; ATP synthase subunit alpha; ATP synthase subunit alpha mitochondrial; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit 1; cardiac muscle; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit; 1; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit; Isoform 1; cardiac muscle; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit; Isoform 2; non-cardiac muscle-like 2; ATP sythase F1 ATPase; alpha subunit; ATP5A; Atp5a1; ATP5AL2; ATPA_HUMAN; ATPM; Epididymis secretory sperm binding protein Li 123m; hATP1; HEL-S-123m; MC5DN4; mitochondrial; Mitochondrial ATP synthetase; Mitochondrial ATP synthetase oligomycin resistant; Modifier of Min 2; Modifier of Min 2 mouse homolog; Modifier of Min 2; mouse; homolog of; MOM2; OMR; ORM; OTTHUMP00000163475
ATP5F1A is an important component of mitochondrial ATP synthase (complex V) that coordinates ATP production from ADP by utilizing the transmembrane proton gradient. As part of the F-type ATPase, the α and β subunits of ATP5F1A form the catalytic core to achieve ATP hydrolysis. ATP5F1A Protein, Human (His-SUMO) is the recombinant human-derived ATP5F1A protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of ATP5F1A Protein, Human (His-SUMO) is 510 a.a., with molecular weight of ~71.2 kDa.
ETS1/EWSR2 Protein, a transcription factor, directly regulates cytokine and chemokine gene expression in diverse cellular contexts. It controls lymphoid cell differentiation, survival, and proliferation, possibly impacting angiogenesis by regulating genes controlling endothelial cell migration and invasion. Additionally, it acts as a dominant-negative for isoform c-ETS-1A. ETS1/EWSR2 Protein, Human (His) is the recombinant human-derived ETS1/EWSR2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of ETS1/EWSR2 Protein, Human (His) is 272 a.a., with molecular weight of ~36 kDa.
ERK3 Protein, an atypical MAPK, phosphorylates MAP2 and MAPKAPK5. Interacting with MAPKAPK5, ERK3/MAPK6 undergoes Ser-189 phosphorylation, facilitating MAPKAPK5 activation. Activated MAPKAPK5 reciprocally phosphorylates ERK3/MAPK6. The complex's precise functional implications, especially in cell cycle entry, remain elusive. ERK3 Protein, Human (His) is the recombinant human-derived ERK3 protein, expressed by E. coli , with N-6*His labeled tag. The total length of ERK3 Protein, Human (His) is 319 a.a., .
Versican Isoform V3 Protein, involved in intercellular signaling, connects cells to the extracellular matrix, regulating cell motility, growth, and differentiation. It binds hyaluronic acid and interacts with FBLN1. Versican Isoform V0 Protein, Human (His, B2M, Myc) is the recombinant human-derived Versican Isoform V0, expressed by E. coli , with N-B2M, C-Myc, N-10*His labeled tag. ,
IL-2R gamma (CD132), a type I cytokine receptor expressed on leucocyte subsets, is a receptor for IL-2. IL-2R gamma forms heterodimer with IL-2R beta, and increases the affinity of IL-2R beta for IL-2. IL-2R gamma takes part in inflammatory response and mediates activation of the cells . IL-2R gamma plays an important role in the development, activation, proliferation, differentiation and regulation of lymphocytes and other cell types. IL-2R gamma/CD132 Protein, Mouse (HEK293, His) is a recombinant mice extracellular region of IL-2R gamma (S25-A263) with a C-Terminal 6*His tag, which is produced in HEK293 cells.
MAPK4, an atypical MAPK protein, phosphorylates microtubule-associated protein 2 (MAP2) and MAPKAPK5, forming a complex with intricate phosphorylation events. Interaction with MAPKAPK5 leads to ERK3/MAPK6 phosphorylation at Ser-189, activating MAPKAPK5, which reciprocally phosphorylates ERK3/MAPK6. The specific cellular role of this interplay, while unclear, suggests ERK3's potential involvement in promoting entry into the cell cycle. MAPK4 Protein, Human (Sf9, His, GST) is the recombinant human-derived MAPK4 protein, expressed by Sf9 insect cells , with N-8*His, N-GST labeled tag. The total length of MAPK4 Protein, Human (Sf9, His, GST) is 586 a.a., .
CSNK1A1L Protein, Human (sf9, His, GST) is the recombinant human-derived CSNK1A1L, expressed by Sf9 insect cells , with His, GST labeled tag. The total length of CSNK1A1L Protein, Human (sf9, His, GST) is 336 a.a.,
The EIF1AX protein is an important member of the 43S preinitiation complex (43S PIC) and is responsible for coordinating mRNA cap-proximal binding, scanning the 5'-untranslated region, and pinpointing the start codon. EIF1AX Protein, Human (His) is the recombinant human-derived EIF1AX protein, expressed by E. coli , with N-6*His labeled tag. The total length of EIF1AX Protein, Human (His) is 144 a.a., with molecular weight of ~22.0 kDa.
PHKG1 is the catalytic subunit of phosphorylase b kinase (PHK), which plays a key role in the neural and hormonal regulation of glycogenolysis (glycogen breakdown) by phosphorylating and activating glycogen phosphorylase. PHKG1 Protein, Human (Active, sf9, GST) is the recombinant human-derived PHKG1, expressed by Sf9 insect cells , with GST labeled tag. ,
Casein kinase I α is a member of casein kinases that exhibits a preference for phosphorylation of acidic proteins such as casein. It phosphorylates many substrates, including CTNNB1 at "Ser-45" involved in Wnt signaling. CSNK1A1 Protein, Human (sf9, His, Strep) is the recombinant human-derived CSNK1A1, expressed by Sf9 insect cells , with Strep, His labeled tag. The total length of CSNK1A1 Protein, Human (sf9, His, Strep) is 336 a.a.,
SLC25A5; ADP/ATP translocase 2; ADP; ATP carrier protein 2; ADP; ATP carrier protein; fibroblast Isoform; Adenine nucleotide translocator 2; ANT 2; Solute carrier family 25 member 5
The SLC25A5 protein is an ADP:ATP antiporter on the inner mitochondrial membrane that imports ADP for ATP synthesis and exports ATP for cellular processes. It operates via an alternating access mechanism, cycling between a cytoplasmic open state and a stromal open state. SLC25A5 Protein, Human (Sf9, His, MBP, FLAG) is the recombinant human-derived SLC25A5 protein, expressed by Sf9 insect cells , with N-MBP, C-Flag, N-8*His labeled tag. The total length of SLC25A5 Protein, Human (Sf9, His, MBP, FLAG) is 297 a.a., .
ERK1 protein is an important serine/threonine kinase in the MAP kinase pathway and cooperates with MAPK1/ERK2 to activate the MAPK/ERK cascade. Stimulated by KIT and KITLG/SCF, this pathway plays a key role in cell growth, adhesion, survival, and differentiation. ERK1 Protein, Human (GST) is the recombinant human-derived ERK1 protein, expressed by E. coli , with N-GST labeled tag. The total length of ERK1 Protein, Human (GST) is 378 a.a., .
CD40 protein is a TNFSF5/CD40LG receptor that transduces signals through TRAF6 and MAP3K8-mediated pathways, activates ERK in macrophages and B cells, and induces immunoglobulin secretion. CD40 exists as monomers and homodimers and interacts with TRAF proteins (TRAF1, TRAF2, TRAF3, TRAF5, and TRAF6). CD40 Protein, Human (Biotinylated, HEK293, His-Avi) is the recombinant human-derived CD40 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of CD40 Protein, Human (Biotinylated, HEK293, His-Avi) is 173 a.a., with molecular weight of 35-40 kDa.
rHuMyelin protein zero-like protein 1/MPZL1, His; Myelin protein zero-like 1; Isoform CRA_b; cDNA FLJ78597; highly similar to Homo sapiens myelin protein zero-like 1 (MPZL1); transcript variant 1; mRNA ; cDNA; FLJ96614; Homo sapiens myelin protein zero-like 1 (MPZL1); Mrna
MPZL1 protein is a cell surface receptor that participates in signal transduction by recruiting PTPN11/SHP-2 to the cell membrane. MPZL1 Protein, Human (HEK293, His) is the recombinant human-derived MPZL1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of MPZL1 Protein, Human (HEK293, His) is 127 a.a., with molecular weight of 20-28 kDa.
PIK3CA Protein, Human (Active, Sf9, His, Strep) is the recombinant human-derived PIK3CA, expressed by Sf9 insect cells , with Strep, His labeled tag. ,
The BTK protein is a key non-receptor tyrosine kinase that is essential for B lymphocyte development and signaling. After BCR activation, BTK initiates a cascade reaction, phosphorylates PLCG2 and activates downstream pathways, affecting calcium mobilization and PKC activation. BTK Protein, Human (Sf9, His) is the recombinant human-derived BTK protein, expressed by Sf9 insect cells , with N-10*His labeled tag.
NRG1 Protein is a direct ligand for ERBB3 and ERBB4 tyrosine kinase receptors. Concomitantly recruits ERBB1 and ERBB2 coreceptors, resulting in ligand-stimulated tyrosine phosphorylation and activation of the ERBB receptors. Perform diverse functions such as inducing growth and differentiation of epithelial, glial, neuronal, and skeletal muscle cells. Binds to ERBB4 and ERBB3. Neuregulin-1/NRG1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Neuregulin-1/NRG1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of Neuregulin-1/NRG1 Protein, Mouse (HEK293, His) is 227 a.a..
PIP4K2B Protein actively synthesizes phosphatidylinositol 4,5-bisphosphate, preferring GTP over ATP in PI(5)P phosphorylation, with enzymatic activity linked to physiological GTP levels. Its unique GTP-sensing ability critically aids metabolic adaptation. PIP4K2B, part of PIP4Ks, negatively influences insulin signaling via a catalytic-independent mechanism, interacting with PIP5Ks to suppress PIP5K-mediated PtdIns(4,5)P2 synthesis, hindering insulin-dependent conversion to PtdIns(3,4,5)P3. This multifaceted role emphasizes PIP4K2B's significance in modulating key signaling pathways for cellular homeostasis and metabolic responsiveness. PIP4K2B Protein, Human (His) is the recombinant human-derived PIP4K2B protein, expressed by E. coli, with N-10*His labeled tag. The total length of PIP4K2B Protein, Human (His) is 415 a.a., with molecular weight of 53.3 kDa.
Trifluoperazine N-glucuronide-d3 is deuterium labeled Trifluoperazine N-Glucuronide. Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation[1].
Fenofibrate-d6 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
Cilostazol-d11 is the deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
Cilostazol-d4 is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].
SAICAR-d is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions[1][2].
Gemfibrozil-d6 is the deuterium labeled Gemfibrozil. Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively .
Fenofibrate-d4 is the deuterium labeled Fenofibrate[1]. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively[2][3].
Fenofibrate-13C6 is a deuterated labeled Fenofibrate . Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment[1][2].
Fipronil- 13C6 is the 13C-labeled Fipronil. Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC50s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
CPT1A Antibody is an unconjugated, approximately 86 kDa, rabbit-derived, anti-CPT1A polyclonal antibody. CPT1A Antibody can be used for: WB, ELISA expriments in mouse, and predicted: human, rat background without labeling.
PDK2 Antibody (YA1395) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1395), targeting PDK2, with a predicted molecular weight of 46 kDa (observed band size: 46 kDa). PDK2 Antibody (YA1395) can be used for WB, IHC-P, ICC/IF, IP, FC experiment in human, mouse, rat background.
ACTN3; Alpha-actinin-3; Alpha-actinin skeletal muscle Isoform 3; F-actin cross-linking protein
WB, IHC-F, IHC-P, ICC/IF
Human, Mouse, Rat
ACTN3 Antibody (YA1997) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1997), targeting ACTN3, with a predicted molecular weight of 103 kDa (observed band size: 103 kDa). ACTN3 Antibody (YA1997) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human, mouse, rat background.
Calcineurin A Antibody (YA2508) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2508), targeting Calcineurin A, with a predicted molecular weight of 59 kDa (observed band size: 59 kDa). Calcineurin A Antibody (YA2508) can be used for WB, ICC/IF, FC experiment in human, mouse, rat background.
Glutaminase Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 73 kDa, targeting to Glutaminase. It can be used for WB,ICC/IF,IP assays with tag free, in the background of Human, Mouse, Rat.
CSNK1A1; Casein kinase I Isoform alpha; CKI-alpha; CK1
WB, IP
Human, Rat
Casein Kinase 1 alpha Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 39 kDa, targeting to Casein Kinase 1 alpha. It can be used for WB,IP assays with tag free, in the background of Human, Rat.
NRG3 Antibody (YA1432) is a biotin-conjugated non-conjugated IgG antibody, targeting NRG3, with a predicted molecular weight of 78 kDa (observed band size: 55 kDa). NRG3 Antibody (YA1432) can be used for WB experiment in human, rat background.
TNNI2; Troponin I; fast skeletal muscle; Troponin I; fast-twitch Isoform
WB, IP
Human, Mouse, Rat
Troponin I Antibody (YA1832) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1832), targeting Troponin I, with a predicted molecular weight of 21 kDa (observed band size: 21 kDa). Troponin I Antibody (YA1832) can be used for WB, IP experiment in human, mouse, rat background.
Cofilin Antibody (YA2822) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2822), targeting Cofilin, with a predicted molecular weight of 19 kDa (observed band size: 19 kDa). Cofilin Antibody (YA2822) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human background.
Toll-Like Receptor 9; CD289; TLR9; Toll like receptor 9; Toll like receptor 9 Isoform A precursor; Toll like receptor 9 Isoform B
WB
Human
Toll-Like Receptor 9 Antibody (YA3321) is a biotin-conjugated non-conjugated IgG antibody, targeting Toll-Like Receptor 9, with a predicted molecular weight of 116 kDa (observed band size: 130 kDa). Toll-Like Receptor 9 Antibody (YA3321) can be used for WB experiment in human background.
MYL2 Antibody (YA2709) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2709), targeting MYL2, with a predicted molecular weight of 19 kDa (observed band size: 19 kDa). MYL2 Antibody (YA2709) can be used for WB, IHC-P, IP experiment in human, mouse, rat background.
ACE Antibody is an unconjugated, approximately 150 kDa, rabbit-derived, anti-ACE monoclonal antibody. ACE Antibody can be used for: WB,IHC-P,FC expriments in human, mouse background without labeling.
Nucleolysin TIA 1 Isoform p40; p40 TIA 1; TIA1 protein; TIAL1; TIAR
IHC-P
Human
TIA1 Antibody (YA1229) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1229), targeting TIA1. TIA1 Antibody (YA1229) can be used for IHC-P experiment in human background.
CAV2; Caveolae protein 20 Kd; Caveolin 2; Caveolin 2 Isoform a and b; Caveolin-2
WB, IHC-F, IHC-P, ICC/IF, IP
Human
Caveolin 2 Antibody (YA2387) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2387), targeting Caveolin 2, with a predicted molecular weight of 18 kDa (observed band size: 18 kDa). Caveolin 2 Antibody (YA2387) can be used for WB, IHC-F, IHC-P, ICC/IF, IP experiment in human background.
Activator protein 1; AP 1; Jun D; jun D proto oncogene; Jund; JunD FL Isoform; Transcription factor jun D
WB, IP
Human, Mouse, Rat
Phospho-JunD (Ser255) Antibody (YA3087) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3087), targeting Phospho-JunD (Ser255), with a predicted molecular weight of 35 kDa (observed band size: 38,42 kDa). Phospho-JunD (Ser255) Antibody (YA3087) can be used for WB, IP experiment in human, mouse, rat background.
MYH6; MYH7; MYHC; MYHCA; MYHCB; Myosin heavy chain 6; Myosin heavy chain; Myosin-6; Myosin heavy chain; cardiac muscle alpha Isoform
WB, IHC-P
Human, Mouse, Rat
MYH6 Antibody (YA3200) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3200), targeting MYH6, with a predicted molecular weight of 224 kDa. MYH6 Antibody (YA3200) can be used for WB, IHC-P experiment in human, mouse, rat background.
Cofilin 1 Antibody (YA1311) is a non-conjugated IgG antibody, targeting Cofilin 1, with a predicted molecular weight of 19 kDa (observed band size: 19 kDa). Cofilin 1 Antibody (YA1311) can be used for WB, IF-Cell, FC experiment in Human, Mouse, Rat, Monkey background.
PP2A alpha/beta Antibody (YA1693) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1693), targeting PP2A alpha/beta, with a predicted molecular weight of 36 kDa (observed band size: 36 kDa). PP2A alpha/beta Antibody (YA1693) can be used for WB, IHC-F, IHC-P, ICC/IF, IP experiment in human, mouse, rat, hamster background.
Phospho-PP2A alpha (Tyr307) Antibody (YA2856) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2856), targeting Phospho-PP2A alpha (Tyr307), with a predicted molecular weight of 36 kDa (observed band size: 36 kDa). Phospho-PP2A alpha (Tyr307) Antibody (YA2856) can be used for WB, IHC-P, ICC/IF, IP experiment in human, mouse, rat background.
AAT4; FAA4; MYH11; Myosin 11; Myosin heavy chain 11; Myosin heavy chain smooth muscle Isoform; Myosin heavy polypeptide 11 smooth muscle; SMHC; SMMHC
WB, IHC-P
Human, Mouse
MYH11 Antibody (YA1620) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1620), targeting MYH11, with a predicted molecular weight of 227 kDa (observed band size: 250 kDa). MYH11 Antibody (YA1620) can be used for WB, IHC-P experiment in human, mouse background.
MYL9 Antibody (YA2093) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2093), targeting MYL9, with a predicted molecular weight of 20 kDa (observed band size: 20 kDa). MYL9 Antibody (YA2093) can be used for WB, IHC-P, IP experiment in human, mouse, rat background.
Alpha Isoform serine threonine protein phosphatase PP1alpha 1 catalytic subunit; Catalytic subunit; PP1A; PP1A_HUMAN; PP1alpha; PP2C ALPHA; PP2CA; Ppp1ca; Protein Phosphatase 2C Alpha Isoform; Serine threonine protein phosphatase PP1 alpha catalytic subunit; Serine threonine protein phosphatase PP1 alpha catalytic subunit protein phosphatase 1; Serine/threonine-protein phosphatase PP1-alpha catalytic subunit.
WB, IHC-F, IHC-P, ICC/IF
Human
PP1C alpha Antibody (YA1040) is a mouse-derived non-conjugated IgG1 antibody (Clone NO.: YA1040), targeting PP1C alpha, with a predicted molecular weight of 38 kDa (observed band size: 38 kDa). PP1C alpha Antibody (YA1040) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human background.
Alpha Isoform serine threonine protein phosphatase PP1alpha 1 catalytic subunit; Catalytic subunit; PP1A; PP1A_HUMAN; PP1alpha; PP2C ALPHA; PP2CA; Ppp1ca; Protein Phosphatase 2C Alpha Isoform; Serine threonine protein phosphatase PP1 alpha catalytic subunit; Serine threonine protein phosphatase PP1 alpha catalytic subunit protein phosphatase 1; Serine/threonine-protein phosphatase PP1-alpha catalytic subunit.
WB, ICC/IF
Human
PP1C alpha Antibody (YA1041) is a mouse-derived non-conjugated IgG1 antibody (Clone NO.: YA1041), targeting PP1C alpha, with a predicted molecular weight of 38 kDa (observed band size: 38 kDa). PP1C alpha Antibody (YA1041) can be used for WB, ICC/IF experiment in human background.
Phospho-Hormone sensitive lipase (Ser853) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 117 kDa, targeting to Phospho-Hormone sensitive lipase (S853). It can be used for WB,IHC-P assays with tag free, in the background of Human, Mouse, Rat.
Factor H Antibody (YA3361) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA3361), targeting Factor H, with a predicted molecular weight of 139 kDa (observed band size: 180 kDa). Factor H Antibody (YA3361) can be used for WB, ICC/IF experiment in human background.
PP 1G; PP-1G; PP1G; PP1G_HUMAN; PP1gamma; PPP 1G; PPP1CC; PPP1CC protein; PPP1G; Protein phosphatase 1 catalytic subunit gamma Isoform; Protein phosphatase 1C catalytic subunit; Protein phosphatase 1C subunit; Protein phosphatase 2C gamma Isoform; Serine/threonine phosphatase 1 gamma; Serine/threonine protein phosphatase PP1 gamma catalytic subunit; Serine/threonine-protein phosphatase PP1-gamma catalytic subunit.
WB
Human
PP1C gamma Antibody (YA1068) is a biotin-conjugated non-conjugated IgG2b antibody, targeting PP1C gamma, with a predicted molecular weight of 37 kDa (observed band size: 37 kDa). PP1C gamma Antibody (YA1068) can be used for WB experiment in human background.
Alpha Isoform serine threonine protein phosphatase PP1alpha 1 catalytic subunit; Catalytic subunit; PP1A; PP1A_HUMAN; PP1alpha; PP2C ALPHA; PP2CA; Ppp1ca; Protein Phosphatase 2C Alpha Isoform; Serine threonine protein phosphatase PP1 alpha catalytic subunit; Serine threonine protein phosphatase PP1 alpha catalytic subunit protein phosphatase 1; Serine/threonine-protein phosphatase PP1-alpha catalytic subunit.
WB, IHC-P, IP
Human, Mouse, Rat
PP1C alpha/beta Antibody (YA1700) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1700), targeting PP1C alpha/beta, with a predicted molecular weight of 38 kDa (observed band size: 38 kDa). PP1C alpha/beta Antibody (YA1700) can be used for WB, IHC-P, IP experiment in human, mouse, rat background.
14-3-3 protein eta; 1433F_HUMAN; Brain protein 14-3-3; eta Isoform; HGNC:12853; Protein AS1; Tyrosine 3/tryptophan 5 monooxygenase activation protein eta polypeptide; YWHA 1; YWHA1; Ywhah.
WB
Human, Mouse, Rat
14-3-3 eta Antibody (YA838) is a non-conjugated and Mouse origined monoclonal antibody about 28 kDa, targeting to 14-3-3 eta (5F2). It can be used for WB assays with tag free, in the background of Human, Mouse, Rat.
SERCA2 ATPase Antibody (YA1931) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1931), targeting SERCA2 ATPase, with a predicted molecular weight of 115 kDa (observed band size: 115 kDa). SERCA2 ATPase Antibody (YA1931) can be used for WB, IHC-F, IHC-P, ICC/IF experiment in human, rat background.
CDKN2A Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 17 kDa, targeting to CDKN2A. It can be used for WB,IP assays with tag free, in the background of Human, Mouse.
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.
PI3 Kinase p110 delta Antibody (YA1617) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA1617), targeting PI3 Kinase p110 delta, with a predicted molecular weight of 119 kDa (observed band size: 119 kDa). PI3 Kinase p110 delta Antibody (YA1617) can be used for WB, ICC/IF experiment in human, mouse, rat background.
phospho-PI3 Kinase p110 beta (Ser1070) Antibody is an unconjugated, approximately 110-123 kDa, rabbit-derived, anti-phospho-PI3 Kinase p110 beta (Ser1070) polyclonal antibody. phospho-PI3 Kinase p110 beta (Ser1070) Antibody can be used for: WB, ELISA, IHC-P, IHC-F, IF expriments in human, mouse, rat, and predicted: chicken, dog, pig, cow, horse, guinea pig background without labeling.
troponin I type 3 (cardiac); Cardiac troponin I; Troponin I, cardiac muscle; Cardiomyopathy, familial hypertrophic, 7, included; CMD1FF; CMD2A; CMH7; cTnI; Familial hypertrophic cardiomyopathy 7; MGC116817; RCM1; Tn1; Tni; TNN I3; TNNC 1; TNNC-1; TNNC1; TNNI3; Troponin I cardiac; Troponin I cardiac muscle; Troponin I cardiac muscle Isoform; Troponin I type 3 cardiac; troponin I, cardiac 3; TroponinI; Troponin I; TNNI3_HUMAN.
WB, IHC-P, ICC/IF, IP
Human
Cardiac Troponin I/TNNC1 Antibody is an unconjugated, approximately 23 kDa, rabbit-derived, anti-Cardiac Troponin I/TNNC1 monoclonal antibody. Cardiac Troponin I/TNNC1 Antibody can be used for:WB,IHC-P,ICC/IF,IP expriments in human background without labeling.
CD 152; CD152; CD152 antigen; Celiac disease 3; CELIAC3; CTLA 4; CTLA-4; Cytotoxic T cell associated 4; Cytotoxic T lymphocyte associated 4; Cytotoxic T lymphocyte associated antigen 4; Cytotoxic T lymphocyte associated protein 4; Cytotoxic T lymphocyte associated serine esterase 4; Cytotoxic T lymphocyte protein 4; Cytotoxic T-lymphocyte-associated antigen 4; Cytotoxic T-lymphocyte-associated protein 4; GSE; IDDM12; CD152 Isoform; CTLA4_HUMAN; GRD4; ICOS; Ligand and transmembrane spliced cytotoxic T lymphocyte associated antigen 4.
WB, ICC/IF
Human, Mouse, Rat
CTLA4 Antibody is a rabbit-derived non-conjugated IgG antibody, targeting CTLA4, with a predicted molecular weight of 25 kDa. CTLA4 Antibody can be used for WB,ICC/IF experiments in human, mouse, rat backgrounds.
phospho-ERK1 + 2 (Thr183/Tyr185) Antibody is an unconjugated, approximately 42/44 kDa, rabbit-derived, anti-phospho-ERK1 + 2 (Thr183/Tyr185) polyclonal antibody. phospho-ERK1 + 2 (Thr183/Tyr185) Antibody can be used for: WB, ELISA, IHC-P, IHC-F, ICC, IF expriments in human, mouse, and predicted: rat, chicken, dog, cow, horse, rabbit, guinea pig background without labeling.
Caspase-1 p20 Antibody is an unconjugated, approximately 20/46 kDa, rabbit-derived, anti-Caspase-1 p20 polyclonal antibody. Caspase-1 p20 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, Flow-Cyt, ICC, IF expriments in human, mouse, rat, background without labeling.
PIK3CA Antibody is an unconjugated, approximately 110 kDa, rabbit-derived, anti-PIK3CA monoclonal antibody. PIK3CA Antibody can be used for: WB, ICC/IF, IP expriments in human, mouse, rat background without labeling.
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsin B, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
LBG20304 (compound 2s) is a ligand for the homologous GluK5 receptor (IC50: 432 nM), more than 40-fold selective over the homologous GluK1-3 isoforms. Low doses of LBG20304 (<10 μM) have no agonist or antagonist functional response at heterologous GluK2/5 receptors, and at high doses (>10 μM), it exhibits low agonist activity in neuronal slices (rat) .
SSOe26 sodium is a 15mer antisense oligonucleotide targeting?HER4. SSOe26 sodium induces exon 26 skipping, leading to the generation of a novel mRNA transcript that excludes exon 26 (CYT2 isoform). SSOe26 sodium decreases tumour growth in mouse xenografts.
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