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PK68 is a potent orally active and specifical typeIIinhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis .
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β typeII receptor and activin typeII receptor activities, without inhibiting BMP typeII receptor.
TypeII topoisomerase inhibitor 1 is a potent and selective E. coliDNA gyraseinhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. TypeII topoisomerase inhibitor 1 inhibitstopoisomerase IV activity (IC50: 0.98 μM). TypeII topoisomerase inhibitor 1 can be used in the research of antibacterial area .
TypeII TRK inhibitor 1 is a potent TRKinhibitor, which inhibits various TRK fusion protein variants and wild type. TypeII TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . TypeII TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Guaiacylglycerol-8-O-4'-(sinapyl alcohol) ether is a DGAT1inhibitor with an IC50 of 92.7 μM and can be extracted from Eleutherococcus senticosus. Guaiacylglycerol-8-O-4'-(sinapyl alcohol) ether can be utilized in research related to typeII diabetes and obesity .
Collagen TypeII Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen TypeII Fragment can be used for research on inflammation and immunity .
PfFAS-IIinhibitor 1 (Compound 3) is a Plasmodium falciparumtypeII fatty acid biosynthesis pathway (PfFAS-II)inhibitor, with an IC50 of 0.63 μM for PfFabI enzyme. PfFAS-IIinhibitor 1 has antimalarial activity .
Topoisomerase IIinhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a TypeII DNA topoisomerase (topo II) inhibitor , as a topo IIα/βinhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential .
Finasteride (MK-906) acetate is a potent and competitive 5α-reductaseinhibitor, with an IC50 of 4.2 nM for typeII 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for typeII 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
Finasteride (MK-906) is an orally active and competitive 5α-reductaseinhibitor, with an IC50 of 4.2 nM for typeII 5α-reductase. Finasteride has approximately a 100-fold greater affinity for typeII 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin IIinhibits cell-free protein synthesis, releases adenine from rat liver ribosomes and from DNA, and has no RNase activity .
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for typeII 5α-reductase. Finasteride has approximately a 100-fold greater affinity for typeII 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
Finasteride (Standard) is the analytical standard of Finasteride. This product is intended for research and analytical applications. Finasteride (MK-906) is a potent and competitive 5α-reductaseinhibitor, with an IC50 of 4.2 nM for typeII 5α-reductase. Finasteride has approximately a 100-fold greater affinity for typeII 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
(Rac)-Managlinat dialanetil ((Rac)-MB06322) is a compound for the inhibition of type 2 diabetes that is in Phase II clinical trials and works by inhibiting gluconeogenesis.
TRK II-IN-1 is a potent typeIITRKinhibitor, with IC50s of 3.3, 6.4, 4.3 and 9.4 nM, for TRKA/B/C and TRKA G667C, respectively. TRK II-IN-1 also inhibitsFLT3, RET, and VEGFR2 with IC50s of 1.3, 9.9, and 71.1 nM, respectively. TRK II-IN-1 can be used for the research of TRK driven cancers .
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD)type I/II with IC50s of 39 nM and 27 nM, respectively.
Naporafenib (LXH254) is a potent, selective, orally active, typeIIBRAF and CRAFinhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .
Gepotidacin mesylate hydrate is an orally active triazaacenaphthylene antibiotic and bacterial typeII topoisomerase inhibitor. Gepotidacin mesylate hydrate inhibits bacterial DNA replication by blocking topoisomerase enzymes. Gepotidacin mesylate hydrate selectively inhibits topoisomerase IV and the B subunit of DNA gyrase .
Pomisartan is an orally active angiotensin II receptor typeAT1 antagonist (IC50=0.26 μM). Pomisartan works by inhibiting the binding of angiotensin II to the AT1 receptor, thereby blocking the vasoconstriction and aldosterone release caused by this interaction. Pomisartan results in a blood pressure-lowering effect .
Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
WWL123, a carbamate-based compound, is a potent and selective ABHD6inhibitor. WWL123 can be used for research of inflammation, metabolic disorders (obesity and typeII diabetes mellitus) and epilepsy .
R59949 is a pan diacylglycerol kinase (DGK)inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of typeII DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
PMX464 (AW 464), a thiol-reactive quinol, is the inhibitor of thioredoxin-thioredoxin reductase (Trx/TrxR) system. PMX464 can inhibit NF-κB-mediated proinflammatory activation of human typeII alveolar epithelial cells .
SCD1 inhibitor-3 is a safe, potent and orally active SCD1inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, typeII diabetes and dyslipidemia, as well as skin diseases, acne and cancer .
Izonsteride (Compound LY320236) is an inhibitor of 5α-reductase (IC50 = 11.6 nM for type I; 7.37 nM for typeII). LY320236 inhibits the activity of steroid 5α-reductase, preventing the conversion of testosterone (T) to dihydrotestosterone (DHT). LY320236 can significantly inhibit the growth of LNCaP tumors in thymic mice without exhibiting obvious host toxicity .
CP-91149 is a GP (glycogen phosphorylase)inhibitor. CP-91149 promotes glycogen resynthesis, but not its overaccumulation. CP-91149 has the potential for TypeII (insulin-dependent) diabetes study .
Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively) .
CDK8-IN-9 (compound 22) is a potent typeIICDK8inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies .
Bimolane (AT-1727), a human topoisomerase IIinhibitor, can be used as an anti-neoplastic agent and for the research of psoriasis. Bimolane shows leukemogenic activity and induces multiple types of chromosomal aberrations in human lymphocytes .
α-Glucosidase-IN-9 (compound 7) is a potent α-glucosidaseinhibitor, with an IC50 of 55.6 μM. α-Glucosidase-IN-9 can be used for typeII diabetes research .
α-Glucosidase-IN-10 (compound 13) is a potent α-glucosidaseinhibitor, with an IC50 of 92.7 μM. α-Glucosidase-IN-10 can be used for typeII diabetes research .
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2inhibitor, with IC50s of 6, 2 and 48 nM for wild-typeLRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibitsSer935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
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 .
CHMFL-ABL-121 is a highly potent typeIIABL kinaseinhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively .
TD-0212 TFA is an orally active dual pharmacology angiotensin IItype 1 receptor (AT1) antagonist and neprilysin (NEP)inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP .
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenaseinhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of typeII diabetes .
MM3122 is a selective typeII transmembrane serine protease (TMPRSS2) inhibitor with an IC50 value of 0.34 nM. MM3122 effectively blocks TMPRSS2, thereby inhibiting the entry of SARS-CoV-2 and MERS-CoV into human cells .
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin IItype 1 receptor (AT1) antagonist and neprilysin (NEP)inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP .
TPEQM-DMA is a NIR-II photosensitizer. TPEQM-DMA accumulates in cancerous mitochondria, and inhibits cancer cell growth. TPEQM-DMA has potent type-I phototherapeutic efficacy to overcome the intrinsic pitfalls of PDT in combating hypoxic tumors .
JTE-952 is a potent, oral active and selective TypeIIinhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis .
Satigrel (E5510) is a potent inhibitor of platelet aggregation. Satigrel inhibits collagen- and arachidonic acid-induced platelet aggregation through preventing thromboxane A2 synthesis by selective inhibition of the target enzyme, PGHS1, which exists in platelets. Satigrel inhibits PGHS1 (IC50: 0.081 μM) and PGHS2 (IC50: 5.9 μM). Satigrel is against Type III PDE, Type V and TypeII (IC50: 15.7 μM, 39.8 μM and 62.4 μM, respectively) .
YLIU-4-105-1 is a TypeII JAK2inhibitor. YLIU-4-105-1 has in vivo pharmacodynamic activity as evidenced by inhibiting pSTAT5, reducing spleen to body weight, and lowering blood reticulocyte counts in a dose-dependent manner .
PTP1B-IN-15 is a potent and selective inhibitor of protein tyrosine phosphatase 1B (PTP1B). PTP1B-IN-15 has the potential for the research of typeII diabetes and obesity .
HG-12-6 is a typeIIinhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation .
TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a typeII TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice .
AT1R antagonist 3 (Compound 1) is an antagonist for angiotensin IItype 1 receptor (AT1R) and an inhibitor for calcium channel type-L CaV1.2 (IC50=0.57 μM). AT1R antagonist 3 exhibits vasodilation efficacy in solated rat aorta (10 μM, 88.7%) and antihypertensive efficacy in rat models .
CHMFL-ABL-039 is a typeII native ABL kinase and drug-resistant V299L mutant BCR-ABLinhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia .
Telmisartan (Standard) is the analytical standard of Telmisartan. This product is intended for research and analytical applications. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
(+)-ITD-1 is an inhibitor for TGF-β, that inhibits the TGF-β2 with an IC50 of 0.46 μM. (+)-ITD-1 promotes the degradation of TGF-b typeII receptor (TGFBR2) and the differentiation of cardiomyocyte, and inhibits the mesoderm formation in the early differentiation stage of mouse embryonic stem cells (mESCs) .
JNJ-26990990 is a broad-spectrum antiepileptic agent with oral activity. JNJ-26990990 can inhibit voltage-gated Na + channels and N-typeCa 2+ channels, but has a very weak inhibitory effect on human carbonic anhydrase-II (IC50 = 110 μM) .
Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
Telmisartan-d3 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
β-Cyfluthrin (beta-Cyfluthrin) is a typeII synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibitingCa 2+ ATPase involved in calcium transport .
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD)type I/II with IC50s of 39 nM and 27 nM, respectively.
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
TGFβRII-IN-2 (Compound 3n) is an inhibitor for transforming growth factor-β typeII receptor (TGFβRII) with IC50 of 2.4 μM, which blocks endothelial-to-mesenchymal transition and cell migration in different cancer cell lines without perturbing the microtubule network .
Quizartinib (AC220) is an orally active, highly selective and potent second-generation typeIIFLT3 tyrosine kinaseinhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
RIPK1-IN-4 (compound 8) is a potent and selective typeII kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase .
RIPK3-IN-1 is a RIPK3typeII DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM .
IHMT-TRK-284 (Compound 34) is a potent, orally active typeII TRK kinaseinhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete .
α-Amylase/α-Glucosidase-IN-3 (Compound 17) is an α-Amylase/α-Glucosidase dual inhibitor, with IC50s of 0.70 μM and 1.10 μM. α-Amylase/α-Glucosidase-IN-3 can be used for research of type-II diabetes mellitus .
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
HG-7-85-01 is a typeII ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibitsT315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-IItype-1 receptors. Barbadin can induce apoptosis .
Imidapril hydrochloride (TA-6366) is an orally active angiotensin-converting enzyme (ACE) and MMP-9inhibitor. Imidapril hydrochloride suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril hydrochloride can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research .
Antidiabetic agent 5 (compound S1) is a antidiabetic agent. Antidiabetic agent 5 inhibits the activity of α-glucosidase and α-amylase with IC50 values of 3.91, 8.89 µM, respectively. Antidiabetic agent 5 decreases sugar levels. Antidiabetic agent 5 has the potential for the research of type-II diabetes .
Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. Quizartinib (AC220) is an orally active, highly selective and potent second-generation typeIIFLT3 tyrosine kinaseinhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation typeIIFLT3 tyrosine kinaseinhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .
Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial typeII and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP) .
Imidapril (TA-6366 free base) is an orally active angiotensin-converting enzyme (ACE) and MMP-9inhibitor. Imidapril suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research .
Atigliflozin (AVE-2268) is an orally active and selective SGLT-2inhibitor, with IC50s of 10 nM and 8.2 μM for hSGLT-2 and hSGLT-1) respectively. Atigliflozin can lower the blood glucose and improve the impaired oral glucose tolerance. Atigliflozin can be used for research of typeII diabetes mellitus .
Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial typeII and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP) .
K-252a, a staurosporine analog, inhibitsprotein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase typeII, and phosphorylase kinase, respectively . K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene .
(Rac)-PAT-494 is a typeII autotaxin inhibitor with the activity of inhibiting the production of lysophosphatidic acid (LPA) in the blood. (Rac)-PAT-494 can participate in the inhibition of diseases related to cancer, fibrosis and inflammation by antagonizing the function of autotaxin. (Rac)-PAT-494 shows high activity in biochemical and plasma tests. (Rac)-PAT-494 can reduce plasma LPA levels after oral administration to rats .
AFG206 is a first-generation ATP competitive “typeII” FLT3inhibitor. AFG206 potently inhibits cell proliferation (IC50 around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia .
Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coliDNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coliDNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
TGFβRII-IN-3 (Compound 2r) is a selective inhibitor of the TGFβ typeII receptor (TGFβ RII) (IC50 = 4.1 μM). TGFβRII-IN-3 inhibits TGFβ signaling by promoting the proteolytic degradation of TGFβ RII. TGFβRII-IN-3 can block endothelial-to-mesenchymal transition and cell migration. TGFβRII-IN-3 can be used in cancer research .
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/IItype AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coliDNA gyrase (IC50=0.109 μg/ml) . Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coliDNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
B-Raf IN 17 (Compound 8e) is a potent and orally active typeII multi-kinaseinhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer .
β-Cyfluthrin (Standard) is the analytical standard of β-Cyfluthrin. This product is intended for research and analytical applications. β-Cyfluthrin (beta-Cyfluthrin) is a typeII synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibitingCa 2+ ATPase involved in calcium transport .
ND-011992 is a reversible, selective quinazoline-typeinhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibitsrespiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study .
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human typeII receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
CDK5-IN-4 (compound 4) is a potent multikinase type-IIinhibitor targeting CDK5, with an IC50 of 9.8 μM. CDK5-IN-4 also inhibits GSK-3α, GSK-3β, CDK9, and CDK2, with IC50 values of 0.98, 4.00, 1.76, and 6.24 μM, respectively. CDK5-IN-4 can be used for glioblastoma research .
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na + channels and N-typeCa 2+ channels, and is effective as a K + channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC50=35 μM) and CA-I (18 μM) .
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
LI-2242 is an inositol hexakisphosphate kinase (IP6K)inhibitor. LI-2242 has inhibition effect for IP6K1, IP6K2, IP6K3 and IPMK with IC50 values of 31 nM, 42 nM, 8.7 nM and 1944 nM, respectively. LI-2242 can be used for thew research of typeII diabetes, obesity, metabolic complications, venous thrombosis, and psychiatric disorders .
c-Met-IN-12 (compound 4r) is an orally active, potent and selective typeIIc-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
Gatifloxacin (Standard) is the analytical standard of Gatifloxacin. This product is intended for research and analytical applications. Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coliDNA gyrase (IC50=0.109 μg/ml) . Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
Gatifloxacin (sesquihydrate) (Standard) is the analytical standard of Gatifloxacin (sesquihydrate). This product is intended for research and analytical applications. Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis?in vivo.
Enpp-1-IN-16 (compound 54) is an ENPP1inhibitor. Enpp-1-IN-16 has the potential to study cancer, especially in cases of high ENPP1 expression or elevated cytoplasmic DNA levels. Enpp-1-IN-16 can also be used in other diseases mediated by ENPP1, such as bacterial or viral infections, insulin resistance and typeII diabetes, chondrocalcinosis and osteoarthritis, calcium pyrophosphate deposition disorder (CPPD), low Phosphatase disease and soft tissue calcification disorders .
Axl-IN-18 (compound 25c) is a potent and selective typeIIAXLinhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
HG-6-63-01 is a typeII RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET .
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. In LPS-induced macrophages, SAP15 inhibitsHDAC5 and NF-κB p65 phosphorylation. In addition, SAP15 treatment increased the expression of aggrecan and typeII collagen and decreased the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials .
Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to typeII deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibitsCYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
MRTX1133 is a noncovalent, potent, and selective KRAS G12Dinhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
JND4135 is a TypeIITRKinhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to typeII deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibitsCYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human typeII receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo .
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment .
TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling . TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment .
Collagen TypeII Fragment is an anti-inflammatory peptide that potently inhibits collagen-induced arthritis (CIA) in mice. Collagen TypeII Fragment can be used for research on inflammation and immunity .
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
SAP15 (Synthetic anti-inflammatory peptide 15) is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. SAP15 has the ability to penetrate cells and is able to induce downregulation of intracellular inflammation. SAP15 inhibits inflammation by inhibiting the phosphorylation of HDAC5 and thereby reducing the phosphorylation of NF-κB p65. In LPS-induced macrophages, SAP15 inhibitsHDAC5 and NF-κB p65 phosphorylation. In addition, SAP15 treatment increased the expression of aggrecan and typeII collagen and decreased the expression of osteocalcin in LPS-induced chondrocytes. SAP15 can be used in the study of inflammation regulation and anti-inflammatory therapy of biomaterials .
Anti-Mouse MHC Class II (I-Ak, I-Ar, I-Af, I-As,I-Ag7) Antibody (10-3.6.2) is a mouse-derived IgG2c, κ type antibody inhibitor, targeting to mouse MHC Class II.
Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenaseinhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of typeII diabetes .
K-252a, a staurosporine analog, inhibitsprotein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase typeII, and phosphorylase kinase, respectively . K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene .
Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to typeII deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibitsCYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
Guaiacylglycerol-8-O-4'-(sinapyl alcohol) ether is a DGAT1inhibitor with an IC50 of 92.7 μM and can be extracted from Eleutherococcus senticosus. Guaiacylglycerol-8-O-4'-(sinapyl alcohol) ether can be utilized in research related to typeII diabetes and obesity .
Momordin II, an oleanane-type triterpene glycoside, is a ribosome inactivating protein. Momordin IIinhibits cell-free protein synthesis, releases adenine from rat liver ribosomes and from DNA, and has no RNase activity .
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD)type I/II with IC50s of 39 nM and 27 nM, respectively.
SPINK2, a robust acrosin inhibitor, is vital for normal spermiogenesis, preventing premature activation of proacrosin and other proteases to avoid spermiogenesis defects. It likely regulates germ cell apoptosis mediated by serine proteases and displays inhibitory activity against trypsin, indicating involvement in diverse serine protease-dependent processes. SPINK2 Protein, Human (HEK293, Fc) is the recombinant human-derived SPINK2 protein, expressed by HEK293 , with C-hFc labeled tag. The total length of SPINK2 Protein, Human (HEK293, Fc) is 61 a.a., with molecular weight of ~33.6-38 kDa.
Telmisartan-d3 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for typeII 5α-reductase. Finasteride has approximately a 100-fold greater affinity for typeII 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].
Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM[1][2].
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD)type I/II with IC50s of 39 nM and 27 nM, respectively.
Telmisartan- 13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Telmisartan-d7 (BIBR 277-d7) is a deuterium labeled Telmisartan (HY-13955). Telmisartan is a potent, long lasting antagonist of angiotensin IItype 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial typeII topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to typeII deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibitsCYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
MRTX1133 is a noncovalent, potent, and selective KRAS G12Dinhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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