TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models[2].In Vivo: TAK-418 (1 mg/kg; p.o.; once daily for 14 days) ameliorates some autism spectrum disorder (ASD) -like behaviors in neurodevelopmental disorder model rodents.TAK-418 increases H3K4me1/2/3 and […]

TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).In Vitro: TAK-615 specifically binds to membranes expressing the human LPA1 receptor with estimated Kd high affinity (KdHi) […]

Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants[2].In Vitro: The IC50 of Taletrectinib (1-1000 nM; 72 hours) against Ba/F3-TPM3-NTRK1, Ba/F3-ETV6-NTRK1, -NTRK2, -NTRK3, […]

Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes[2].

TAM-IN-2 is a TAM inhibitor extracted from patent US 20170275290 A1, pyrrolotriazine compound 0904.

TAMRA-Azide-PEG-biotin is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.In Vitro: PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke[2].In Vitro:TAN-67 (SB-205607) dihydrobromide has high potency (EC50=1.72 nM) for the inhibition of forskolin-stimulated cAMP accumulation at human delta-opioid receptors expressed by […]

Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria[2].IC50 & Target: β-lactamaseIn Vitro: Taniborbactam hydrochloride (VNRX-5133 hydrochloride) has IC50s of […]

Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model.IC50 & Target: IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM […]

Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC50s of 61/7/6 nM, respectively.IC50 & Target: IC50: 61 nM (JNK1), 7 nM (JNK2), 6 nM (JNK3)In Vitro: Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM). Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis […]

Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM[2].IC50 & Target: Ki: 0.13 nM (MCL1)[2].In Vitro: Tapotoclax is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (Ki=0.13 nM), with potential pro-apoptotic and antineoplastic activities. Upon administration, Tapotoclax binds to and inhibits the activity of MCL-1. […]

TAPS is a biological buffer, remain lysozyme native structure intact and prevents thermal denaturation against high temperatures. TAPS exhibits pKa value of 8.1, while the half-maximum values of connexin channel activity is 8.5 (pH)[2].

Tarasaponin VI is a natural product isolated from Aralia elata. Tarasaponin VI shows potent inhibitory activity on ethanol absorption.

Taraxasterol is a pentacyclic triterpenoid isolated from Taraxacum mongolicum. Taraxasterol has a role as a metabolite and an anti-inflammatory agent.

Taraxerone is isolated from Sedum sarmentosum. Taraxerone enhances effects on alcohol dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH) activities with EC50 values of 512.42 and 500.16 μM, respectively.IC50 & Target:EC50: 512.42 μM (ADH); 500.16 μM (ALDH)In Vivo: Taraxerone significantly lowers the plasma alcohol and acetaldehyde concentrations in mice. Compare to the control group, the ADH and […]

Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of […]

Tarloxotinib bromide (TH-4000) is an irreversible EGFR/HER2 inhibitor.IC50 & Target: EGFR/HER2.In Vitro: To confirm the mechanism of action, Tarloxotinib bromide is shown to be metabolized efficiently under hypoxia using a panel of human NSCLC cell lines (rate of TKI release 0.4-2.1 nM/hr/106 cells), a process that is inhibited by oxygen (TKI release 80% (538 vs […]

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.IC50 & Target: IC50: 1.0 nM (Aurora A); 95 nM (Aurora B)In Vitro: TAS-119 enhances the […]

TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2

TAS1553 is a potent, orally active protein–protein interaction (PPI) inhibitor with an IC50 values of 0.0396 μM. TAS1553 inhibits DNA replication and reduces intracellular dATP pool. TAS1553 induces apoptosis. TAS1553 can be used for cancer research.In Vitro: TAS1553 (0.001-1 μM) inhibits the enzymatic activity of RNR in a dose-dependent manner.TAS1553 (3 d) has anti-proliferative activity […]

TAT-DEF-Elk-1 TFA (TDE TFA) is a cell-penetrating peptide inhibitor of?Elk-1,?mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 TFA blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 activation. TAT-DEF-Elk-1 TFA is a useful tool to analyze the role of Elk-1 in this process during the development of […]

TAT-Gap19 TFA, a Cx mimetic peptide, is a specific connexin43 hemichannel (Cx43 HC) inhibitor. TAT-Gap19 TFA does not inhibits the corresponding Cx43 GJCs. TAT-Gap19 TFA traverses the blood-brain barrier and alleviate liver fibrosis in mice[2].In Vivo: A single injection of TAT-Gap19 TFA (i.v. via the tail vein; 55 mg/kg) produces significant immune signal in the […]

TAT-GluA2 3Y, an interference peptide, blocks long-term depression (LTD) at glutamatergic synapses by disrupting the endocytosis of AMPAR. TAT-GluA2 3Y can alleviate Pentobarbital-induced spatial memory deficits and synaptic depression[2].IC50 & Target: AMPAR

Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95[2].In Vitro: Tat-NR2BAA […]

Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.In Vitro: Obeticholic acid is conjugated with taurine in the liver to form Tauro-obeticholic acid, which is secreted into bile. Microorganisms in the ileum and colon can deconjugate Tauro-obeticholic acid, converting it into the parent drug, which […]

Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM[2].IC50 & Target:IC50: 40 μM (FXR)In Vitro: T-βMCA sodium inhibits FXR reporter activity in the CRC cell line HT29 (EC50 ~10 μM).T-βMCA sodium dose-dependently increases WNT signaling in HT29 and HCT116 cells.T-βMCA […]

Taurodeoxycholic acid, a bile acid, stabilizes the mitochondrial membrane, decreases free radical formation. Taurodeoxycholic acid inhibits apoptosis by blocking a calcium-mediated apoptotic pathway as well as caspase-12 activation. Taurodeoxycholic acid exhibits neuroprotective effect in 3-nitropropionic acid induced mouse model or genetic mouse model of Huntington’s disease (HD)[2].In Vitro: Taurodeoxycholic acid (50 μM, 100 μM; 4 […]

Taurolithocholic acid sodium salt, a potent cholestatic agent, is a potent Ca2+ agonist.In Vitro: Taurolithocholic acid (TLCA) at low concentrations (5 μM) tends to selectively increase the membrane-associated fraction of the e-isoform of PKC by 44.1% ± 40.2%.TLCA (10 μM) selectively induces translocation of theε-isoform of PKC to the hepatocellular membranes, a key step for […]

Taurolithocholic Acid 3-sulfate (disodium) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.

Tavaborole (AN-2690) is an antifungal agent with activity against Trichophyton species, in a topical solution formulation for the potential treatment of onychomycosis.In Vitro: Tavaborole (AN-2690) shows an 8-fold increase in activity against C. neoformans, and an 8-fold increase in activity against A. fumigatus. Tavaborole (AN-2690) obviously inhibit the cells expressing GlLeuRS-D444A, but has no effect […]

Taxifolin 7-O-rhamnoside (Taxifolin 7-O-α-L-rhamnoside) is a flavonoid isolated from Hypericum japonicum.

Taxifolin 7-O-β-D-glucoside (Taxifolin 7-O-glucoside) is one of the main metabolites at the seed germination stage in Scutellaria baicalensis. Taxifolin 7-O-β-D-glucoside, a flavonoid, mainly exists in the episperm and participates in defending against pathogens and UV-damage.

Tazofelone (LY 213829) is a cyclooxygenase-II (COX-II) inhibitor. Tazofelone transform into sulfoxide and quinol metabolites is primarily mediated by CYP3A. Tazofelone can be used for the research of inflammatory bowel disease[2].

TBA-7371 is a potent, noncovalent DprE1 inhibitor. TBA-7371 has potent antitubercular activity .IC50 & Target: DprE1

TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity.IC50 & Target:IC50: 1 nM (TBK1), 5.6 […]

TBT1 is a first-generation inhibitor of the MsbA transporter. TBT1 is an LPS transport inhibitor and MsbA ATPase stimulator in strains from the Acinetobacter genus. TBT1 stimulated ATPase activity with an EC50 of 13 μM.

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain[2].In Vitro: TC-N 1752 (compound […]

TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity[2].In Vitro: TC14012 (1 mM) inhibits more than 95% the infection of […]

TCA1 is a small molecule with activity against drug-susceptible and -resistant Mycobacterium tuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW.In Vitro: TCA1 shows bactericidal activity against both replicating (WT and drug resistant) and nonreplicating Mycobacterium tuberculosis (Mtb). TCA1 inhibits biofilm formation by Mtb H37Rv. TCA1 […]

TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons[2].IC50 & Target: IC50: 0.6 μM (UCH-L3) and 75 μM (UCH-L1)In Vitro: TCID (4,5,6,7-Tetrachloroindan-1,3-dione; compound 11) inhibits UCH-L1 with an IC50 of 75 μM. […]