tc i

TC-I 2014 shows antiallodynic properties in pain models. TC-I 2014 is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 antagonist (IC50: 0.8 nM, 3.0 nM, and 4.4 nM for canine, human and rat channels respectively).

α2β1 integrin inhibitor

APS6-45 inhibits RAS/MAPK signaling and exhibits anti-tumor activity.

ICI-204879 HCl is a potent and selective agonists at the opioid kappa-receptor.

TC-I2000 is an TRPM8 channel blocker. Inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells with IC50 of 53 nM.

BCATc Inhibitor 2 exhibited an IC50 of 0.8 microM in the hBCATc assays; it is an active and selective inhibitor. BCATc Inhibitor 2 also blocked calcium influx into neuronal cells following inhibition of glutamate uptake, and demonstrated neuroprotective e

Sphistin Synthetic Peptide (12-38, Fitc in N-Terminal-Fluorescently Labeled Peptide) represents truncated fragments of the parent peptide, characterized by an N-terminal fluorescent label (Fitc).

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

antcin A is a steroid-like phytochemical isolated from the fruiting bodies of a precious edible mushroom Antrodia cinnamomea with strong anti-inflammatory and anti-tumor effects.

TCIP 1 is a small molecule in the category of transcriptional/epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

Gefapixant citrate (AF-219 citrate) is an orally available, highly potent P2X3 receptor antagonist with antitussive properties that inhibits hP2X2/3. It can be used to study chronic cough.

Vat-Cit-PAB-Monomethyl Dolastatin 10 is an ADC linker-conjugated drug designed to deliver potent antitumor activity through Monomethyl Dolastatin 10, a potent tubulin inhibitor, connected via the Vat-Cit-PAB (ADC linker).

DK-TCIP2 is an anticancer agent formed by linking the CDK9 inhibitor SNS-032 and the BCL6 inhibitor BI-3812. This compound exhibits anticancer activity both in vivo and in vitro, making it suitable for research in lymphoma.

CDK-TCIP1 is a bivalent molecule that links the CDK9 inhibitor SNS-032 with the BCL6 ligand BI3812. It effectively and specifically kills cells overexpressing BCL6, with an EC50 of 7.7 nM for SUDHL5 cells.

TCIP3 is a bivalent molecular glue (molecular glue) that can simultaneously bind to both p300/CBP and BCL6. It redirects p300 and CBP to activate programmed cell death genes, which are typically repressed by the oncogenic driver BCL6. TCIP3 is useful for studying diffuse large B-cell lymphoma (DLBCL) and is not toxic to untransformed tonsil lymphocytes or fibroblasts.

EB-TCIP (BAK-04-212) is a bivalent molecule composed of AP1867 and BI-3812. It facilitates the reversible formation of a ternary complex between FKBPF36V and BCL6BTB, thereby recruiting FKBP12F36V-tagged EWS/FLI1 to DNA sites bound by the transcriptional regulator BCL6, rapidly inducing expression of BCL6 target genes such as SOCS2 and CXCL11. EWS/FLI1 is a fusion transcription factor found in Ewing sarcoma. EB-TCIP is applicable for studying transcriptional dysregulation in cancer.

Maropitant citrate is a synthetic neurokinin-1 receptor antagonist and substance P inhibitor, used for controlling vomiting in cats and dogs.

TCID (UCH-L3 Inhibitor)(IC50=0.6 μM) is a DUB inhibitor of ubiquitin C-terminal hydrolase L3. It has the 125-fold selectivity to L1.

Maropitant citrate anhydrous is a neurokinin (NK1) receptor antagonist.

Antcin-B exhibits a high-affinity inhibition of 3CLPro, which is potentially significant in SARS-CoV-2 research [1].

TAT-CIRP, a trans-activating (Tat) cold-inducible RNA-binding protein-derived peptide, functions as an inhibitor of myeloid differentiation protein 2 (MD2). It has demonstrated significant neuroprotective effects against ischemic and hemorrhagic stroke in mouse models [1].

Tat-CIRP, a peptide inhibitor, impedes the protein-protein interaction between myeloid differentiation 2 (MD-2), also known as lymphocyte antigen 96 (LY96), and cold-inducible RNA binding protein (CIRP) by binding to MD-2. This disrupts the MD-2 and CIRP interaction as confirmed in co-immunoprecipitation assays. Notably, in vivo studies reveal that Tat-CIRP, at dosages of 10 and 20 mg/kg, significantly reduces infarct volume in both a mouse model of middle cerebral artery occlusion (MCAO) and a rhesus monkey model of thrombosis-induced stroke. Additionally, it improves motor function, evidenced by decreased time to manipulate and withdraw food with the affected arm in the primate model.

LAPTc-IN-1 (compound 4), with a K i of 0.27 μM, serves as a competitive inhibitor of acidic M17 leucinopeptidase (LAPTc) and stands as a potential antagonist against the parasite Trypanosoma cruzi [1].

Antcin B is an inhibitor of SARS-CoV-2 3-chymotrypsin-like protease (3CL Pro). It interacts with several crucial amino acid residues of 3CL Pro, including Leu141, Asn142, Glu166, and His163, through hydrogen bonding, salt bridges, and hydrophobic interactions, thereby inhibiting its activity. This inhibition blocks the cleavage of viral polyproteins and suppresses the replication of the SARS-CoV-2 virus within host cells. Antcin B shows potential for research in the context of COVID-19.