T2145

Temsirolimus (CCI-779) is a specific mTOR inhibitor ( IC50: 1.76 μM), used in the treatment of advanced renal cell cancer.

5-Bromothiazol-2-amine (Compound 54) is a basic amine compound. It has an IC50 value greater than 10 µM against Aurora A.

5,10,15,20-Tetrakis(4-chlorophenyl)porphyrin (Compound 5) is a photosensitizer. It does not exhibit significant photodynamic cytotoxicity and is primarily used in the optimization of photosensitizer structures for photodynamic therapy (PDT) in psoriasis.

(E)-Belizatinib ((E)-TSR-011) (compound 36) is the (E)-isomer of Belizatinib, and serves as a potent, highly selective, and orally active inhibitor of anaplastic lymphoma kinase (ALK), with an enzymatic IC50 of 0.005 μM and a cellular IC50 of 0.048 μM. The compound exhibits over 61-fold selectivity against JAK2, SRC, and IGF1R, and demonstrates excellent efficacy and pharmacokinetic properties in rats and dogs. (E)-Belizatinib is applicable for research in ALK-driven cancers.

Galectin-3-IN-7 is a selective Galectin-3 inhibitor with a Kd value of 5.7 nM, demonstrating a selectivity over Gal-1 that is 390 times greater. It downregulates pro-fibrotic signaling pathways, including ACTA2, COL1A2, and FN1, in TGFβ-stimulated LX2 hepatic stellate cells. Galectin-3-IN-7 is useful in fibrosis research.

β-carboline-ACS81 is a potent antitumor β-carboline derivative. It induces apoptosis in HL-60 cells by causing mitochondrial membrane potential collapse and arrests the cell cycle at the G2/M phase. This compound exhibits significant antiproliferative activity against HL-60 cells (IC50 = 1.52 μM). β-carboline-ACS81 is applicable for research in leukemia, histiocytic lymphoma, hepatocellular carcinoma, malignant melanoma, colorectal cancer, and lung cancer.

SCPI-3 is a potent and competitive inhibitor of mosquito sterol carrier protein-2 (SCP-2), with inhibition concentrations of AeSCP-2IC50 = 0.159 µM and AeSCP-xIC50 = 0.285 µM. It physiologically impacts cholesterol metabolism in cultured insect cells, showing an IC50 of 3.09 µM in Aag-2 cells. SCPI-1 exhibits insecticidal activity against Aedes aegypti, with an LD50 of 12.3 µM.

Anticanceragent 289 is an H2O2-responsive anticancer prodrug. It demonstrates H2O2-induced DNA alkylation activity and selectively inhibits the proliferation of cancer cells with high ROS expression, compared to non-malignant cells. It significantly suppresses tumor growth in vivo without visible toxicity. Anticanceragent 289 is applicable for research in triple-negative breast cancer (TNBC).

MRC71 is a TRIMTAC degrader that specifically targets the Halo tag, comprising a PEG linker and a chloroalkane group. It selectively degrades oligomeric CAV1- and Cavin1-mEGFP-Halo, but not monomeric mEGFP-Halo, and exhibits a concentration-dependent degradation profile characteristic of hooked effects.

SV119 hydrochloride is a sigma-2 ligand with a Ki value of 5.2 nM. It enhances the efficient transport of drugs across cancer cell membranes. Combining dm-Erastin with SV119 hydrochloride successfully overcomes internalization barriers observed in pancreatic cancer while retaining the inherent antitumor activity of Erastin. Additionally, SV119 hydrochloride exhibits cytotoxic effects on triple-negative breast cancer (TNBC) cells and induces apoptosis (apoptosis).

Teprenone Impurity 5 (5Z-GGA) is the cis isomer of Teprenone. It exhibits inhibitory activity on the proliferation of human ovarian cancer cells, Caov-3, and can halt the invasion process of these cancer cells. Additionally, Teprenone Impurity 5 induces the expression of heat shock protein 70 (HSP70) and thioredoxin (Trx). This compound is applicable for research in ovarian cancer.

Nefazodone (Nefadar) is an oral antidepressant that is an antagonist of postsynaptic 5-HT 2A receptor and 5-HT 2C receptor, and also inhibits the reuptake of norepinephrine, dopamine, and serotonin (SNDRI).

SERCA2a activator 2 (Compound 25) is a potent activator of SERCA2a (cardiac type) and also activates SERCA1a (skeletal muscle type). Under [Ca²⁺]MAX conditions, it enhances SERCA2a ATPase activity and facilitates Ca²⁺ uptake with EC₅₀ values of 4 μM and 0.80 μM, respectively. It consistently activates under near-physiological [Ca²⁺]MID conditions as well. Furthermore, SERCA2a activator 2 exhibits low cytotoxicity, making it useful for researching diseases such as heart failure.

(S)-Bleximenib (Compound 28) ((S)-JNJ-75276617) is an isomer of Bleximenib. It demonstrates an IC50 greater than 1 μM in MEIS1 mRNA expression assays, making it applicable for research in acute myeloid leukemia.

(-)-Norfenfluramine (l-Norfenfluramine) is a metabolite of Fenfluramine. It effectively counteracts abnormal locomotor activity in zebrafish and can be utilized in epilepsy research.

Carba1 is a bifunctional carbazole derivative that activates nicotinamide phosphoribosyltransferase (NAMPT) and enhances the biosynthesis of NAD. It binds to the colchicine site on tubulin, potentially boosting the antitumor effects of various chemotherapeutics such as Paclitaxel. Carba1 has neuroprotective properties and regulates cellular energy metabolism. It is applicable in research on cancer and chemotherapy-induced peripheral neuropathy (CIPN).

CaMKIIδ-IN-1 (Compound 15e) hydrochloride is a pyrimidine-based inhibitor of CaMKIIδ with an IC50 value of 12 nM.

Taprizosin (UK-338003) mesylate is an α-adrenoreceptor antagonist.

XS018661 is a dual inhibitor targeting the YEATS domains of ENL and its homolog protein AF9, with IC50 values of 1.6 μM and 3 μM, respectively, and Kd values of 754 nM and 523 nM, respectively.

sEH/FLAP-IN-2 is a selective dual inhibitor of sEH (IC50 = 12.6 nM) and FLAP. It significantly reduces lipids derived from 5-LOX/FLAP and sEH, thereby promoting the redistribution of these lipids. sEH/FLAP-IN-2 is applicable in peritonitis research.

PROTACCDK6ligand 2 is a ligand specifically targeting the CDK6 protein, playing a crucial role in forming the PROTACCDK6 Degrader1.

NIM258 is a potent nonimmunosuppressive cyclophilin inhibitor, with a Kd of 1.2 nM for cyclophilin A, and demonstrates anti-HCV activity with an EC50 of 40 nM. It is applicable in research related to HCV infection.

Anecortave Acetate (NSC-24345), an angiostatic steroid, is used for proteomics research.

6-Methoxy-N,N-diethylpentylone hydrochloride is an alkaloid derivative employed in the study of neurological disorders.