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SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

ATRA-hydroxyimino, also known as CRABP-II ligand 1, is a chemical compound derived from Retinoic acid (ATRA). This compound binds to the cIAP1 ligand, specifically Bestatin, through a linker, resulting in the formation of a complex called SNIPER. The purpose of this complex is to degrade CRABP-II within IMR-32 cells[1].

JND4135, a type II TRK inhibitor, exhibits IC50 values targeting TRKA, TRKB, and TRKC at 2.79, 3.19, and 3.01 nM, respectively. It can overcome resistance due to TRKxDFG and other mutations in the BaF3 stable model, inhibiting the phosphorylation of TRKs WT, xDFG mutations, and their downstream signaling molecules. Additionally, JND4135 induces G0/G1 phase arrest and cell apoptosis (apoptosis) in BaF3–CD74-TRKA-G667C cells. This compound also demonstrates antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model by suppressing tumor growth.

HG-6-63-01 serves as a type II RET tyrosine kinase inhibitor (TKI). It effectively targets and inhibits REarranged during Transfection (RET) kinase, disrupting signaling pathways in human thyroid cancer cell lines possessing oncogenic RET alleles. Moreover, this compound reduces the phosphorylation and signaling of RET oncogenic mutants. HG-6-63-01 further suppresses the proliferation of fibroblasts transformed by RET/C634R and RET/M918T, as well as thyroid cancer cells with RET mutations, showing potential as a therapeutic option for cancers with oncogenic activation of RET.

CYP3A4-IN-4 (compound Δ,Λ-3) constitutes a Ru(II)-Ir(III) complex that acts as a photoactive inhibitor of the primary human drug-metabolizing enzyme CYP3A4. This complex features a [Ru(tpy)(Me2bpy)] photocaging group and exhibits an IC50 of 2.2 μM for the inhibition of microsomal CYP3A4 under irradiation conditions (λirr=530 nm, tirr=15 min). The phototherapeutic index (PI) of CYP3A4-IN-4 is 5.4.

Sitamaquine hydrochloride (WR 6026) is an orally active 8-aminoquinoline analog with antileishmanial activity. This compound inhibits mitochondrial complex II (succinate dehydrogenase) and is characterized by its lipophilic weak base properties. It rapidly accumulates in the acidic compartments of Leishmania parasites, predominantly localizing within the acidocalcisomes.

Angiotensin I-13C6,15N (human, mouse, rat) TFA is a labeled version of Angiotensin I, using isotopes 13C and 15N, specifically targeted for human, mouse, and rat studies. This compound serves as a precursor to angiotensin II, which is formed through the cleavage by angiotensin-converting enzyme (ACE).

RIP3 Activator 1 (compound C8) is an effective RIP3 activator that inhibits cell growth and induces necroptotic cell death (necroptosis) and autophagy through the RIP3/p62/Keap1 signaling pathway. Additionally, this compound enhances the expression of p-MLKL and promotes the accumulation of LC3-II and p62 proteins.

Y-30141 is closely related to the commonly used ROCK inhibitor, Y-27632. This compound inhibits the kinase activity of both ROCK-I and ROCK-II by competitively binding to the catalytic site, showing 20 to 30 times greater affinity for ROCK kinases compared to other Rho effector kinases. Furthermore, the inhibition mechanism and action profile of Y-30141 have also been investigated.

Thalidomide-Photoswitch3-NH2 hydrochloride is essential in creating PHOTACs, which are PROTACs activated by specific light wavelengths. These compounds become inactive in darkness and switch to an active cis isomer state under 390 nm irradiation, while wavelengths above 450 nm reverse this activation. This compound comprises a CRBN-recruiting ligand, an azobenzene photoswitchable crosslinker, and a pendant amine that interacts with an acid on the target warhead, and is used to synthesize PHOTAC-I-10 and PHOTAC-II-6.

CDK12/13-IN-3 (Compound 12b) is an orally active CDK inhibitor targeting CDK12 and CDK13, with IC50 values of 107.4 nM and 79.4 nM, respectively. This compound inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression involved in the DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative effects against various cancer cells with nanomolar IC50 values. In mouse models, it demonstrates antitumor activity, favorable pharmacokinetic properties, and an oral bioavailability of 53.6%.

Ran-IN-1 (Compound M36) is an orally active and selective inhibitor of Ran GTPase. It binds allosterically with high specificity to the switch II pocket of GDP-bound Ran (RanGDP), stabilizing its inactive state and reducing the formation of active Ran-GTP. Ran-IN-1 induces apoptosis in epithelial ovarian cancer (EOC) cells and inhibits DNA repair pathways such as homologous recombination (HR) and non-homologous end joining (NHEJ). This compound shows potential for research in epithelial ovarian cancer, particularly in high-grade serous carcinoma.

SDH-IN-25 is an SDH inhibitor with an IC50 of 4.82 mg/L, demonstrating broad-spectrum and potent antifungal activity. By binding to SDH amino acid residues (TRP173, TYR58, and ARG43), it mimics the action mode of the commercial fungicide flutolanil. SDH-IN-25 induces changes in hyphal morphology, disrupts respiratory metabolism by binding to complex II, generates reactive oxygen species (ROS), and affects mitochondrial membrane potential (MMP) in hyphae. This compound is utilized in agricultural disease control research.

CDK9-IN-37 (Compound 24) is a CDK9 inhibitor with high selectivity, demonstrating an EC50 of 5.5 nM and minimal inhibition of other CDK subtypes. It shows significant antiproliferative activity against acute myeloid leukemia cells MOLM-13, with an IC50 of 0.034 μM. CDK9-IN-37 suppresses CDK9 signaling, reducing RNAP II CTD (Ser2) phosphorylation, downregulating the anti-apoptotic protein McI-1, inducing apoptosis, and causing cell cycle arrest at the G2/M phase. This compound is applicable in the research of acute myeloid leukemia (AML).

TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.

Dyrk1A-IN-7 (Compound 29) is a selective DYRK1A kinase inhibitor with notable kinase selectivity, exhibiting an IC50 value of 28 nM for DYRK1A and a Kd of 17.5 nM for CLK2. This selective inhibitor is applicable in research related to cancer, type II diabetes, and neurological disorders.

3-Fluoro-evodiamine glucose (Compound 8) is an evodiamine-glucose conjugate. It enhances the expression of glucose transporter 1 (GLUT1) and inhibits topoisomerase I/II activity. Additionally, 3-Fluoro-evodiamine glucose induces apoptosis and causes cell cycle arrest at the G2/M phase. This compound demonstrates anti-tumor activity both in vivo and in vitro, with no significant toxicity observed.

(2R,4R)-APDC hydrate ((2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic acid hydrate) is an agonist for group II metabotropic glutamate receptors (mGluR). It influences cell proliferation by inhibiting glutamate release, enhancing motor responses generated by D1 receptor activation, or reducing brain-derived neurotrophic factor (BDNF) levels. This compound is applicable in research on epilepsy and other neurological disorders.

4-Iodo-SAHA (1k), an orally active inhibitor of both class I and class II histone deacetylase (HDAC), exhibits EC50 values of 1.1, 0.95, 0.12, 0.24, 0.85, and 1.3 μM for Skbr3, HT29, U937, JA16, and HL60 cell lines, respectively. This compound holds potential for cancer research purposes [1].

Quinacrine is a compound with multiple actions that is commonly used as an anti-protozoal agent. It has also been shown to be a highly potent autophagy inhibitor, although the dose required to achieve this effect is considerably cytotoxic (LD50 = 2.5 μM). Quinacrine analog 34 is a derivative of quinacrine that was designed with an improved cell viability profile (LD50 = 27 μM) to inhibit autophagy. At a minimum concentration of 0.5 μM, this compound has been shown to increase the protein levels of the autophagy biomarker LC3-II and to induce lysosome deacidification.

Angiotensin I/II (1-6) TFA is a chemical compound comprising amino acids 1-6, derived from the Angiotensin I/II peptide. This peptide is formed by the cleavage of angiotensinogen by renin, with Angiotensin I subsequently hydrolyzed by angiotensin-converting enzyme (ACE) to produce biologically active Angiotensin II. Angiotensin II has been extensively studied for its potential applications in the treatment of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy[1][2][3].

TBK1/IKKε-IN-4, a 6-aminopyrazolopyrimidine derivative, serves as a potent, selective inhibitor for TBK1 and IKKε, demonstrating IC50 values of 13 nM and 59 nM, respectively. This compound exhibits significantly reduced activity, by 100- to 1000-fold, against other protein kinases, such as PDK1, PI3K family members, and mTOR[1].

Rp-8-CPT-cAMPS is a powerful and competitive antagonist of cAMP-induced activation of cAMP-dependent protein kinase (PKA) I and II. Acting as a potent cAMP analog, Rp-8-CPT-cAMPS exhibits a preference for site A of RI over site A of RII. Additionally, it favors site B of RII over site B of RI. This compound effectively inhibits cAMP-dependent PKA activation and demonstrates selectivity in binding to specific sites within the protein kinase.

β-Cyfluthrin is a type II synthetic pyrethroid compound commonly utilized as an active ingredient in agricultural insecticide products. It exerts its insecticidal properties by acting as a neurotoxicant, primarily impacting the calcium concentration within nervous tissue. This effect is achieved through the inhibition of Ca 2+ ATPase, a crucial component involved in calcium transport.