V-9302 is a competitive antagonist of transmembrane glutamine flux that selectively and potently targets the amino acid transporter ASCT2 with an IC50 of 9.6 μM. V-9302 exhibits anti-tumor activity[1].
TDP1 Inhibitor-2 (compound 5) is a potent inhibitor for TDP1 (tyrosyl-DNA phosphodiesterase 1), with an IC50 of 99 nM. TDP1 Inhibitor-2 also can inhibit SCAN1 (spinocerebellar ataxia syndrome with axonal neuropathy), with an IC50 of 3.5 μM[1].
1'-epi Gemcitabine hydrochloride is the inactive isomer of Gemcitabine hydrochloride (HY-B0003), and can be used as an experimental control. Gemcitabine Hydrochloride (LY 188011 Hydrochloride) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine Hydrochloride inhibits DNA synthesis and repair, resulting in autophagyand apoptosis[1][2].
MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC50 of 4 nM.
KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research[1].
Glucodichotomine B (Compound 13) is a natural product which can be isolated from the roots of Chinese medicinal plant Stellaria dichotoma L. var. lanceolata. Glucodichotomine B shows antitumor activity[1].
hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with Ki values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively[1].
Clathrin-IN-2 is potent inhibitor of clathrin mediated endocytosis (CME) with an IC50 value of 2.3 μM. Clathrin-IN-2 also has inhibitiory for dyn I GTPase with an IC50 value of 7.7 μM[1].
ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 µΜ[1].
Upifitamab is a naked antibody of upifitamab rilsodotin. Upifitamab rilsodotin is an antibody-coupled drug (ADC) targeting NaPi2b and is used in ovarian cancer research, particularly in platinum-resistant recurrent ovarian cancer[1].
Zanolimumab (Anti-Human CD4 Recombinant Antibody) is a fully human monoclonal antibody targets CD4. Zanolimumab effectively inhibits T-cell receptor (TCR) signal transduction. Zanolimumab can be used for the research of heumatoid arthritis, psoriasis, melanoma, cutaneous and peripheral T-cell lymphoma[1].
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy[1].
TOPK-p38/JNK-IN-1 (Compound B12) is an orally active TOPK-p38/JNK signaling pathway inhibitor with the IC50 value of 2.14 µM for NO production. TOPK-p38/JNK-IN-1 shows anti-inflammatory activities. TOPK-p38/JNK-IN-1 also inhibits phosphorylate downstream related proteins and avoids degradation of TOPK[1].
G0-C14 is a cationic lipid-like compound alkyl-modified polyamidoamine (PAMAM) dendrimer. G0-C14 involves in the preparation of a series of macrophage-targeted nanoparticles (NPs). NPs can be used for drug and vaccine delivery[1][2].
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis[1][2].
3’-O-(2-Methoxyethyl)-2-aminoadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1(IC50= 5 nM) in cells.IC50 value: 5 nM [1]Target: MTH1 inhibitorTH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.
ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects[1][2].
PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.
Macozinone is a new drug candicate that inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043target: DprE1In vitro: PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro. [1]In vivo: PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL.[2] PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB). [3]
Ifetroban (BMS-180291) sodium is an orally active antagonist of thromboxane A2 (TXA2) or prostaglandin H2 (PGH2) receptor. Ifetroban sodium shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban sodium can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research[1][2][3][4].
Kusunokinin ((-)-Kusunokinin) is a nature product that could be isolated form P. nigrum. Kusunokinin has anticancer activity. Kusunokinin arrests cell cycle at G2/M phase and induce apoptosis[1].
2’-Amino-2’-deoxy-5’-O-(4,4’-dimethoxytrityl)-5-methyluridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Tetrabenazine ((+)-) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1. target: VMAT-2In vitro: Tetrabenazine ((+)-) inhibit the activity of the transporter but appear to interact differently with the protein. [2] Tetrabenazine ((+)-) inhibits reserpine binding to the transporter, suggesting that the sites may interact in an allosteric manner. [1]In vivo: 0.9% saline (80%) and dimethylsulfoxide (DMSO) (20%). Tetrabenazine ((+)-) blocks dopamine (DA) storage and depletes striatal DA; Tetrabenazine ((+)-) was shown to induce tremulous jaw movements (TJMs) in rats and mice. The reference dose for administration is 2.0 mg/kg.[2]
2'-O-Methyl-5'-O-dmt-inosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia[1][2].
KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1, with an IC50 of 16.5 nM. KH-CB20 also can inhibits DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM)[1].
L-Azidohomoalanine-1,2,3,4-13C4 hydrochloride is the 13C- and 15N-labeled L-Azidohomoalanine hydrochloride. L-Azidohomoalanine hydrochloride is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity[1].
Rabdosin B is an ent-kaurene diterpenoid with anticancer effects. Rabdosin B induces DNA damage in cells, and inhibits lettuce root hair development of seedlings[1][2].
BT8009 is a Nectin-4 targeting toxin conjugate with a Kd value of 2.5 nmol/L for human Nectin-4 (hNectin-4) extra-cellular domain (ECD). BT8009 consists of a Nectin-4-binding bicyclic peptide, a cleavable linker system and monomethylauristatin E (MMAE). BT8009 can be used for the research of advanced and metastatic urothelial cancer[1].