Dodoviscin A is a pigmentation-altering agent, which can be isolated from the aerial parts of Dodonaea viscosa. Dodoviscin A inhibits melanin production in B16-F10 melanoma cells. Dodoviscin A suppresses mushroom tyrosinase activity, and tyrosinase activity induced by 3-isobutyl-1-methylxanthine. Dodoviscin A also inhibits the phorphosylation of cAMP response element binding protein, induced by 3-isobutyl-1-methylxanthine and forskolin[1].
7-Ketositosterol is a phytosterol isolated from the fruits of the mulberry tree (Morus alba L.). 7-Ketositosterol can significantly inhibit Cisplatin (HY-17394)-induced apoptosis in LLC-PK1 cells and has the potential to improve Cisplatin-induced nephrotoxicity[1].
CPI-1328 is an EZH2 inhibitor with a Ki value of 63 fM.
(-)-Syringaresinol, found in stems of Annona Montana, possesses anti-cancer activity[1].
KY-1044 (Alomfilimab; SAR 445256) is a fully human IgG1 antibody targeting inducible costimulatory receptor (ICOS). KY-1044 depletes ICOShigh cells via antibody-dependent cellular cytotoxicity (ADCC) through the engagement of FcgRIIIa. KY-1044 act as a costimulatory molecule on cells expressing lower ICOS levels, such as CD8+ TEff cells (through FcgR-dependent clustering). KY-1044 exploit the differential expression of ICOS on T-cell subtypes to improve the intratumoral immune contexture and restore an antitumor immune response[1].
AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively.
HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1).
Duocarmycin Analog is an analog of Duocarmycin, and used as an DNA alkylator and ADC cytotoxin[1].
AT7519 Hydrochloride is a potent inhibitor of CDKs, with IC50s of 210, 47, 100, 13, 170, and <10 nM for CDK1, CDK2, CDK4 to CDK6, and CDK9, respectively.
Ombrabulin hydrochloride is a derivative of CA-4 phosphate, which is known to exhibit antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.
Propargyl-C1-NHS ester is a nonclaevable linker for antibody-drug-conjugation (ADC).
Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate shows synergistic anti-cancer effects[1][2].
Ramelteon-d5 is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation[1][2].
PIN1 inhibitor 2 (compound 12) is a potent PIN1 inhibitor. PIN1 inhibitor 2 shows antitumor activity with an IC50 of 9.55 µM for MCF7 cells. PIN1 inhibitor 2 has the potential for the research of breast cancer[1].
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
STF-62247 is TGN inhibitor with IC50 of 0.625μM and 16μM in RCC4 and RCC4/VHL cells,respectively.It specifically induces autophagic cell death in cells that have lost VHL, an essential mutation in the development of RCC.IC50: 0.625/16μM in RCC4 and RCC4/VHL cells,respectively.[1]In vitro: STF-62247 induces cytotoxicity in VHL-deficient cells in a HIF-independent manner, STF-62247 increases acidification in VHL-deficient cells ,TGN is a target of STF-62247 and a drug-selective pathway synthetically lethal in VHL-deficient cells.[1] Golgi trafficking are required as initial signals in STF-62247-induced autophagy.[2]STF-62247 increases radiosensitivity in a VHL-dependent manner.[3]In vivo: SN12C, SN12C-VHL shRNA, or 786-O cells were implanted subcutaneously into the flanks of immunodeficient mice. The selective cytotoxicity of STF-62247 for the VHL-deficient cells was also demonstrated in 786-O cells compared to their wild-type VHL counterparts by clonogenic assay in vitro. Daily treatment with STF-62247 significantly reduced tumor growth of VHL-deficient cells. This decrease in tumor growth was concentration dependent. Importantly, drug treatment did not have any effect on the growth of SN12C tumor cells that have wild-type VHL. Together,STF-62247 reduces tumor growth in VHL-deficient cells in mice.[1]
WNY1613 is a potent and selective PI3Kδ inhibitor with piperazinone-containing purine scaffold. WNY1613 induces cancer cell apoptosis and inhibits the phosphorylation of PI3K downstream components in NHL cell lines. WNY1613 exhibits anti-NHL activity in vitro and in vivo[1].
MUN57694 is 26S proteasome inhibitor. MUN57694 was reported in WO 2006128196. This product has not formal name. For the convenience of scientific communication, we named it by combining its Inchi key (3 letters from the first letter of each section) with the last 5 digits of its CAS number or its molecule weight if its CAS number is not available
OTS186935 is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM[1].
DL-erythro-Dihydrosphingosine is a potent inhibitor of PKC and phospholipase A2 (PLA2)[1][2].
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors[1][2].
7-Methoxy obtusifolin (Compound 4) is a competitive tyrosinase inhibitor with an IC50 of 7.0 μM[1].
PD-1/PD-L1-IN-18 (Compound L31) is a small-molecule inhibitor of the PD-1/PD-L1 protein-protein interaction. PD-1/PD-L1-IN-18 blocks PD-1/PD-L1 with the IC50 of 1.054 μM. Antitumor Activity[1].
A potent and selective inhibitor of FAK phosphorylation with biochemical IC50 of 1.2 pM (pFAK Y397), cellular IC50 of 1 nM; displays 8-fold selectivity over PYK2, 26-fold selectivity over RSK1/2 , and >1000-fold selectivity over SRC, AURKA, AURKB, INSR, and KDR; suppresses pFAK Y397 and pFAK Y861 in tumors and liver, shows tumor growth inhibition in TOV21G xenografts in mice.
BRD 8899 is a potent and selective inhibitor of the serine/threonine kinase STK33 with IC50 of 0.11 nM (25 uM ATP); exhibits significant off-target inhibition of a few other kinases, including RIOK1 (97% inhibition), MST4 (96%), RSK4 (89%), ATK1 (85%), KITD816V (85%), ROCK1 (84%), and FLT3 (81%), while STK33 is inhibited by 89%; shows no effect cell viability in 35 cancer cell lines, fails to kill KRAS-dependent cells.
CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.
CSNK1-IN-2 is a CSNK1A1 inhibitor. CSNK1-IN-1 has inhibitory activity for CSNK1A1 kinase with IC50 values of 2.52 μM. CSNK1-IN-2 can be used for the research of proliferative disorders[1].
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
Nrf2-IN-1 (Compound 4f) is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2), acts as a promising agent in acute myeloid leukemia (AML) therapy[1].
Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].