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Salviolone is a natural diterpenoid derivative that can against melanomacells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanomacells .
4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanomacell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanomacells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling .
Anticancer agent 106 (compound 10ic) is an anticancer agent that induces apoptosis in B16-F10 melanomacells. Anticancer agent 106 also potently inhibits metastatic nodules in a mouse model of lung metastatic melanoma. Anticancer agent 106 can be used in the study of cancer, especially lung metastatic melanoma .
Palmostatin B is an Acyl protein thioesterase 1 and 2 (APT-1, APT-2) inhibitor. Palmostatin B reduces cell viability in a panel of NRAS mutant melanomacell lines. Palmostatin B inhibits Ras depalmitoylation in cells .
Reticulol (K 251-1) is an inhibitor of cyclic adenosine 3', 5'-monophosphate phosphodiesterase. Reticulol shows antitumor activity independent with cell cycle arrest or apoptosis. Reticulol inhibits cell growth of murine melanomacells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma .
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanomacell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities .
THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma .
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanomacells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanomacells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanomacells .
Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l .
Dihydrodehydrodiconiferyl alcohol (compound 2) is a kind of neolignan. Dihydrodehydrodiconiferyl alcohol can be isolated from Anogeissus acuminata. Dihydrodehydrodiconiferyl alcohol has specific cytotoxic activity on melanoma cancer cell line .
Box5 is a potent Wnt5a antagonist. Box5 inhibits Wnt5a signaling and inhibits Wnt5a-mediated Ca 2+ release. Box5 inhibits cell migration. Box5 has the potential for the research of melanoma .
Dacarbazine hydrochloride is a cell cycle nonspecific antineoplastic alkylating agent. Dacarbazine hydrochloride inhibits T and B lymphoblastic response, with IC50 values of 50 and 10 μg/mL, respectively. Dacarbazine hydrochloride can be used for the research of metastatic malignant melanoma .
(−)-L-threo-PDMP hydrochloride is the hydrochloride form of (−)-L-threo-PDMP. L-threo-PDMP is a glucosylceramide synthase (GCS) inhibitor. L-threo-PDMP stimulates the proliferation of cultured aortic smooth muscle cells, and that increases the level of LacCer in B16 melanomacells .
Picrocrocin, an apocarotenoid found in Saffron. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanomacells .
Box5 TFA is a potent Wnt5a antagonist. Box5 TFA inhibits Wnt5a signaling and inhibits Wnt5a-mediated Ca 2+ release. Box5 TFA inhibits cell migration. Box5 TFA has the potential for the research of melanoma .
Ru-4T is a phototherapy agent. Ru-4T has phototherapeutic efficacy (PI = 114,000) against melanomacells (SK-MEL-28) under broad-band visible light (400-700 nm) with EC50 values of 740 pM .
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanomacells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs) .
CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer .
IZTZ-1, an imidazole-benzothiazole conjugate, is a c-MYC G4 ligand. IZTZ-1 is able to downregulate the c-MYC expression by stabilizing c-MYC G4. IZTZ-1 induces cell cycle arrest, apoptosis, thereby inhibiting cell proliferation in B16 cells. IZTZ-1 shows antitumor activity, and can be used for melanoma research .
Chelidonine, an isoquinoline alkaloid, can be isolated from Chelidonium majus L.. Chelidonine causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, and prevents cell cycle progression of stem cells in Dugesia japonica. Chelidonine has cytotoxic activity against melanomacell lines. with anticancer and antiviral activity .
SP-2-225 is a selective HDAC6 inhibitor. SP-2-225 enhance the production of cancer-associated antigens and macrophage antigen cross-presentation to T cells. SP-2-225 reduces the tumor volume in a syngeneic SM1 melanoma model .
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanomacells. Epirosmanol also exhibits DPPH radical scavenging activity .
Eftilagimod alfa (IMP321) is a recombinant LAG-3Ig fusion protein that binds to MHC class II. Eftilagimod alfa mediates antigen-presenting cell (APC) activation followed by CD8 T-cell activation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research .
Cytostatin sodium is an effective and selective protein phosphatase 2A (PP2A) inhibitor with an IC50 value of 210 nM. Cytostatin sodium exhibits anti-metastatic properties, good antitumor activity, and can induce apoptosis. Cytostatin sodium can also prevent the adhesion of B16 melanomacells to components of the extracellular matrix (laminin and collagen). Cytostatin sodium belongs to the family of natural product fosriecin .
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanomacells with S100B over those without S100B . Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM) .
Dacarbazine citrate is a cell cycle nonspecific antineoplastic alkylating agent. Dacarbazine citrate inhibits T and B lymphoblastic response, with IC50 values of 50 and 10 μg/mL, respectively. Dacarbazine Citrate can be used for the research of apoptosis and various cancers such as metastatic malignant melanoma .
CDK2-IN-9 is a potent CDK2 inhibitor with an IC50 of 0.63 µM. CDK2-IN-9 shows antiproliferative activity. CDK2-IN-9 induces apoptosis and cell cycle arrest at S and G2/M phase. CDK2-IN-9 has the potential for the research of melanoma .
HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a Kd value of 35.7 μM. HEMTAC CDK4/6 degrader 1 induces CDK4/6 degradation in B16F10 melanomacells. HEMTAC CDK4/6 degrader 1 arrests cell cycle at G0/G1 phase and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in research of cancer . HEMTAC CDK4/6 degrader 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma .
3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside, a saponin, is isolated from Polaskia chichipe Backbg. 3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside shows ability to inhibit melanin biosynthesis by B16 melanomacell with inhibitory activity 84.2% at 100μM[1].
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanomacells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanomacells .
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanomacells . 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanomacell lines with varying degrees of tyrosinase activity .
TT-012 specifically binds to dynamic MITF and destroys the latter's dimer formation and DNA-binding ability. TT-012 inhibits the transcriptional activity of MITF in B16F10 melanomacells. TT-012 inhibits the growth of high-MITF melanomacells, and inhibits the tumor growth and metastasis with tolerable toxicity to liver and immune cells in animal models .
D-threo-PDMP hydrochloride is a glucosylceramide (GlcCer) synthase inhibitor that inhibits glucosylceramide (GlcCer) and lactosylceramide (LacCer) levels in B16 melanomacells. D-threo-PDMP hydrochloride lacks reactivity to the other two surface antigens anti-melanoma monoclonal antibodies M562 and M622 and the major histocompatibility antigen anti-H-2KbDb monoclonal antibody, so it is specific for B16 melanoma sex .
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanomacells. Graveoline also exhibits antifungal activity .
Cryptomeridiol can be isolated from Phaulopsis imbricata. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH-stimulated B16 melanomacells .
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
Gochnatiolide A is a dimeric sesquiterpene that can be found in Ainsliaea henryi. Gochnatiolide A exhibits antiproliferative activity against the kidney, melanoma, ovarian-resistant and glioma cell lines .
Tyrosinase-IN-10 (Compound 23) is a partially competitive tyrosinase inhibitor with an IC50 of 1.6 μM against tyrosinase activity from human melanomacell lysates .
Machilin A is a lignan isolated from the methanolic extract of Phoebe bark. Machilin A inhibits melanin biosynthesis in B-16 mouse melanomacells with an IC50 of 39.9 μM.
Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity . Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanomacells .
Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cellapoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
Pancratistatin is an isoquinoline alkaloid that can be isolated from Hymenocallis littoralis. Pancratistatin induces apoptosis of human melanomacells. Pancratistatin can be used for the research of neuroblastoma, leukemia and breast cancer .
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanomacell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanomacells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggers apoptosis .
Quinaldopeptin, a quinomycin antibiotic isolated from the culture of Streptoverticillium album strain, is highly active against Gram-positive bacteria and anaerobes and strongly cytotoxic against cultured B16 melanomacells .
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Benzyl isothiocyanate-d7 is the deuterium labeled Benzyl isothiocyanate. Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity[1][2]. Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanomacells[2].
Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells . Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p
Citropten (5,7-Dimethoxycoumarin) is a coumarin isolated from bergamot oil. Citropten (5,7-Dimethoxycoumarin) has an antiproliferative activity against A2058 human melanomacell line .
Cardanol monoene (Cardanol C15:1) is a phenolic compound which can be found in cashew nut shell liquid. Cardanol monoene can induce mitochondria-associated apoptosis in human melanomacells .
Octacosane-d58 is the deuterium labeled Octacosane[1]. Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[2][3][4].
Ipilimumab is a fully human monoclonal antibody IgG1κ that blocks the inhibitory receptor cytotoxic T lymphocyte antigen 4 (CTLA-4) on T cells. Ipilimumab can be used in unresectable or metastatic melanoma (MM) studies .
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
Cloxiquine (5-Chloro-8-quinolinol) is an antibacterial, antifungal and antiamoebic agent. Cloxiquine can be used for the research of tuberculosis and dermatoses. Cloxiquine suppresses the growth and metastasis of melanomacells through activation of PPARγ .
ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanomacell lines proliferation and induce apoptosis, and has antitumor activity in vitro .
(S)-(-)-MRJF22 is haloperidol metabolite II valproate ester. (S)-(-)-MRJF22 exhibits the high antimigratory effects in endothelial and tumor cells. (S)-(-)-MRJF22 is a potential multifunctional agent against uveal melanoma .
Neorauflavane is a potent tyrosinase inhibitor derived from Campylotropis hirtella, with an IC50 value of 30 nM for tyrosinase monophenolase activity and an IC50 value of 500 nM for diphenolase activity. Neorauflavane can effectively reduce the melanin content of B16 melanomacells .
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanomacell lines (a-375 and b-16f1) and PC-3 prostate cancer cells. In addition, a member of this group (compound 3) expressed 2 μ M concentration inhibited the invasion of DU-145 cells by 80%.
ACA-28 (compound 2a) is a potent ERK MAPK signaling modulator. ACA-28 selectively inhibits cancer cell growth by inducing apoptosis with ERK hyperactivation
ACA-28 inhibits cell growth of melanomacells (SK-MEL-28) and normal melanocytes (NHEM), with IC50 values of 5.3 and 10.1 μM, respectively .
CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanomacell lines expressing mPGES1 .
3'-Deoxy-4-O-methylsappanol shows cytotoxicity against melanoma HMV II cell (IC50=50.4 μM) and has significant anti-melanogenic activities (EC50=72 μM) .
ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanomacell lines proliferation and induce apoptosis, and has antitumor activity in vitro .
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
SB-216 is a potent tubulin polymerization inhibitor. SB-216 shows strong antiproliferative potency in a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer. SB-216 can be used for cancer research .
Lankacidin C is an inhibitor of protein synthesis in vitro. Lankacidin C inhibits the activity of L1210 leukemia, B16 melanoma and 6C3 HED/OG lymphosarcoma cell lines. Lankacidin C has antibacterial activity and antitumor activity .
TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2 . TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma .
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells .
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis .
Flanvotumab (IMC-20D7S) is a human monoclonal antibody targeting to tyrosinase-related protein (TYRP1), specifically expressed in melanocytes and melanomacells. Flanvotumab acts function via natural killing-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Flanvotumab has potent anti-tumor activity and good tolerance .
Lycorine hydrochloride is the main active ingredient of the herbal medicine derived from Lycoris radiata (L’Her.) Herb. and is also a melanoma vasculogenic inhibitor and has anti-tumor activity . Lycorine hydrochloride effectively inhibits mitotic proliferation of Hey1B cells (IC50 of 1.2 μM) .
Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanomacell lines. Exarafenib has anticancer activity .
Anticancer agent 89 is a benzothiazole-2-thiophene S-glycoside derivative with antitumor activity, has high inhibition against the three cell line from ovarian cancer (OVCAR-4), renal cancer (A498), and melanoma (SK-MEL-5) .
Ansamitocin P 3' (Antibiotic C 15003P3') is an anti-tumor antibiotic. Ansamitocin P 3' prolongs the survival of mice with leukemia P388, melanoma B16, leukemia L1210, sarcoma 180, Ehrlich carcinoma and mast cell tumor P815 .
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
NSC49652 is a reversible, orally active p75 neurotrophin receptor (p75 NTR, also known as NGFR, TNFRSF16, and CD271) agonist. NSC49652 targets the transmembrane domain of p75 NTR. NSC49652 induces apoptosis and affects the viability of melanomacells .
Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid, also known as ganoderic acid 24. Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid shows high cytotoxicity against cancer cells, such as human lung cancer cells CH27, melanomacells M21, and oral cancer cells HSC-3 .
Cinnamic acid- 13C3 (3-Phenylacrylic acid- 13C3) is the 13C labeled Cinnamic acid (HY-N0610A). Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells .
Autophagy/REV-ERB-IN-1
hydrochloride (Compound 24) is a dual autophagy and REV-ERB inhibitor with
anticancer activity. Autophagy/REV-ERB-IN-1 (hydrochloride) has improved
potency in blocking autophagy, enhanced toxicity against cancer cells.
Autophagy/REV-ERB-IN-1 (hydrochloride) can be used for the research for
melanoma .
Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM . Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanomacells through modulation of Ca 2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 .
L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanomacells with S100B over those without S100B . Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM) .
γ-Linolenic Acid methyl ester (Methyl GLA) is an esterified version of γ-Linolenic Acid (GLA), which is an ω-6 fatty acid, serves as melanomacell proliferation inhibitors. γ-Linolenic Acid methyl ester inhibits ADP-induced blood platelet aggregation and induces apoptosis .
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanomacell line .
Antiproliferative agent-26 (compound 4g) is an antiproliferative agent with much broad range of activity targeting Leukemia, CNS, Melanoma, Renal and Breast (at the concentration of 10 μM). Antiproliferative agent-26 inhibits colony forming and arrests cell cycle at G1 phase/S phase at 5 μM and 25 μM, respectively .
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
HDAC6-IN-19 (Compound 14g) is a HDAC6 inhibitor (IC50: 2.68 nM). HDAC6-IN-19 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 61.6 nM, 98.7 nM and 103 nM. HDAC6-IN-19 potently inhibits multiple cancer cell proliferation, including leukemia, colon cancer, melanoma, and breast cancer cell lines .
TP-472 is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7 . TP-472 induces apoptosis of melanomacells .
L-Buthionine-(S,R)-sulfoximine hydrochloride is a cell-permeable, potent, fast acting, orally active and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively .
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .
TBHQ (Standard) is the analytical standard of TBHQ. This product is intended for research and analytical applications. TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2 . TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma .
Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability .
16,16-Dimethyl prostaglandin A1 (di-Me-PGA1) is a prostaglandin analog that can inhibit DNA synthesis in Lewis lung carcinoma and B 16 amelanotic melanomacells. 16,16-Dimethyl prostaglandin A1 also inhibits viral replication in both HSV and HIV-1 infection systems .
CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer .
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanomacell line .
Methyl p-coumarate (Methyl 4-hydroxycinnamate), an orally active esterified derivative of p-Coumaric acid (pCA), can be isolated from the flower of Trixis michuacana var longifolia. Methyl p-coumarate could inhibit the melanin formation in B16 mouse melanomacells. Methyl p-coumarate also has strong in vitro inhibitory effect on A. alternata and other pathogens .
CDK2-IN-8 is a potent CDK2 inhibitor with an IC50 of 1.74 µM. CDK2-IN-8 shows antiproliferative activity. CDK2-IN-8 has the potential for the research of melanoma .
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanomacells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
Anticancer agent 157 (compound 15) is a NO inhibitor (IC50=0.62 μg/mL) with anti-inflammatory and anticancer activities. Anticancer agent 157 can bind to iNOS (inducible NO synthase) and caspase 8, causing nuclear fragmentation and chromatin condensation, inducing apoptosis. Anticancer agent 157 inhibits HT29 colon cancer cells (IC50=2.45 μg/mL), Hep-G2 liver cancer cells (IC50=3.25 μg/mL), and B16-F10 murine melanomacells (IC50=3.84 μg/mL) .
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanomacells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM) .JR-AB2-011 decreases the phosphorylation level of Akt, decreases MMP2 activity, thereby reducing the ability of tumor cells to migrate and invade. JR-AB2-011 also induces non-apoptotic cell death .
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
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 melanomacells. 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 .
Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanomacells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
UNC1062 is a MERTK-selective tyrosine kinase inhibitor, reduces activation of MERTK-mediated downstream signaling, induces apoptosis in culture, reduces colony formation in soft agar, and inhibits invasion of melanomacells. UNC1062 potently inhibits MERTK kinase activity (MERTK IC50=1.1 nM, Morrison Ki=0.33 nM) and exhibits specificity within the TAM family (TYRO3 IC50=60 nM, AXL IC50=85 nM) .
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity .
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells .
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor . NVP-BBD130 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Vanicoside E is an antioxidant and antitumor agent. Vanicoside E inhibits L-Tyrosine (HY-N0473) and L-DOPA (HY-N0304) with IC50s of 45.23 μM and 189.96 μM, respectively .
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanomacell growth .
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanomacell growth .
Cyclic-di-GMP is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP can be used in cancer research .
Cyclic-di-GMP sodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP sodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP sodium can be used in cancer research .
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .
Cyclic-di-GMP diammonium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP diammonium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP diammonium can be used in cancer research .
Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research .
SIRT1/2/3-IN-1 (compound 10) is a highly potent, selective and cell permeable inhibitor of SIRT1, SIRT2 and SIRT3 with IC50s of 0.54, 0.253, and 0.72 μM, respectively. SIRT1/2/3-IN-1 (compound 10) can be used for research of cancer .
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
PD-L1-IN-3 (Compound 4a) is a compound that targets PD-1/PD-L1, the IC50 value and EC50 value is 4.97nM and 2.70 μM for inhibit PD-L1 and Jurkat T cells, respectively. PD-L1-IN-3 can bind PD-L1 dimer to prevent PD-1 binding to PD-L1, therefore blocking PD-1 signaling. PD-L1-IN-3 can be used for lung cancer and melanoma diseases research .
1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 µM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
Vindesine is a semisynthetic derivative of vinblastine. Vindesine is a potent anticancer agent. Vindesine can be used for the research of melanoma and lung cancers .
ICMT-IN-1 (compound 75) is an inhibitor of ICMT (IC50=0.0013 μM). ICMT-IN-1 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
ICMT-IN-21 (compound 6ag) is an ICMT inhibitor (IC50=8.8 μM), a sulfonamide-modified farnesyl cysteine (SMFC). The farnesyl and carboxylic acid motifs of ICMT-IN-21 are important structures for inhibiting ICMT .
ICMT-IN-35 (compound 10n) is a FTPA-triazole compound and ICMT inhibitor (IC50=0.8 μM). ICMT-IN-35 is taken up by mammalian cells and can prevent K-Ras membrane localization and induce K-Ras mislocalization. Furthermore, ICMT-IN-35 is selectively cytotoxic against ICMT+/+ MEF cells and has low micromolar activity (IC50=0.8 μM) against metastatic pancreatic cancer cell lines .
ICMT-IN-48 (compound 1) is an ICMT inhibitor that is competitive (Km=13 μM) for the prenylated methyl acceptor, the first substrate of ICMT. ICMT-IN-48 inhibits ICMT activity with IC50s affected by the concentration of the second substrate S-adenosylmethinine (SAM), and the IC50s are 3.5 μM (1×Km SAM) and 2.3 μM (10×Km SAM), respectively .
ICMT-IN-53 (compound 12) is an ICMT inhibitor (IC50=0.96 μM) with PAMPA permeability and antiproliferative activity. ICMT-IN-53 inhibits the proliferation of MDA-MB-231 and PC3 with IC50s of 5.14 μM and 5.88 μM, respectively .
ICMT-IN-7 (compound 74) is an inhibitor of ICMT (IC50=0.015 μM). ICMT-IN-7 dose-dependently induces ICMT accumulation in the cytoplasm of HCT-116 cells and inhibits the proliferation of multiple cancer cell lines expressing K-Ras and N-Ras .
ICMT-IN-54 (compound 7c) is an adamantyl analogue and an ICMT inhibitor (IC50=12.4 μM), which can inhibit ICMT Methylation. ICMT-in-54 inhibits BFC (N-biotinyl-(6-aminohexanoic)-S-farnesyl-L-cysteine) methylation in saccharomyces cerevisiae expressing ICMT, which is an indirect effect of inhibiting ICMT methylation .
Vem-L-Cy5 (compound 3)，modified with the NIR fluorophore cyanine-5 (Cy5)，is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF V600E，and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability，and inhibits cell growth of many types of cancer .
A2-Iso5-2DC18 is a dihydroimidazole-linked lipid, served as potent mRNA delivery vehicle. A2-Iso5-2DC18 can be used for antitumor research, including B16F10 melanoma. .
Chlorin e6 is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer .
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
CDK1-IN-5 (10h) is a selective CDK1 inhibitor with IC50s of 42.19, 188.71 and 354.15 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-5 inhibits growth of cancer cells by affecting cell cycle. CDK1-IN-5 can be used for the research of cancer .
CDK1-IN-3 (8g) is a selective CDK1 inhibitor with IC50s of 36.8, 305.17 and 369.37 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN-3 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-3 can be used for the research of cancer .
CDK1-IN-4 (10d) is a selective CDK1 inhibitor with IC50s of 44.52, 624.93 and 135.22 nM for CDK1, CDK2 and CDK5, respectively. CDK1-IN4 inhibits the growth of cancer cells by affecting cell cycle. CDK1-IN-4 can be used for the research of cancer .
Topoisomerase II inhibitor 20 (Compound 3e) is a potent topoisomerase II (Topoisomerase II) inhibitor with an IC50 of 0.98 µM. Topoisomerase II inhibitor 20 induces apoptosis and has broad-spectrum anticancer activity .
Ursolic acid is a naturally occurring triterpenoid that has orally active. Ursolic acid induces the apoptosis of human cancer cells through multiple signaling pathways. Ursolic acid has anti-inflammatory and anticarcinogenic activity .
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion .
5-epi-Arvestonate A is a sesquiterpenoid isolated from the whole plants of Seriphidium transiliense. 5-epi-Arvestonate A promotes melanogenic production by activating the transcription of microphthalmia-associated transcription factor (MITF) and tyrosinase family genes. 5-epi-Arvestonate A inhibits the expression of IFN-γ-chemokine through the JAK/STAT signaling pathway in immortalized human keratinocyte (HaCaT) cells .
REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion .
Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1 .
DJ101 is a potent and metabolically stable tubulin inhibitor. DJ101 targets the colchicine binding site and overcomes taxane resistance. DJ101 also inhibits melanoma tumor growth and lung metastasis. DJ101 can be used for prostate cancer research .
Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1 .
Box5 TFA is a potent Wnt5a antagonist. Box5 TFA inhibits Wnt5a signaling and inhibits Wnt5a-mediated Ca 2+ release. Box5 TFA inhibits cell migration. Box5 TFA has the potential for the research of melanoma .
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanomacells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanomacells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
Fibronectin Type III Connecting Segment Fragment 1-25 is a peptide that is responsible for melanomacell adhesion, and plays an important role in development of the peripheral nervous system in chicken .
Box5 is a potent Wnt5a antagonist. Box5 inhibits Wnt5a signaling and inhibits Wnt5a-mediated Ca 2+ release. Box5 inhibits cell migration. Box5 has the potential for the research of melanoma .
Tyrosinase (192-200), human mouse is a nonapeptide. Tyrosinase (192-200), human mouse can be recognized by cytolytic T cell (CTL) on the HLA-B44 molecule. Tyrosinase (192-200), human mouse can be used in research of melanoma associated cancers .
Gp100 (25-33), mouse sequence is found in residues 25 to 33 of the mouse self/tumor antigen glycoprotein (mgp100). Mgp100 is an enzyme involved in pigment synthesis, and the epitope fragment is expressed in both normal melanocytes and melanomacells .
Gp100 (25-33), human (Hgp100 (25-33)) is the amino acids 25-33 fragment of the human melanoma antigen. It is a 9-amino acid (AA) epitope restricted by H-2D b and recognized by the T cells .
Gp100 (25-33), mouse TFA sequence is found in residues 25 to 33 of the mouse self/tumor antigen glycoprotein (mgp100). Mgp100 is an enzyme involved in pigment synthesis, and the epitope fragment is expressed in both normal melanocytes and melanomacells .
Gp100 (25-33), human TFA (Hgp100 (25-33) TFA) is the amino acids 25-33 fragment of the human melanoma antigen. It is a 9-amino acid (AA) epitope restricted by H-2D b and recognized by the T cells .
LyP-2 is a peptide that homes to tumor lymphatics. LyP2 homes to lymphatics of C8161 melanomas and cervical carcinomas and K14-HPV16 skin, but not to MDA-MB435 tumors, showing heterogeneity in the molecular markers of tumor cells and lymphatics .
MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanomacells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
Properdistatin is a peptide derived from the thrombospondin 1 (TSP-1) domain of properdin. Properdistatin inhibits angiogenesis and improves vascular function. Properdistatin has the potential for the research of melanoma .
REDV is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV can be used for the research of cell adhesion .
REDV TFA is the minimal active sequence within the CS5 site of the alternatively spliced type III connecting segment (IIICS) region of fibronectin. REDV TFA can mediate adhesion to the IIICS region of plasma fibronectin by binding the integrin alpha 4 beta 1(α4β1). REDV TFA can be used for the research of cell adhesion .
L-Glutamic γ-monohydroxamate is an antitumor agent, inhibits cell proliferation. L-Glutamic γ-monohydroxamate selectively inhibits the uptake of L-histidine into microvascular endothelial cell. L-Glutamic γ-monohydroxamate, as a vanadium ligand, activates glucose uptake and metabolism, thus decreases the blood glucose levels in vivo .
Vibostolimab is an anti-TIGIT (T cell immunoglobulin and ITIM domain) monoclonal antibody. Vibostolimab shows antitumor activity, and can be used in non-small cell lung cancer (NSCLC) and melanoma research .
Eftilagimod alfa (IMP321) is a recombinant LAG-3Ig fusion protein that binds to MHC class II. Eftilagimod alfa mediates antigen-presenting cell (APC) activation followed by CD8 T-cell activation. Eftilagimod alfa can be used for metastatic melanoma and metastatic breast carcinoma research .
Ipilimumab is a fully human monoclonal antibody IgG1κ that blocks the inhibitory receptor cytotoxic T lymphocyte antigen 4 (CTLA-4) on T cells. Ipilimumab can be used in unresectable or metastatic melanoma (MM) studies .
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 .
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells .
Flanvotumab (IMC-20D7S) is a human monoclonal antibody targeting to tyrosinase-related protein (TYRP1), specifically expressed in melanocytes and melanomacells. Flanvotumab acts function via natural killing-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Flanvotumab has potent anti-tumor activity and good tolerance .
Salviolone is a natural diterpenoid derivative that can against melanomacells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanomacells .
Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l .
Reticulol (K 251-1) is an inhibitor of cyclic adenosine 3', 5'-monophosphate phosphodiesterase. Reticulol shows antitumor activity independent with cell cycle arrest or apoptosis. Reticulol inhibits cell growth of murine melanomacells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma .
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanomacell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities .
Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanomacells .
Dihydrodehydrodiconiferyl alcohol (compound 2) is a kind of neolignan. Dihydrodehydrodiconiferyl alcohol can be isolated from Anogeissus acuminata. Dihydrodehydrodiconiferyl alcohol has specific cytotoxic activity on melanoma cancer cell line .
Picrocrocin, an apocarotenoid found in Saffron. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanomacells .
Chelidonine, an isoquinoline alkaloid, can be isolated from Chelidonium majus L.. Chelidonine causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, and prevents cell cycle progression of stem cells in Dugesia japonica. Chelidonine has cytotoxic activity against melanomacell lines. with anticancer and antiviral activity .
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanomacells. Epirosmanol also exhibits DPPH radical scavenging activity .
3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside, a saponin, is isolated from Polaskia chichipe Backbg. 3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside shows ability to inhibit melanin biosynthesis by B16 melanomacell with inhibitory activity 84.2% at 100μM[1].
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanomacells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanomacells .
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanomacells. Graveoline also exhibits antifungal activity .
Cryptomeridiol can be isolated from Phaulopsis imbricata. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH-stimulated B16 melanomacells .
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
Gochnatiolide A is a dimeric sesquiterpene that can be found in Ainsliaea henryi. Gochnatiolide A exhibits antiproliferative activity against the kidney, melanoma, ovarian-resistant and glioma cell lines .
Machilin A is a lignan isolated from the methanolic extract of Phoebe bark. Machilin A inhibits melanin biosynthesis in B-16 mouse melanomacells with an IC50 of 39.9 μM.
Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity . Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanomacells .
Pancratistatin is an isoquinoline alkaloid that can be isolated from Hymenocallis littoralis. Pancratistatin induces apoptosis of human melanomacells. Pancratistatin can be used for the research of neuroblastoma, leukemia and breast cancer .
Sanggenol L induces caspase-dependent and caspase-independent apoptosis in melanoma skin cancer cells . Sanggenol L induces of apoptosis via suppression of PI3K/Akt/mTOR signaling and cell cycle arrest via activation of p53 in p
Citropten (5,7-Dimethoxycoumarin) is a coumarin isolated from bergamot oil. Citropten (5,7-Dimethoxycoumarin) has an antiproliferative activity against A2058 human melanomacell line .
Cardanol monoene (Cardanol C15:1) is a phenolic compound which can be found in cashew nut shell liquid. Cardanol monoene can induce mitochondria-associated apoptosis in human melanomacells .
Neorauflavane is a potent tyrosinase inhibitor derived from Campylotropis hirtella, with an IC50 value of 30 nM for tyrosinase monophenolase activity and an IC50 value of 500 nM for diphenolase activity. Neorauflavane can effectively reduce the melanin content of B16 melanomacells .
Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models .
3'-Deoxy-4-O-methylsappanol shows cytotoxicity against melanoma HMV II cell (IC50=50.4 μM) and has significant anti-melanogenic activities (EC50=72 μM) .
Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
Lankacidin C is an inhibitor of protein synthesis in vitro. Lankacidin C inhibits the activity of L1210 leukemia, B16 melanoma and 6C3 HED/OG lymphosarcoma cell lines. Lankacidin C has antibacterial activity and antitumor activity .
Lycorine hydrochloride is the main active ingredient of the herbal medicine derived from Lycoris radiata (L’Her.) Herb. and is also a melanoma vasculogenic inhibitor and has anti-tumor activity . Lycorine hydrochloride effectively inhibits mitotic proliferation of Hey1B cells (IC50 of 1.2 μM) .
Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid, also known as ganoderic acid 24. Lanosta-7,9(11),24-trien-3α-hydroxy-26-oic acid shows high cytotoxicity against cancer cells, such as human lung cancer cells CH27, melanomacells M21, and oral cancer cells HSC-3 .
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanomacells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
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 melanomacells. 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 .
Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity .
Vanicoside E is an antioxidant and antitumor agent. Vanicoside E inhibits L-Tyrosine (HY-N0473) and L-DOPA (HY-N0304) with IC50s of 45.23 μM and 189.96 μM, respectively .
Cyclic-di-GMP is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP can be used in cancer research .
Cyclic-di-GMP sodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP sodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP sodium can be used in cancer research .
Cyclic-di-GMP diammonium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP diammonium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP diammonium can be used in cancer research .
Cyclic-di-GMP disodium is a STING agonist and a bacterial second messenger that coordinates different aspects of bacterial growth and behavior, including motility, virulence, biofilm formation, and cell cycle progression. Cyclic-di-GMP disodium has anti-cancer cell proliferation activity and also induces elevated CD4 receptor expression and cell cycle arrest. Cyclic-di-GMP disodium can be used in cancer research .
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
Ursolic acid is a naturally occurring triterpenoid that has orally active. Ursolic acid induces the apoptosis of human cancer cells through multiple signaling pathways. Ursolic acid has anti-inflammatory and anticarcinogenic activity .
5-epi-Arvestonate A is a sesquiterpenoid isolated from the whole plants of Seriphidium transiliense. 5-epi-Arvestonate A promotes melanogenic production by activating the transcription of microphthalmia-associated transcription factor (MITF) and tyrosinase family genes. 5-epi-Arvestonate A inhibits the expression of IFN-γ-chemokine through the JAK/STAT signaling pathway in immortalized human keratinocyte (HaCaT) cells .
CD63 protein acts as a receptor for TIMP1, activating cell signaling pathways and promoting cell survival. It plays a key role in integrin signaling, leading to activation of AKT, FAK/PTK2, and MAP kinases. CD63 Protein, Human (Cell-Free, His) is the recombinant human-derived CD63 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CD63 Protein, Human (Cell-Free, His) is 237 a.a., with molecular weight of 31.5 kDa.
Cinnamic acid-d6 is the deuterium labeled Cinnamic acid. Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
Octacosane-d58 is the deuterium labeled Octacosane[1]. Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[2][3][4].
Cinnamic acid- 13C3 (3-Phenylacrylic acid- 13C3) is the 13C labeled Cinnamic acid (HY-N0610A). Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells .
Benzyl isothiocyanate-d7 is the deuterium labeled Benzyl isothiocyanate. Benzyl isothiocyanate is a member of natural isothiocyanates with antimicrobial activity[1][2]. Benzyl isothiocyanate potent inhibits cell mobility, migration and invasion nature and matrix metalloproteinase-2 (MMP-2) activity of murine melanomacells[2].
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