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Anti-melanoma agent 3 (compound 5cb) is a 2-aryl-4-benzoyl-imidazole (ABI) derivative and an inhibitor of melanoma xenogeneic tumors. Anti-melanoma agent 3 exerts anticancer activity by interacting with the colchicine binding site to inhibit tubulin polymerization .
Anticancer agent 106 (compound 10ic) is an anticancer agent that induces apoptosis in B16-F10 melanoma cells. 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 .
Salviolone is a natural diterpenoid derivative that can against melanoma cells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells .
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells . 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity .
Tyrosinase-IN-10 (Compound 23) is a partially competitive tyrosinase inhibitor with an IC50 of 1.6 μM against tyrosinase activity from human melanoma cell lysates .
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanoma cells. Graveoline also exhibits antifungal activity .
6-Acetylnimbandiol (6-O-Acetylnimbandiol) is a non-cytotoxic tyrosinase inhibitor (IC50=69.85 μM) that effectively inhibits melanin production and MITF expression. 6-Acetylnimbandiol can be used in melanoma research .
Cryptomeridiol can be isolated from Phaulopsis imbricata. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH-stimulated B16 melanoma cells .
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 melanoma cells. TT-012 inhibits the growth of high-MITF melanoma cells, and inhibits the tumor growth and metastasis with tolerable toxicity to liver and immune cells in animal models .
RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
Etaracizumab (LM 609) is an αvβ3 integrin IgG1 monoclonal antibody. Etaracizumab inhibits angiogenesis and melanoma tumor growth. Etaracizumab can be used to research anticancer .
Prolgolimab (BCD-100) is a human IgG1 anti-PD-1 monoclonal antibody containing the Fc-silencing 'LALA' mutation. Prolgolimab can be used for the research of advanced melanoma .
Nurulimab (BCD-145) is an anti-cytotoxic T lymphocyte antigen-4 (anti-CTLA-4) human monoclonal antibody. Nurulimab can be can be used in 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 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
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 .
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 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC50 of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma .
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 .
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 .
(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 .
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanoma cell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities .
Benserazide is a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the research of melanoma .
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 .
Anticancer agent 105 is a compound based on thienopyrimidine scaffold, with with good safety and anticancer properties. Anticancer agent 105 shows selective toxicity towards melanoma cancer, and induces apoptosis. And Anticancer agent 105 significantly inhibits the metastatic nodules, even in pulmonary metastatic melanoma mouse model .
ADT-OH is a hydrogen sulfide-releasing donor. ADT-OH induces apoptosis and inhibits the development of melanoma in vivo by upregulating FADD. ADT-OH has the potential for the research of cancer 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 .
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 .
Immune initiator-1 (Compound 1a) is an amino acid-modified near-infrared Aza-BODIPY photosensitizer, acts as an immune initiator for potent photodynamic research in melanoma .
Palmitoleoyl 3-carbacyclic phosphatidic acid (3ccPA 16:1) is an intermediately potent inhibitor of autotaxin (ATX) with an IC50 of 620 nM. Palmitoleoyl 3-carbacyclic phosphatidic acid can be used for melanoma research .
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 melanoma cell 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 .
Tyrosinase-IN-17 (Compound 5b) is a lipophilic, skin-permeable, and non-cytotoxic Tyrosinase inhibitor (pIC50=4.99). Tyrosinase-IN-17 can be used for research on melanin-related diseases, such as melanoma, melanogenesis, etc .
Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells .
ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model .
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) .
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 .
Picrocrocin, an apocarotenoid found in Saffron. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells .
2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM .
4'-Bromo-resveratrol is a potent and dual inhibitor Sirtuin-1 and Sirtuin-3. 4'-Bromo-resveratrol inhibits melanoma cell growth through mitochondrial metabolic reprogramming. 4'-Bromo-resveratrol imparts antiproliferative effects in melanoma cells through a metabolic reprogramming and affecting the cell cycle and apoptosis signaling .
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 melanoma cells through activation of PPARγ .
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 melanoma cells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma .
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 melanoma cells (SK-MEL-28) under broad-band visible light (400-700 nm) with EC50 values of 740 pM .
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 .
GD3 Ganglioside is a prominent ganglioside of human melanoma. GD3 Ganglioside is an inducer of mitochondrial permeability. GD3 ganglioside directly targets mitochondria in a bcl-2-controlled fashion. GD3 ganglioside is rapidly synthesized from accumulated ceramide after the clustering of death-inducing receptors and triggers apoptosis .
Tremelimumab (Ticilimumab) is a fully human monoclonal antibody specific for cytotoxic T-lymphocyte antigen-4 (CTLA-4) and can be used for metastatic melanoma research .
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 .
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 .
IVMT-Rx-3 is a inhibitor of SDCBP targeting of the PDZ1 and PDZ2 Domains of MDA-9/Syntenin. IVMT-Rx-3 blocks MDA-9/Syntenin interaction with Src, reduces NF-κB activation, and inhibits MMP-2/MMP-9 expression. IVMT-Rx-3 inhibits Melanoma Metastasis [1]
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 melanoma cells .
TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research .
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 melanoma cell lines. Palmostatin B inhibits Ras depalmitoylation in cells .
ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro .
Anticancer agent 174 (BA-3) is an anticancer agent. Anticancer agent 174 induces tumor cell apoptosis through the mitochondrial pathway. Anticancer agent 174 inhibits cancer cell proliferation in melanoma mouse xenograft model .
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 .
ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro .
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 .
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 melanoma cell lines. Exarafenib has anticancer 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 .
(−)-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 melanoma cells .
Antitumor agent-56 (Compound 33) is a triptolide derivative with antitumor, anti-inflammatory and NO release activities. Antitumor agent-56 significantly inhibits the growth of melanoma. Antitumor agent-56 is orally active .
Glembatumumab is a fully human IgG2 monoclonal antibody directed against the extracellular structural domain of GPNMB expressed in human breast cancer and melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethyl auristatin E to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-agent coupling (ADC) with antitumor activity .
(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM .
(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM .
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 .
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. 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) .
Melanin probe-1 is an 18F-picolinamides based PET probe. Melanin probe-1 can be used for PET imaging of malignant melanoma. Melanin probe-1 exhibits high tumor targeting efficiency, excellent tumor imaging contrasts, desirable biodistribution patterns, and good in vivo stability .
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanoma cells. Epirosmanol also exhibits DPPH radical scavenging activity .
Arylsulfonamide 64B (HIF inhibitor 64B) is an inhibitor of the hypoxia-induced factor (HIF). Arylsulfonamide 64B inhibits hypoxia/HIF-induced expression of c-Met and CXCR4 and reduces primary tumor growth and metastasis of uveal melanoma mouse model .
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 .
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 melanoma cells 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 melanoma cells with S100B over those without S100B . Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM) .
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 melanoma cell lines. with anticancer and antiviral activity .
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
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 .
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 .
N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity .
BRD4 Inhibitor-28 (Compound 18) is an orally active BRD4 Inhibitor. BRD4 Inhibitor-28 inhibits BRD40-BD1, BRD40-BD2 with IC50s of 15, 55 nM. BRD4 Inhibitor-28 also inhibits BRD2-BD1, BRD3-BD1, BRDT-BD1 with IC50s of 19, 25, 68 nM. BRD4 Inhibitor-28 has anti-melanoma activity .
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 .
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 melanoma cells. 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) .
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 .
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 .
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 .
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders .
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 melanoma cell growth .
Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease .
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor . CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis .
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 .
D-threo-PDMP hydrochloride is a glucosylceramide (GlcCer) synthase inhibitor that inhibits glucosylceramide (GlcCer) and lactosylceramide (LacCer) levels in B16 melanoma cells. 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 .
Methyl tetradecanoate-d27 is the deuterium labeled Methyl myristate. Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma[1].
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. .
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 melanoma cell lines expressing mPGES1 .
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 melanoma cell 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 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanoma cells .
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 melanoma cells. 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 .
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
Toripalimab is the first domestic anti-tumor PD-1 antibody in China. Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma .
Anticancer agent 107(Compd 11jc) has significant antitumor activity and can be used as an anticancer agent in the study of pulmonary metastatic melanoma .
Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma .
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].
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 .
Machilin A is a lignan isolated from the methanolic extract of Phoebe bark. Machilin A inhibits melanin biosynthesis in B-16 mouse melanoma cells with an IC50 of 39.9 μM.
EGFR-IN-58 (Compound 4a) is a potent, ATP-competitive, and selective EGFR inhibitor. EGFR-IN-58 shows potent cytotoxicity against melanoma, colon, and blood cancers .
Pancratistatin is an isoquinoline alkaloid that can be isolated from Hymenocallis littoralis. Pancratistatin induces apoptosis of human melanoma cells. Pancratistatin can be used for the research of neuroblastoma, leukemia and breast cancer .
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 melanoma cells .
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.
Citropten (5,7-Dimethoxycoumarin) is a coumarin isolated from bergamot oil. Citropten (5,7-Dimethoxycoumarin) has an antiproliferative activity against A2058 human melanoma cell 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 melanoma cells .
Bruceantin(NSC165563) is first isolated from Brucea javanica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
Porcn-IN-2 (Example 107) is a Wnt inhibitor, with an IC50 value of 0.05 nM. Porcn-IN-2 can be used for research of cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia, etc .
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 melanoma cells .
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 melanoma cells .
RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model .
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 .
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 .
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
Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanoma cells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggers apoptosis .
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) .
WYC-209, a synthetic retinoid, is a retinoic acid receptor (RAR) agonist. WYC-209 induces apoptosis primarily via the caspase 3 pathway (IC50=0.19 μM for inmalignant murine melanoma TRCs), and has long-term effects with little toxicity .
IACS-8779 disodium is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy. IACS-8779 disodium shows robust activation of the STING pathway in vitro and a superior systemic anti-tumor response in the B16 murine model of melanoma .
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 .
Darovasertib (LXS196) is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. Darovasertib has the potential for uveal melanoma research .
Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (Ki= 0.0023 M) and mouse pancreas (Ki= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis .
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).
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 .
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 melanoma cells through modulation of Ca 2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 .
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 melanoma cells[2].
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.
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription . Lycorine is also a melanoma vasculogenic inhibitor . Lycorine can be used for the study of prostate cancer and metabolic diseases .
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells 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 melanoma cell proliferation inhibitors. γ-Linolenic Acid methyl ester inhibits ADP-induced blood platelet aggregation and induces apoptosis .
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 melanoma cell line .
2-Thiouracil- 13C, 15N2 is the 13C, 15N labeled 2-Thiouracil. 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
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 .
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 melanoma cells .
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 .
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 .
BAY-985 is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy .
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 .
Calpain inhibitors are lipophilic and show moderate to good antiproliferative activity in vitro compared with melanoma cell 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 melanoma cells (SK-MEL-28) and normal melanocytes (NHEM), with IC50 values of 5.3 and 10.1 μM, respectively .
Flanvotumab (IMC-20D7S) is a human monoclonal antibody targeting to tyrosinase-related protein (TYRP1), specifically expressed in melanocytes and melanoma cells. Flanvotumab acts function via natural killing-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Flanvotumab has potent anti-tumor activity and good tolerance .
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 .
Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
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 melanoma cells. 16,16-Dimethyl prostaglandin A1 also inhibits viral replication in both HSV and HIV-1 infection systems .
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 melanoma cell 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 melanoma cells. Methyl p-coumarate also has strong in vitro inhibitory effect on A. alternata and other pathogens .
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 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
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 .
Leukotriene B4 ethanolamide (LTB4 ethanolamide) is an antagonist and a partial agonist for Leukotriene B4 (LTB4) receptor 1 (BLTR1). Leukotriene B4 ethanolamide ameliorates the tumor progression, which is only asscociated with inflammation .
Elsinochrome A is a perylene quinone photosensitizer, and can generate reactive oxygen species (ROS) to induce apoptosis and autophagy under light excitation. Elsinochrome A also shows antifungal activity against C. albicans biofilm through photodynamic antimicrobial chemotherapy (PACT). Elsinochrome A can be used for research of photodynamic therapy (PDT) (Ex: 460 nm) .
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction .
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 .
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 .
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 melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
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 .
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, melanoma cells M21, and oral cancer cells HSC-3 .
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 .
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 .
Apovincamine (cis-Apovincamine) is an indole alkaloid isolated from the Malaysian Alstonia pneumatophora (Apocynaceae). Apovincamine shows anti-melanogenesis activity .
KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models .
KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects .
KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity .
Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity .
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells 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 .
JC2-11 is an inhibitor of inflammatory corpuscles. JC2-11 inhibits domain-containing protein NLRC 4, absent in melanoma 2 (AIM 2) and non-canonical (NC) inflammatory corpuscles. JC2-11 reduces the secretion of caspase-1 (p20), the cleavage of gasdermin D (GSDMD), and the releases of IL-1β and lactate dehydrogenases (LDH) in inflammatory bodies. JC2-11 inhibits the activation of inflammatory bodies by destroying the production of reactive oxygen species and the activity of caspase-1 .
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 melanoma cell growth .
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 .
p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .
RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities .
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation .
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 .
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 .
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 melanoma cells (IC50=3.84 μg/mL) .
Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities .
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. Oglufanide inhibits vascular endothelial growth factor (VEGF). Oglufanide can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide shows antitumor and anti-angiogenesis activities .
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC) .
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 .
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
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 .
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 .
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 .
PROTAC SMARCA2 degrader-2 is a potent and selective SMARCA2/4 PROTAC degrader with an IC50 of <0.1 μΜ in HeLa HiBiT assay. PROTAC SMARCA2 degrader-2 is extracted from patent WO2023287787A1 and has the potential for SMARCA4-related or deficient cancer research .
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 .
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 .
Gypenoside LXXV, isolated from Gynostemma pentaphyllum, is one of the deglycosylated shapes of ginsenoside Rb1. Gypenoside LXXV significantly reduces cancer cell viability and displays an anti-cancer effect .
DHODH-IN-26 (compound B2) is a mitochondria-targeting DHODH inhibitor. DHODH-IN-26 shows anticancer activity, triggers the formation of reactive oxygen species (ROS), promots mitochondrial lipid peroxidation, and induces ferroptosis .
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression .
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .
Momordicoside L is a Cucurbitane Triterpenoid, that can be isolated from the leaves of Momordica charantia. Momordicoside L shows anticancer activity .
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 .
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 .
Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle . Antitumor activity .
Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research .
WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively .
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 .
Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct .
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 .
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 .
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 .
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 .
BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu .
BOLD-100 (NKP-1339; IT-139) free base is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution .
Phospholipid PL1 is a phospholipid-derived nanoparticle, can deliver costimulatory receptor mRNA (CD137 or OX40) to T cells. Phospholipid PL1 could induce the activation of various immune cells, including T cells and dendritic cells (DCs) in order to boost antitumor immunity .
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
c-Fms-IN-12 (Compound 4g) is an FMS kinase inhibitor. c-Fms-IN-12 can also inhibits c-KIT. c-Fms-IN-12 is a potential broad-spectrum anticancer agent against multiple cancer types. c-Fms-IN-12 induces A549 cell apoptosis .
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 .
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 .
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 .
Phospholipid PL1 is a phospholipid-derived nanoparticle, can deliver costimulatory receptor mRNA (CD137 or OX40) to T cells. Phospholipid PL1 could induce the activation of various immune cells, including T cells and dendritic cells (DCs) in order to boost antitumor immunity .
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 melanoma cells 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 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
MAGE-3 (271-279) is a 271-279 residue peptide derived from melanoma antigens encoded by MAGE-3. MAGE-3 is a cytolytic T lymphocyte (CTL)-defined MAGE-3 protein associated with the human leukocyte antigen (HLA)-A2 molecule. MAGE-3 is overexpressed in different human tumor types, including malignant melanoma, but not by normal tissues except for testis and placenta .
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 .
Fibronectin Type III Connecting Segment Fragment 1-25 is a peptide that is responsible for melanoma cell 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 .
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 .
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 .
MAGE-3 Antigen (167-176) (human) is a polypeptide containing eight amino acids. MAGE-3 Antigen (167-176) (human) is a human leukocyte antigen HLA-B44 molecules epitope encoded by melanoma antigen gene (MAGE) .
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 (619-627) is amino acids 619 to 627 fragment of human melanoma antigen glycoprotein 100 (gp100). Gp100 has been a widely studied target for melanoma immunotherapy .
Gp100 (619-627) acetate is amino acids 619 to 627 fragment of human melanoma antigen glycoprotein 100 (gp100). Gp100 has been a widely studied target for melanoma immunotherapy .
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 melanoma cells .
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 melanoma cells .
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 .
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 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction .
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. Oglufanide inhibits vascular endothelial growth factor (VEGF). Oglufanide can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide shows antitumor and anti-angiogenesis activities .
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 .
Etaracizumab (LM 609) is an αvβ3 integrin IgG1 monoclonal antibody. Etaracizumab inhibits angiogenesis and melanoma tumor growth. Etaracizumab can be used to research anticancer .
Prolgolimab (BCD-100) is a human IgG1 anti-PD-1 monoclonal antibody containing the Fc-silencing 'LALA' mutation. Prolgolimab can be used for the research of advanced melanoma .
Nurulimab (BCD-145) is an anti-cytotoxic T lymphocyte antigen-4 (anti-CTLA-4) human monoclonal antibody. Nurulimab can be can be used in research of melanoma .
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 .
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 .
Tremelimumab (Ticilimumab) is a fully human monoclonal antibody specific for cytotoxic T-lymphocyte antigen-4 (CTLA-4) and can be used for metastatic melanoma research .
Glembatumumab is a fully human IgG2 monoclonal antibody directed against the extracellular structural domain of GPNMB expressed in human breast cancer and melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethyl auristatin E to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-agent coupling (ADC) with antitumor activity .
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 .
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 .
Toripalimab is the first domestic anti-tumor PD-1 antibody in China. Toripalimab is a selective, recombinant, humanized monoclonal antibody against PD-1. Toripalimab is able to bind to PD-1 and block the interaction with its ligands. Toripalimab has exhibited primary anti-tumor effects in tumors such as melanoma, lung cancer, digestive tract tumors, hepatobiliary and pancreatic tumors, neuroendocrine neoplasms, nasopharyngeal carcinoma and urothelial carcinoma .
Flanvotumab (IMC-20D7S) is a human monoclonal antibody targeting to tyrosinase-related protein (TYRP1), specifically expressed in melanocytes and melanoma cells. Flanvotumab acts function via natural killing-mediated antibody-dependent cell-mediated cytotoxicity (ADCC). Flanvotumab has potent anti-tumor activity and good tolerance .
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 .
Salviolone is a natural diterpenoid derivative that can against melanoma cells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells .
Graveoline (Rutamine) is an anti-cancer agent that can trigger apoptosis and autophagy in skin melanoma cells. Graveoline also exhibits antifungal activity .
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 .
6-Acetylnimbandiol (6-O-Acetylnimbandiol) is a non-cytotoxic tyrosinase inhibitor (IC50=69.85 μM) that effectively inhibits melanin production and MITF expression. 6-Acetylnimbandiol can be used in melanoma research .
Cryptomeridiol can be isolated from Phaulopsis imbricata. Cryptomeridiol has melanogenesis inhibitory activity in the α-MSH-stimulated B16 melanoma cells .
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 .
Inuviscolide is an apoptosis inducer. Inuviscolide can induce of G2/M arrest in human melanoma cell lines. Inuviscolide exhibits antineoplastic and anti-inflammatory activities .
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 .
Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells .
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) .
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 melanoma 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 melanoma cells and human lung tumor cells. Reticulol protects its lung metastasis via the bloodstream by inhibiting the growth of B16F10 melanoma .
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 .
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanoma cells. Epirosmanol also exhibits DPPH radical scavenging activity .
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 melanoma cell lines. with anticancer and antiviral activity .
N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma 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 melanoma cell 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 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitory activity on melanin production in B16 melanoma cells .
Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma .
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 .
Machilin A is a lignan isolated from the methanolic extract of Phoebe bark. Machilin A inhibits melanin biosynthesis in B-16 mouse melanoma cells with an IC50 of 39.9 μM.
Pancratistatin is an isoquinoline alkaloid that can be isolated from Hymenocallis littoralis. Pancratistatin induces apoptosis of human melanoma cells. Pancratistatin can be used for the research of neuroblastoma, leukemia and breast cancer .
Citropten (5,7-Dimethoxycoumarin) is a coumarin isolated from bergamot oil. Citropten (5,7-Dimethoxycoumarin) has an antiproliferative activity against A2058 human melanoma cell 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 melanoma cells .
Bruceantin(NSC165563) is first isolated from Brucea javanica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
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 melanoma cells .
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 melanoma cells .
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 .
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
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) .
Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (Ki= 0.0023 M) and mouse pancreas (Ki= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis .
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. Lycorine is a potent and orally active SCAP inhibitor with a Kd value 15.24 nM. Lycorine downregulates the SCAP protein level without changing its transcription . Lycorine is also a melanoma vasculogenic inhibitor . Lycorine can be used for the study of prostate cancer and metabolic diseases .
Elsinochrome A is a perylene quinone photosensitizer, and can generate reactive oxygen species (ROS) to induce apoptosis and autophagy under light excitation. Elsinochrome A also shows antifungal activity against C. albicans biofilm through photodynamic antimicrobial chemotherapy (PACT). Elsinochrome A can be used for research of photodynamic therapy (PDT) (Ex: 460 nm) .
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 .
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, melanoma cells M21, and oral cancer cells HSC-3 .
Apovincamine (cis-Apovincamine) is an indole alkaloid isolated from the Malaysian Alstonia pneumatophora (Apocynaceae). Apovincamine shows anti-melanogenesis activity .
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells 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 .
p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .
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 .
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. Oglufanide inhibits vascular endothelial growth factor (VEGF). Oglufanide can stimulate the immune response to hepatitic C virus (HCV) and intracellular bacterial infections. Oglufanide shows antitumor and anti-angiogenesis activities .
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 .
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 .
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 .
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 .
Gypenoside LXXV, isolated from Gynostemma pentaphyllum, is one of the deglycosylated shapes of ginsenoside Rb1. Gypenoside LXXV significantly reduces cancer cell viability and displays an anti-cancer effect .
Momordicoside L is a Cucurbitane Triterpenoid, that can be isolated from the leaves of Momordica charantia. Momordicoside L shows 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 .
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively .
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 .
MIA proteins exhibit significant growth inhibitory effects on melanoma cells in vitro, extending their effects to various neuroectodermal tumors such as gliomas. In addition to playing an inhibitory role in cell growth, MIA proteins are also involved in molecular interactions, interacting with FASLG and TMIGD2. MIA Protein, Human (His) is the recombinant human-derived MIA protein, expressed by E. coli , with C-6*His labeled tag. The total length of MIA Protein, Human (His) is 107 a.a., with molecular weight of ~14.0 kDa.
MIA proteins exhibit significant growth inhibitory effects on melanoma cells in vitro, extending their effects to various neuroectodermal tumors such as gliomas. In addition to playing an inhibitory role in cell growth, MIA proteins are also involved in molecular interactions, interacting with FASLG and TMIGD2. MIA Protein, Human (N-His) is the recombinant human-derived MIA protein, expressed by E. coli , with N-6*His labeled tag. The total length of MIA Protein, Human (N-His) is 107 a.a., with molecular weight of ~14.0 kDa.
GSDMC protein serves as the precursor of pore-forming proteins and undergoes cleavage to release Gasdermin-C. This N-terminal moiety binds to the membrane, forming pores with an inner diameter of 10 to 15 nm and inducing pyroptosis. GSDMC Protein, Human (His-SUMO) is the recombinant human-derived GSDMC protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of GSDMC Protein, Human (His-SUMO) is 508 a.a., with molecular weight of ~73.7 kDa.
IL-19 Protein, Human is a member of the Interleukin-10 family. The biological functions and clinical implications of Interleukin-19 is still undefined.
MAGEA4 protein critically regulates cell proliferation by inhibiting G1 phase arrest and negatively modulates p53-mediated apoptosis. Its role in controlling key checkpoints emphasizes its impact on cellular homeostasis, suggesting significance in averting aberrant cell growth. MAGEA4 Protein, Human (HEK293, His) is the recombinant human-derived MAGEA4 protein, expressed by HEK293, with C-10*His labeled tag. The total length of MAGEA4 Protein, Human (HEK293, His) is 317 a.a., with molecular weight of 36.7 kDa.
Otoraplin/OTOR Protein, Human (CHO) is a protein encoded by OTOR gene, is homologous to the protein encoded by CDRAP/MIA, and may acts in cartilage development and maintenance.
PRAME is located in the CRL2 E3 ubiquitin-protein ligase complex and directs ubiquitination and degradation, specifically targeting the truncated MSRB1/SEPX1 selenoprotein. It is recruited to active promoter regions and is involved in chromatin regulation. Melanoma antigen preferentially/PRAME, Human (His) is the recombinant human-derived Melanoma antigen preferentially/PRAME, expressed by E. coli , with N-6*His labeled tag. The total length of Melanoma antigen preferentially/PRAME, Human (His) is 509 a.a., with molecular weight of ~61.9 kDa.
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.
Interleukin-24 (IL-24) belongs to the IL10 family of cytokines that selectively induces apoptosis in cancer cells and is recognized during melanoma cell differentiation. IL-24 overexpression increases the expression of GADD family genes and induces cell apoptosis. IL-24 Protein, Human (HEK293, His) is the recombinant human-derived IL-24 protein, expressed by HEK293 , with C-10*His labeled tag. The total length of IL-24 Protein, Human (HEK293, His) is 155 a.a., with molecular weight of ~35 kDa.
IL-24 protein, produced by T-cells, regulates immune responses, tissue homeostasis, defense, and oncogenesis. It induces type I interferon response in influenza infection, signaling through IL20RA/IL20RB or IL20RB/IL22RA1 receptor complexes to stimulate JAK1-STAT3 and MAPK pathways. IL-24 promotes secretion of IL8 and MMP1, maintains ER homeostasis, and serves as a quality control mechanism for the ubiquitin proteasome system. IL-24 Protein, Human (HEK293, Fc) is the recombinant human-derived IL-24 protein, expressed by HEK293 , with C-mFc labeled tag. The total length of IL-24 Protein, Human (HEK293, Fc) is 155 a.a., with molecular weight of ~44.6 KDa.
IL-24 protein, produced by T-cells, regulates immune responses, tissue homeostasis, defense, and oncogenesis. It induces type I interferon response in influenza infection, signaling through IL20RA/IL20RB or IL20RB/IL22RA1 receptor complexes to stimulate JAK1-STAT3 and MAPK pathways. IL-24 promotes secretion of IL8 and MMP1, maintains ER homeostasis, and serves as a quality control mechanism for the ubiquitin proteasome system. Animal-Free IL-24 Protein, Human (His) is the recombinant human-derived animal-FreeIL-24 protein, expressed by E. coli, with C-His labeled tag. The total length of Animal-Free IL-24 Protein, Human (His) is 155 a.a., with molecular weight of ~19.10 kDa.
The MLANA protein is essential in melanosome biosynthesis, ensuring the stability of GPR143, and plays a key role in the expression, stability, transport, and processing of the melanocyte protein PMEL. Its interaction with PMEL and GPR143 highlights its integral role in the complex network required for second-stage melanosome formation. MLANA Protein, Human (His, B2M) is the recombinant human-derived MLANA protein, expressed by E. coli , with N-His, B2M labeled tag. The total length of MLANA Protein, Human (His, B2M) is 118 a.a., with molecular weight of ~27.2 kDa.
IL-24 Protein, a crucial immune regulatory cytokine, plays a pivotal role in modulating immune responses. Animal-Free IL-24 Protein, Mouse (His) is the recombinant mouse-derived animal-FreeIL-24 protein, expressed by E. coli , with C-His labeled tag. The total length of Animal-Free IL-24 Protein, Mouse (His) is 155 a.a., with molecular weight of ~18.94 kDa.
Syntenin-1; melanoma differentiation-associated protein 9; Pro-TGF-alpha cytoplasmic domain-interacting protein 18; Scaffold protein Pbp1; Syndecan-binding protein 1; SDCBP; MDA9; SYCL;
Syntenin-1 is a multifunctional adapter protein that coordinates multiple cellular processes, including transmembrane protein trafficking, neural and immune regulation, exosome biogenesis, and tumorigenesis. It actively regulates TGFB1 signaling and enhances SMAD2/3 activation, TGFB1-induced epithelial-mesenchymal transition (EMT), and cell migration. Syntenin-1 Protein, Human (C-His) is the recombinant human-derived Syntenin-1 protein, expressed by E. coli , with C-6*His labeled tag. The total length of Syntenin-1 Protein, Human (C-His) is 297 a.a., with molecular weight of ~ 32.0 kDa.
Syntenin-1; melanoma differentiation-associated protein 9; Pro-TGF-alpha cytoplasmic domain-interacting protein 18; Scaffold protein Pbp1; Syndecan-binding protein 1; SDCBP; MDA9; SYCL;
Syntenin-1 protein is known to mediate Syndecan signaling and has a PDZ domain that binds transmembrane proteins. It affects cytoskeletal membrane organization, cell adhesion, protein trafficking, and transcription factor activation. Syntenin-1 Protein, Human (N-His) is the recombinant human-derived Syntenin-1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of Syntenin-1 Protein, Human (N-His) is 298 a.a., with molecular weight of ~32 kDa.
GRO-alpha/CXCL1 protein attracts neutrophils and potentially contributes to inflammation through autocrine effects on endothelial cells. Processed forms of GRO-alpha, including GRO-alpha(4-73), GRO-alpha(5-73), and GRO-alpha(6-73), exhibit 30-fold greater chemotactic activity than the full-length protein. GRO-alpha/CXCL1 Protein, Human (His) is the recombinant human-derived GRO-alpha/CXCL1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GRO-alpha/CXCL1 Protein, Human (His) is 73 a.a., with molecular weight of 11.9 kDa.
GRO-alpha (CXCL1) Protein, with chemotactic properties, attracts and activates neutrophils during inflammatory responses. This hematoregulatory chemokine also suppresses hematopoietic progenitor cell proliferation, emphasizing its intricate role in hematopoiesis regulation. The truncated form KC(5-72) notably exhibits significantly enhanced hematopoietic activity in vitro. GRO-alpha/CXCL1 Protein, Mouse (His) is the recombinant mouse-derived GRO-alpha/CXCL1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of GRO-alpha/CXCL1 Protein, Mouse (His) is 68 a.a., with molecular weight of 11.5 kDa.
CXCL1 (Chemokine (C-X-C motif) ligand 1), also known as GRO alpha, NAP-3 or MGSA, belongs to the sub-family of CXC chemokine. CXCL1 is involved in the development of many inflammatory diseases, including the induction of angiogenesis and recruitment of neutrophils. CXCL1 is produced by many cell types, and activates CXCR2 and, at high levels, CXCR1. GRO-alpha/CXCL1 Protein, Human (HEK293, His) is produced in HEK293 cells with a C-Terminal His-tag. It consists of 73 amino acids (A35-N107).
AIM2 protein is a key sensor in the AIM2 inflammasome, which can activate the inflammasome in response to cytoplasmic dsDNA, thereby inducing pyroptosis. This complex is triggered by pathogens or injury signals and plays a critical role in innate immunity and inflammation. AIM2 Protein, Human is the recombinant human-derived AIM2 protein, expressed by E. coli , with tag free. The total length of AIM2 Protein, Human is 200 a.a., .
AIM2 protein is a key sensor in the AIM2 inflammasome, which can activate the inflammasome in response to cytoplasmic dsDNA, thereby inducing pyroptosis. This complex is triggered by pathogens or injury signals and plays a critical role in innate immunity and inflammation. AIM2 Protein, Human (His) is the recombinant human-derived AIM2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of AIM2 Protein, Human (His) is 200 a.a., .
AIM2 Protein, a member of the IFI20X/IFI16 family, exhibits potential regulatory functions in cell proliferation and tumorigenic reversion. Induced by interferon-gamma, AIM2 plays a key role in immune responses. Notably expressed in tissues like lymph node and appendix, AIM2 is a significant player in diverse cellular processes and immune-related functions. AIM2 Protein, Human (sf9, GST) is the recombinant human-derived AIM2 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of AIM2 Protein, Human (sf9, GST) is 343 a.a., with molecular weight of ~65.2 kDa.
The CDKN1A protein critically controls cell cycle progression and mediates DNA damage-induced G2 arrest through p53/TP53-dependent and CREB3L1-mediated p53-independent pathways. It inhibits cyclin-dependent kinase activity, blocking cell cycle progression by preventing phosphorylation of key substrates. CDKN1A Protein, Human (GST) is the recombinant human-derived CDKN1A protein, expressed by E. coli , with N-GST labeled tag. The total length of CDKN1A Protein, Human (GST) is 163 a.a., with molecular weight of 45 kDa.
Methyl tetradecanoate-d27 is the deuterium labeled Methyl myristate. Methyl myristate is a saturated fatty acid methyl ester obtained from the esterification of myristic acid. Methyl myristate shows a high melanin induction in B16F10 melanoma[1].
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-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.
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 .
Dacarbazine-d6 is the deuterium labeled Dacarbazine. Dacarbazine(DTIC-Dome; DTIC) is an antineoplastic agent. It has significant activity against melanomas.
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 melanoma cells[2].
2-Thiouracil- 13C, 15N2 is the 13C, 15N labeled 2-Thiouracil. 2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
p21 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 18 kDa, targeting to p21. It can be used for WB,ICC/IF assays with tag free, in the background of Human, Mouse, Rat.
p21 Antibody (YA254) is a non-conjugated and Rabbit origined monoclonal antibody about 18 kDa, targeting to p21. It can be used for WB assays with tag free, in the background of Human, Mouse.
![3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside](http://file.medchemexpress.com/product_pic/hy-n9521.gif)
