HA15

SKU: orb1223265

Description

HA15 targets specifically BiP/GRP78/HSPA5. HA15 exhibits anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

Images & Validation

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Key Properties

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CAS Number	1609402-14-3
MW	466.58
Purity	>98% (HPLC)
Formula	C₂₃H₂₂N₄O₃S₂
SMILES	CC(=O)Nc1nc(c2cccc(NS(=O)(=O)c3c4cccc(N(C)C)c4ccc3)c2)cs1
Target	GRP78\| HSPA5\| BiP
Solubility	DMSO : ≥ 50 mg/mL. 107.16 mM; H2O : < 0.1 mg/mL

Bioactivity

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In Vivo

HA15 (0.7 mg/mouse/day; i.h.; over 2 weeks) inhibits melanoma tumor development in mice, induces no apparent toxicity and no change in their behavior, body mass, or liver mass, suggesting an absence of hepatomegaly. HA15 (0.7 mg/mouse; i.p.; 5 days/week) suppresses MPM tumor growth In vivo. Animal model: 6-weeks female BALB/c nu/nu (nude) mice with A375 melanoma cells xenograft. Dosage: 0.7 mg/mouse/day dministration: Subcutaneous injection; over a period of 2 weeks. Result: Attenuated the development of tumors. Animal model: Mouse, NSG (NOD-scid IL2Rγnull). Dosage: 0.7 mg/mouse. Administration: Intraperitoneal injection, 5 days/week, for 5 weeks. Result: Suppressed MPM tumor growth.

In Vitro

HA15 (10 μM; 1-24 hours) induces an early endoplasmic reticulum stress (ER Stress). HA15 (0-10 μM; 24 hours) decreases melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO), with an IC50 of 1-2.5 μM in A375 cells. HA15 (1-10 μM; 24 hours) induces apoptosis in A375 cells. HA15 (1-24 μM; 24 hours) induces autophagy. HA15 (10 μM; 48 hours) has high efficiency in inducing cell death and ER stress in BRAF-inhibitor-resistant melanoma cells. And HA15 inhibits tumor growth through autophagic and apoptotic mechanisms initiated by ER stress. No deleterious effects on the viability of normal human melanocytes or human fibroblasts were observed with low or high doses of HA15. Cell Viability Assay Cell line: A375 cells. Concentration: 1 μM, 2.5 μM, 5 μM, 7.5 μM, 10 μM Incubation time: 24 hours. Result: Decreased melanoma cell viability in a dose-dependent manner compared with control conditions (DMSO) in A375 cells. Apoptosis Analysis. Cell line: A375 cells. Concentration: 1 μM, 5 μM, 10 μM. Incubation time: 24 hours. Result: Induces apoptosis. Cell Autophagy Assay Cell line: A375 cells. Concentration: 1 μM, 4 μM, 10 μM, 24 μM. Incubation time: 24 hours. Result: Increased LC3B-II expression after 1 hour and persisted after 24 hours, enhanced the expression level of Beclin 1, clearly be indicated that induces autophagy. Western blot analysis. Cell line: A375 cells. Concentration: 10 μM. Incubation time: 1 hour, 4 hours, 10 hours, 24 hours. Result: Exhibited a rapid induction within 1 hour of the ER stress markers (phosphorylation of PERK and elF2α and a weak increase in ATF4 and CHOP expression)

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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HA15 | HA-15 | HA 15

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Gene Symbol

GRP78| HSPA5| BiP

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HA15 (orb1223265)

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Clonality:	Recombinant
Conjugation:	Unconjugated

Purity:	95.00%
CAS Number:	1824663-82-2
MW:	~150 kDa

Purity:	99.77%
CAS Number:	1609402-14-3
MW:	466.58
Formula:	C₂₃H₂₂N₄O₃S₂

CAS Number:	1965310-52-4
MW:	763.99
Formula:	C₃₇H₄₅N₇O₅S₃

HA15

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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HA15 (orb1223265)

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